ceritinib [Ligand Id: 7397] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL2403108 (Ceritinib, Ceritinib[mi], LDK-378, LDK378, NVP-LDK-378-NX, NVP-LDK378-NX, Zykadia) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| 26S proteasome regulatory subunit 6B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3831205] [UniProtKB: P43686] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| protein kinase AMP-activated catalytic subunit alpha 1/5`-AMP-activated protein kinase catalytic subunit alpha-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4045] [GtoPdb: 1541] [UniProtKB: Q13131] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| protein kinase AMP-activated non-catalytic subunit gamma 1/5`-AMP-activated protein kinase subunit gamma-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2393] [GtoPdb: 1545] [UniProtKB: P54619] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| protein kinase AMP-activated non-catalytic subunit gamma 2/5`-AMP-activated protein kinase subunit gamma-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2453] [GtoPdb: 1546] [UniProtKB: Q9UGJ0] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| aarF domain containing kinase 1/AarF domain-containing protein kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105885] [GtoPdb: 1925] [UniProtKB: Q86TW2] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Actin-related protein 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6090] [UniProtKB: P61160] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Actin-related protein 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105857] [UniProtKB: P61158] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| tyrosine kinase non receptor 2/Activated CDC42 kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4599] [GtoPdb: 2246] [UniProtKB: Q07912] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 6.03 | pKd | 929 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Inhibition of ACK1 (unknown origin) | B | 7.47 | pIC50 | 33.6 | nM | IC50 | J Med Chem (2021) 64: 16328-16348 [PMID:34735773] |
| activin A receptor type 1/Activin receptor type-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5903] [GtoPdb: 1785] [UniProtKB: Q04771] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| activin A receptor type 1B/Activin receptor type-1B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5310] [GtoPdb: 1787] [UniProtKB: P36896] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| activin A receptor type 2B/Activin receptor type-2B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5466] [GtoPdb: 1792] [UniProtKB: Q13705] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Acyl-CoA dehydrogenase family member 10 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105816] [UniProtKB: Q6JQN1] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Acyl-CoA dehydrogenase family member 11 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105707] [UniProtKB: Q709F0] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Adenine phosphoribosyltransferase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105819] [UniProtKB: P07741] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Adenosine kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3589] [GtoPdb: 1231] [UniProtKB: P55263] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Adenylate kinase 2, mitochondrial in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4938] [UniProtKB: P54819] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Mitochondrial adenine nucleotide translocator 2/ADP/ATP translocase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3709670] [GtoPdb: 1063] [UniProtKB: P05141] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Mitochondrial adenine nucleotide translocator 3/ADP/ATP translocase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105854] [GtoPdb: 1064] [UniProtKB: P12236] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ALK receptor tyrosine kinase/ALK tyrosine kinase receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4247] [GtoPdb: 1839] [UniProtKB: Q9UM73] | ||||||||
| ChEMBL | Binding affinity to wild-type human partial length ALK (I1088 to E1409 residues) expressed in mammalian expression system by KINOMEscan assay | B | 8.89 | pKd | 1.3 | nM | Kd | Eur J Med Chem (2018) 151: 304-314 [PMID:29627725] |
| ChEMBL | Inhibition of ALK (unknown origin) | B | 5.43 | pKi | 3700 | nM | Ki | J Med Chem (2019) 62: 10005-10025 [PMID:31188592] |
| ChEMBL | Inhibition of human N-terminal GST-tagged ALK G1202R mutant cytoplasmic domain (1058 to 1620 residues) expressed in baculovirus expression system after 1 hr by mobility shift assay | B | 4.04 | pIC50 | 91000 | nM | IC50 | Eur J Med Chem (2018) 158: 322-333 [PMID:30223120] |
| ChEMBL | Inhibition of human N-terminal GST-tagged ALK L1196M mutant cytoplasmic domain (1058 to 1620 residues) expressed in baculovirus expression system after 1 hr by mobility shift assay | B | 4.46 | pIC50 | 35000 | nM | IC50 | Eur J Med Chem (2018) 158: 322-333 [PMID:30223120] |
| ChEMBL | Inhibition of human N-terminal GST-tagged ALK cytoplasmic domain (1058 to 1620 residues) expressed in baculovirus expression system after 1 hr by mobility shift assay | B | 5.54 | pIC50 | 2900 | nM | IC50 | Eur J Med Chem (2018) 158: 322-333 [PMID:30223120] |
| ChEMBL | Inhibition of recombinant human N-terminal GST-tagged ALK cytoplasmic domain (1058 to 1620 residues) expressed in baculovirus infected Sf21 cells using kinase substrate22 by mobility shift assay | B | 6.09 | pIC50 | 810 | nM | IC50 | Eur J Med Chem (2021) 212: 113150-113150 [PMID:33453602] |
| ChEMBL | Inhibition of N-terminal GST-tagged human ALK G1202R mutant cytoplasmic domain (1058 to 1620 residues) expressed in baculovirus expression system using srctide as substrate incubated for 1 hr by mobility shift assay | B | 6.7 | pIC50 | 201 | nM | IC50 | Eur J Med Chem (2019) 171: 297-309 [PMID:30927566] |
| ChEMBL | Inhibition of wild-type ALK (unknown origin) | B | 6.7 | pIC50 | 198 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 1514-1517 [PMID:31005443] |
| ChEMBL | Inhibition of recombinant human N-terminal GST-tagged ALK (1058 to 1620 residues) cytoplasmic domain G1202R mutant using srctide as substrate incubated for 1 hr by mobility shift assay | B | 6.71 | pIC50 | 197 | nM | IC50 | Bioorg Med Chem (2019) 27: 115051-115051 [PMID:31492532] |
| ChEMBL | Inhibition of human N-terminal GST-fused ALK G1202R mutant cytoplasmic domain (1058 to 1620 residues) expressed in baculovirus infected Sf21 insect cells using Srctide as substrate measured after 1 hr by mobility shift assay | B | 6.76 | pIC50 | 172 | nM | IC50 | Bioorg Med Chem (2021) 37: 116108-116108 [PMID:33756437] |
| ChEMBL | Inhibition of ALK F1174L mutant (unknown origin) | B | 6.94 | pIC50 | 114.3 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 1514-1517 [PMID:31005443] |
| ChEMBL | Inhibition of ALK G1202R mutant (unknown origin) incubated for 1 hr and measured by mobility shift assay | B | 6.95 | pIC50 | 112 | nM | IC50 | Eur J Med Chem (2022) 241: 114626-114626 [PMID:35939995] |
| ChEMBL | Inhibition of recombinant human N-terminal GST-tagged ALK G1202R mutant (1058 to 1620 residues) expressed in baculovirus expression system using Srctide as substrate incubated for 1 hr by mobility shift assay | B | 6.97 | pIC50 | 108 | nM | IC50 | Eur J Med Chem (2021) 214: 113259-113259 [PMID:33581554] |
| ChEMBL | Inhibition of recombinant human N-terminal GST-tagged ALK cytoplasmic domain (1058 to 1620 residues) G1202R mutant expressed in baculovirus expression system using peptide substrate after 1 hr by mobility shift assay | B | 7.04 | pIC50 | 91 | nM | IC50 | Eur J Med Chem (2018) 143: 123-136 [PMID:29174809] |
| ChEMBL | Inhibition of N-terminal GST-tagged human ceritinib-resistant ALK G1202R mutant (1058 to 1620 residues) cytoplasmic domain expressed in baculovirus infected Sf21 cells incubated for 1 hrs in the presence of ATP by mobility shift assay | B | 7.06 | pIC50 | 87 | nM | IC50 | Eur J Med Chem (2022) 238: 114493-114493 [PMID:35691173] |
| ChEMBL | Inhibition of ALK G1202R mutant (unknown origin) using peptide substrate incubated for 60 mins in presence of ATP by HTRF assay | B | 7.1 | pIC50 | 80 | nM | IC50 | Bioorg Med Chem (2020) 28: 115719-115719 [PMID:33069075] |
| ChEMBL | Inhibition of ALK F1174L mutant auto-phosphorylation in human Kelly cells after 3 hrs by MSD assay | B | 7.1 | pIC50 | 79 | nM | IC50 | J Med Chem (2019) 62: 2618-2637 [PMID:30789735] |
| ChEMBL | Inhibition of ALK L1196M mutant (unknown origin) using peptide as substrate after 60 mins by HTRF assay | B | 7.19 | pIC50 | 64 | nM | IC50 | Eur J Med Chem (2016) 123: 80-89 [PMID:27474925] |
| ChEMBL | Inhibition of ALK L1196M mutant (unknown origin) | B | 7.32 | pIC50 | 47.65 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 1514-1517 [PMID:31005443] |
| ChEMBL | Inhibition of ALK (unknown origin) transfected in mouse BA/F3 cells | B | 7.39 | pIC50 | 40.7 | nM | IC50 | J Med Chem (2013) 56: 5673-5674 [PMID:23837797] |
| ChEMBL | Inhibition of TEL-fused ALK (unknown origin) by cell-based assay | B | 7.39 | pIC50 | 40.7 | nM | IC50 | J Med Chem (2013) 56: 5675-5690 [PMID:23742252] |
| ChEMBL | Inhibition of recombinant human N-terminal GST-tagged ALK cytoplasmic domain (1058 to 1620 residues) L1196M mutant expressed in baculovirus expression system using peptide substrate after 1 hr by mobility shift assay | B | 7.46 | pIC50 | 35 | nM | IC50 | Eur J Med Chem (2018) 143: 123-136 [PMID:29174809] |
| ChEMBL | Inhibition of ALK L1196M mutant (unknown origin) using peptide substrate incubated for 60 mins in presence of ATP by HTRF assay | B | 7.46 | pIC50 | 35 | nM | IC50 | Bioorg Med Chem (2020) 28: 115719-115719 [PMID:33069075] |
| ChEMBL | Inhibition of ALK L1196M mutant (unknown origin) using peptide as substrate measured after 30 mins by fluorescence assay | B | 7.54 | pIC50 | 29 | nM | IC50 | Eur J Med Chem (2017) 126: 536-549 [PMID:27915169] |
| ChEMBL | Inhibition of ALK L1196M mutant (unknown origin) by homogeneous time resolved fluorescence assay | B | 7.54 | pIC50 | 29 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 3992-3998 [PMID:26235945] |
| ChEMBL | Inhibition of ALK L1196M mutant (unknown origin) after 30 mins by HTRF assay | B | 7.54 | pIC50 | 29 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 1720-1725 [PMID:26923695] |
| ChEMBL | Inhibition of ALK L1196M mutant (unknown origin) using TK as substrate after 30 mins by HTRF assay | B | 7.54 | pIC50 | 29 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 2185-2191 [PMID:28385505] |
| ChEMBL | Inhibition of crizotinib-resistant ALK L1196M mutant (unknown origin) using peptide substrate incubated for 30 mins in presence of ATP by fluorescence assay | B | 7.54 | pIC50 | 29 | nM | IC50 | Bioorg Med Chem (2016) 24: 207-219 [PMID:26712094] |
| ChEMBL | Inhibition of human ALK secondary L1196M mutant assessed as decreased enzymatic reactions measured after 1 hr by mobility shift assay | B | 7.57 | pIC50 | 27 | nM | IC50 | Bioorg Med Chem (2021) 47: 116396-116396 [PMID:34534734] |
| ChEMBL | Inhibition of NPM-fused ALK (unknown origin) expressed in mouse BAF3 cells after 2 to 3 days by luciferase reporter gene assay | B | 7.59 | pIC50 | 26 | nM | IC50 | J Med Chem (2013) 56: 5675-5690 [PMID:23742252] |
| ChEMBL | Inhibition of GST-tagged human ALK cytoplasmic domain (1058 to 1620 residues) expressed in baculovirus expression system using Poly G:T (4:1) as substrate after 30 mins by Z-LYTE assay | B | 7.7 | pIC50 | 20 | nM | IC50 | Eur J Med Chem (2017) 136: 497-510 [PMID:28528303] |
| ChEMBL | Inhibition of crizotinib-resistant ALK G1202R mutant (unknown origin) using peptide substrate incubated for 30 mins in presence of ATP by fluorescence assay | B | 7.7 | pIC50 | 20 | nM | IC50 | Bioorg Med Chem (2016) 24: 207-219 [PMID:26712094] |
| ChEMBL | Inhibition of wild type N-terminal GST tagged ALK G1202R mutant cytoplasmic domain (1058 to 1620 end residues) (unknown origin) expressed in Sf21 cells incubated for 1 hr in presence of ATP | B | 7.76 | pIC50 | 17.23 | nM | IC50 | Bioorg Med Chem (2022) 66: 116794-116794 [PMID:35576654] |
| ChEMBL | Inhibition of wild type ALK (unknown origin) after 30 mins by HTRF assay | B | 7.85 | pIC50 | 14 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 1720-1725 [PMID:26923695] |
| ChEMBL | Inhibition of wild type ALK (unknown origin) using TK as substrate after 30 mins by HTRF assay | B | 7.85 | pIC50 | 14 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 2185-2191 [PMID:28385505] |
| ChEMBL | Inhibition of wild type ALK (unknown origin) by homogeneous time resolved fluorescence assay | B | 7.85 | pIC50 | 14 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 3992-3998 [PMID:26235945] |
| ChEMBL | Inhibition of ALK (unknown origin) using peptide substrate incubated for 30 mins in presence of ATP by fluorescence assay | B | 7.85 | pIC50 | 14 | nM | IC50 | Bioorg Med Chem (2016) 24: 207-219 [PMID:26712094] |
| ChEMBL | Inhibition of wild-type ALK (unknown origin) using peptide as substrate measured after 30 mins by fluorescence assay | B | 7.85 | pIC50 | 14 | nM | IC50 | Eur J Med Chem (2017) 126: 536-549 [PMID:27915169] |
| ChEMBL | Inhibition of ALK G1202R mutant (unknown origin) using peptide as substrate measured after 30 mins by fluorescence assay | B | 7.89 | pIC50 | 13 | nM | IC50 | Eur J Med Chem (2017) 126: 536-549 [PMID:27915169] |
| ChEMBL | Inhibition of recombinant human N-terminal GST-tagged ALK L1196M mutant (1058 to 1620 residues) expressed in baculovirus expression system using Srctide as substrate incubated for 1 hr by mobility shift assay | B | 7.89 | pIC50 | 12.9 | nM | IC50 | Eur J Med Chem (2021) 214: 113259-113259 [PMID:33581554] |
| ChEMBL | Inhibition of ALK L1196M mutant (unknown origin) incubated for 1 hr and measured by mobility shift assay | B | 7.99 | pIC50 | 10.3 | nM | IC50 | Eur J Med Chem (2022) 241: 114626-114626 [PMID:35939995] |
| ChEMBL | Inhibition of ALK L1196M mutant (unknown origin) | B | 8.01 | pIC50 | 9.7 | nM | IC50 | Bioorg Med Chem Lett (2022) 75: 128990-128990 [PMID:36113668] |
| ChEMBL | Inhibition of N-terminal GST-tagged human ceritinib-resistant ALK L1196M mutant (1058 to 1620 residues) cytoplasmic domain expressed in baculovirus infected Sf21 cells incubated for 1 hrs in the presence of ATP by mobility shift assay | B | 8.02 | pIC50 | 9.6 | nM | IC50 | Eur J Med Chem (2022) 238: 114493-114493 [PMID:35691173] |
| ChEMBL | Inhibition of human N-terminal GST-fused ALK L1196M mutant cytoplasmic domain (1058 to 1620 residues) expressed in baculovirus infected Sf21 insect cells using Srctide as substrate measured after 1 hr by mobility shift assay | B | 8.12 | pIC50 | 7.6 | nM | IC50 | Bioorg Med Chem (2021) 37: 116108-116108 [PMID:33756437] |
| ChEMBL | Inhibition of ALK L1196M (unknown origin) incubated for 1 hr | B | 8.13 | pIC50 | 7.4 | nM | IC50 | Bioorg Med Chem (2020) 28: 115715-115715 [PMID:33069079] |
| ChEMBL | The determination of IC50 of the inhibiting effect to kinase ALK: 96-well plates was coated under 37° C. with coating buffer (125 μl/well) overnight, and coating buffer was polypeptide substrate [Poly (4:1 Glu, Tyr) Peptide, available from SignalChem] containing 2.5 μg/well ALK kinase in PBS. Then, each well was washed with 200 μl of buffer (PBS containing 0.05% Tween 80), and placed at 37° C. for at least 2 hours to dryness.Serial diluted test compounds in different concentrations (compounds prepared in any one of Examples 1 to 16, dissolved in DMSO) were added to each well in 5 μl/well, followed by addition of kinase buffer (25 mM Hepes, pH 7.5, 5 mM MnCl2, 5 mM MgCl2), 0.3 mM ATP, and 100 ng/well recombinant human ALK (Abnova Corporation), to a total volume of 100 μl each well. After kept at 30° C. for 15 minutes, the reaction mixture was removed, and washed with 200 μl of wash buffer (PBS containing 0.05% Tween 80) for 5 times.100 μl/well of mouse anti-phosphotyrosine monoclonal antibody (clone 4G10, purchased from EMD Millipore Corporation) were used in the detection of phosphorylated peptide substrate. Monoclonal antibody was diluted at 1:500 with PBS containing 4% bovine serum albumin. After incubated at room temperature for 30 minutes, the antibody solution was removed, and each well was washed with 200 μl of wash buffer (PBS containing 0.05% Tween 80) for 5 times.100 μl/well of secondary antibody (anti-mouse IgG) was added. The secondary antibody was diluted at 1:1000 with PBS containing 4% bovine serum albumin, incubated for 30 minutes at room temperature; and the wells were washed again as said above.100 μl/well of TMB substrate solution was used for color development, and the same volume of 0.18 M H2SO4 was added to terminate the color development. Finally, the absorbance at 450 nm or 490 nm was read, and the IC50 was calculated. | B | 8.3 | pIC50 | <5 | nM | IC50 | US-10618884-B2. Deuterated diaminopyrimidine compounds and pharmaceutical compositions comprising such compounds (2020) |
| ChEMBL | The determination of IC50 of the inhibiting effect to kinase ALK: 96-well plates was coated under 37° C. with coating buffer (125 μl/well) overnight, and coating buffer was polypeptide substrate [Poly (4:1 Glu, Tyr) Peptide, available from SignalChem] containing 2.5 μg/well ALK kinase in PBS. Then, each well was washed with 200 μl of buffer (PBS containing 0.05% Tween 80), and placed at 37° C. for at least 2 hours to dryness.Serial diluted test compounds in different concentrations (compounds prepared in any one of Examples 1 to 16, dissolved in DMSO) were added to each well in 5 μl/well, followed by addition of kinase buffer (25 mM Hepes, pH 7.5, 5 mM MnCl2, 5 mM MgCl2), 0.3 mM ATP, and 100 ng/well recombinant human ALK (Abnova Corporation), to a total volume of 100 μl each well. After kept at 30° C. for 15 minutes, the reaction mixture was removed, and washed with 200 μl of wash buffer (PBS containing 0.05% Tween 80) for 5 times.100 μl/well of mouse anti-phosphotyrosine monoclonal antibody (clone 4G10, purchased from EMD Millipore Corporation) were used in the detection of phosphorylated peptide substrate. Monoclonal antibody was diluted at 1:500 with PBS containing 4% bovine serum albumin. After incubated at room temperature for 30 minutes, the antibody solution was removed, and each well was washed with 200 μl of wash buffer (PBS containing 0.05% Tween 80) for 5 times.100 μl/well of secondary antibody (anti-mouse IgG) was added. The secondary antibody was diluted at 1:1000 with PBS containing 4% bovine serum albumin, incubated for 30 minutes at room temperature; and the wells were washed again as said above.100 μl/well of TMB substrate solution was used for color development, and the same volume of 0.18 M H2SO4 was added to terminate the color development. Finally, the absorbance at 450 nm or 490 nm was read, and the IC50 was calculated. | B | 8.3 | pIC50 | <5 | nM | IC50 | US-10618884-B2. Deuterated diaminopyrimidine compounds and pharmaceutical compositions comprising such compounds (2020) |
| ChEMBL | The determination of IC50 of the inhibiting effect to kinase ALK: 96-well plates was coated under 37° C. with coating buffer (125 μl/well) overnight, and coating buffer was polypeptide substrate [Poly (4:1 Glu, Tyr) Peptide, available from SignalChem] containing 2.5 μg/well ALK kinase in PBS. Then, each well was washed with 200 μl of buffer (PBS containing 0.05% Tween 80), and placed at 37° C. for at least 2 hours to dryness.Serial diluted test compounds in different concentrations (compounds prepared in any one of Examples 1 to 16, dissolved in DMSO) were added to each well in 5 μl/well, followed by addition of kinase buffer (25 mM Hepes, pH 7.5, 5 mM MnCl2, 5 mM MgCl2), 0.3 mM ATP, and 100 ng/well recombinant human ALK (Abnova Corporation), to a total volume of 100 μl each well. After kept at 30° C. for 15 minutes, the reaction mixture was removed, and washed with 200 μl of wash buffer (PBS containing 0.05% Tween 80) for 5 times.100 μl/well of mouse anti-phosphotyrosine monoclonal antibody (clone 4G10, purchased from EMD Millipore Corporation) were used in the detection of phosphorylated peptide substrate. Monoclonal antibody was diluted at 1:500 with PBS containing 4% bovine serum albumin. After incubated at room temperature for 30 minutes, the antibody solution was removed, and each well was washed with 200 μl of wash buffer (PBS containing 0.05% Tween 80) for 5 times.100 μl/well of secondary antibody (anti-mouse IgG) was added. The secondary antibody was diluted at 1:1000 with PBS containing 4% bovine serum albumin, incubated for 30 minutes at room temperature; and the wells were washed again as said above.100 μl/well of TMB substrate solution was used for color development, and the same volume of 0.18 M H2SO4 was added to terminate the color development. Finally, the absorbance at 450 nm or 490 nm was read, and the IC50 was calculated. | B | 8.3 | pIC50 | <5 | nM | IC50 | US-10618884-B2. Deuterated diaminopyrimidine compounds and pharmaceutical compositions comprising such compounds (2020) |
| ChEMBL | In Vitro assay: The determination of IC50 of the inhibiting effect to kinase ALK 96-well plates was coated under 37° C. with coating buffer (125 ul/well) overnight, and coating buffer was polypeptide substrate [Poly (4:1 Glu, Tyr) Peptide, available from SignalChem] containing 2.5 ug/well ALK kinase in PBS. Then, each well was washed with 200 ul of buffer (PBS containing 0.05% Tween 80), and placed at 37° C. for at least 2 hours to dryness. Serial diluted test compounds in different concentrations (compounds prepared in any one of Examples 1 to 16, dissolved in DMSO) were added to each well in 5/well, followed by addition of kinase buffer (25 mM Hepes, pH 7.5, 5 mM MnCl2, 5 mM MgCl2), 0.3 mM ATP, and 100 ng/well recombinant human ALK (Abnova Corporation), to a total volume of 100 ul each well. After kept at 30° C. for 15 minutes, the reaction mixture was removed, and washed with 200 ul of wash buffer (PBS containing 0.05% Tween 80) for 5 times. | B | 8.3 | pIC50 | <5 | nM | IC50 | US-9809572-B2. Deuterated diaminopyrimidine compounds and pharmaceutical compositions comprising such compounds (2017) |
| ChEMBL | In Vitro assay: The determination of IC50 of the inhibiting effect to kinase ALK 96-well plates was coated under 37° C. with coating buffer (125 ul/well) overnight, and coating buffer was polypeptide substrate [Poly (4:1 Glu, Tyr) Peptide, available from SignalChem] containing 2.5 ug/well ALK kinase in PBS. Then, each well was washed with 200 ul of buffer (PBS containing 0.05% Tween 80), and placed at 37° C. for at least 2 hours to dryness. Serial diluted test compounds in different concentrations (compounds prepared in any one of Examples 1 to 16, dissolved in DMSO) were added to each well in 5/well, followed by addition of kinase buffer (25 mM Hepes, pH 7.5, 5 mM MnCl2, 5 mM MgCl2), 0.3 mM ATP, and 100 ng/well recombinant human ALK (Abnova Corporation), to a total volume of 100 ul each well. After kept at 30° C. for 15 minutes, the reaction mixture was removed, and washed with 200 ul of wash buffer (PBS containing 0.05% Tween 80) for 5 times. | B | 8.3 | pIC50 | <5 | nM | IC50 | US-9809572-B2. Deuterated diaminopyrimidine compounds and pharmaceutical compositions comprising such compounds (2017) |
| ChEMBL | In Vitro assay: The determination of IC50 of the inhibiting effect to kinase ALK 96-well plates was coated under 37° C. with coating buffer (125 ul/well) overnight, and coating buffer was polypeptide substrate [Poly (4:1 Glu, Tyr) Peptide, available from SignalChem] containing 2.5 ug/well ALK kinase in PBS. Then, each well was washed with 200 ul of buffer (PBS containing 0.05% Tween 80), and placed at 37° C. for at least 2 hours to dryness. Serial diluted test compounds in different concentrations (compounds prepared in any one of Examples 1 to 16, dissolved in DMSO) were added to each well in 5/well, followed by addition of kinase buffer (25 mM Hepes, pH 7.5, 5 mM MnCl2, 5 mM MgCl2), 0.3 mM ATP, and 100 ng/well recombinant human ALK (Abnova Corporation), to a total volume of 100 ul each well. After kept at 30° C. for 15 minutes, the reaction mixture was removed, and washed with 200 ul of wash buffer (PBS containing 0.05% Tween 80) for 5 times. | B | 8.3 | pIC50 | <5 | nM | IC50 | US-9809572-B2. Deuterated diaminopyrimidine compounds and pharmaceutical compositions comprising such compounds (2017) |
| ChEMBL | In Vitro assay: The determination of IC50 of the inhibiting effect to kinase ALK 96-well plates was coated under 37° C. with coating buffer (125 ul/well) overnight, and coating buffer was polypeptide substrate [Poly (4:1 Glu, Tyr) Peptide, available from SignalChem] containing 2.5 ug/well ALK kinase in PBS. Then, each well was washed with 200 ul of buffer (PBS containing 0.05% Tween 80), and placed at 37° C. for at least 2 hours to dryness. Serial diluted test compounds in different concentrations (compounds prepared in any one of Examples 1 to 16, dissolved in DMSO) were added to each well in 5/well, followed by addition of kinase buffer (25 mM Hepes, pH 7.5, 5 mM MnCl2, 5 mM MgCl2), 0.3 mM ATP, and 100 ng/well recombinant human ALK (Abnova Corporation), to a total volume of 100 ul each well. After kept at 30° C. for 15 minutes, the reaction mixture was removed, and washed with 200 ul of wash buffer (PBS containing 0.05% Tween 80) for 5 times. | B | 8.3 | pIC50 | <5 | nM | IC50 | US-9809572-B2. Deuterated diaminopyrimidine compounds and pharmaceutical compositions comprising such compounds (2017) |
| ChEMBL | The determination of IC50 of the inhibiting effect to kinase ALK: 96-well plates was coated under 37° C. with coating buffer (125 μl/well) overnight, and coating buffer was polypeptide substrate [Poly (4:1 Glu, Tyr) Peptide, available from SignalChem] containing 2.5 μg/well ALK kinase in PBS. Then, each well was washed with 200 μl of buffer (PBS containing 0.05% Tween 80), and placed at 37° C. for at least 2 hours to dryness.Serial diluted test compounds in different concentrations (compounds prepared in any one of Examples 1 to 16, dissolved in DMSO) were added to each well in 5 μl/well, followed by addition of kinase buffer (25 mM Hepes, pH 7.5, 5 mM MnCl2, 5 mM MgCl2), 0.3 mM ATP, and 100 ng/well recombinant human ALK (Abnova Corporation), to a total volume of 100 μl each well. After kept at 30° C. for 15 minutes, the reaction mixture was removed, and washed with 200 μl of wash buffer (PBS containing 0.05% Tween 80) for 5 times.100 μl/well of mouse anti-phosphotyrosine monoclonal antibody (clone 4G10, purchased from EMD Millipore Corporation) were used in the detection of phosphorylated peptide substrate. Monoclonal antibody was diluted at 1:500 with PBS containing 4% bovine serum albumin. After incubated at room temperature for 30 minutes, the antibody solution was removed, and each well was washed with 200 μl of wash buffer (PBS containing 0.05% Tween 80) for 5 times.100 μl/well of secondary antibody (anti-mouse IgG) was added. The secondary antibody was diluted at 1:1000 with PBS containing 4% bovine serum albumin, incubated for 30 minutes at room temperature; and the wells were washed again as said above.100 μl/well of TMB substrate solution was used for color development, and the same volume of 0.18 M H2SO4 was added to terminate the color development. Finally, the absorbance at 450 nm or 490 nm was read, and the IC50 was calculated. | B | 8.3 | pIC50 | <5 | nM | IC50 | US-10618884-B2. Deuterated diaminopyrimidine compounds and pharmaceutical compositions comprising such compounds (2020) |
| ChEMBL | The determination of IC50 of the inhibiting effect to kinase ALK: 96-well plates was coated under 37° C. with coating buffer (125 μl/well) overnight, and coating buffer was polypeptide substrate [Poly (4:1 Glu, Tyr) Peptide, available from SignalChem] containing 2.5 μg/well ALK kinase in PBS. Then, each well was washed with 200 μl of buffer (PBS containing 0.05% Tween 80), and placed at 37° C. for at least 2 hours to dryness.Serial diluted test compounds in different concentrations (compounds prepared in any one of Examples 1 to 16, dissolved in DMSO) were added to each well in 5 μl/well, followed by addition of kinase buffer (25 mM Hepes, pH 7.5, 5 mM MnCl2, 5 mM MgCl2), 0.3 mM ATP, and 100 ng/well recombinant human ALK (Abnova Corporation), to a total volume of 100 μl each well. After kept at 30° C. for 15 minutes, the reaction mixture was removed, and washed with 200 μl of wash buffer (PBS containing 0.05% Tween 80) for 5 times.100 μl/well of mouse anti-phosphotyrosine monoclonal antibody (clone 4G10, purchased from EMD Millipore Corporation) were used in the detection of phosphorylated peptide substrate. Monoclonal antibody was diluted at 1:500 with PBS containing 4% bovine serum albumin. After incubated at room temperature for 30 minutes, the antibody solution was removed, and each well was washed with 200 μl of wash buffer (PBS containing 0.05% Tween 80) for 5 times.100 μl/well of secondary antibody (anti-mouse IgG) was added. The secondary antibody was diluted at 1:1000 with PBS containing 4% bovine serum albumin, incubated for 30 minutes at room temperature; and the wells were washed again as said above.100 μl/well of TMB substrate solution was used for color development, and the same volume of 0.18 M H2SO4 was added to terminate the color development. Finally, the absorbance at 450 nm or 490 nm was read, and the IC50 was calculated. | B | 8.3 | pIC50 | <5 | nM | IC50 | US-10618884-B2. Deuterated diaminopyrimidine compounds and pharmaceutical compositions comprising such compounds (2020) |
| ChEMBL | The determination of IC50 of the inhibiting effect to kinase ALK: 96-well plates was coated under 37° C. with coating buffer (125 μl/well) overnight, and coating buffer was polypeptide substrate [Poly (4:1 Glu, Tyr) Peptide, available from SignalChem] containing 2.5 μg/well ALK kinase in PBS. Then, each well was washed with 200 μl of buffer (PBS containing 0.05% Tween 80), and placed at 37° C. for at least 2 hours to dryness.Serial diluted test compounds in different concentrations (compounds prepared in any one of Examples 1 to 16, dissolved in DMSO) were added to each well in 5 μl/well, followed by addition of kinase buffer (25 mM Hepes, pH 7.5, 5 mM MnCl2, 5 mM MgCl2), 0.3 mM ATP, and 100 ng/well recombinant human ALK (Abnova Corporation), to a total volume of 100 μl each well. After kept at 30° C. for 15 minutes, the reaction mixture was removed, and washed with 200 μl of wash buffer (PBS containing 0.05% Tween 80) for 5 times.100 μl/well of mouse anti-phosphotyrosine monoclonal antibody (clone 4G10, purchased from EMD Millipore Corporation) were used in the detection of phosphorylated peptide substrate. Monoclonal antibody was diluted at 1:500 with PBS containing 4% bovine serum albumin. After incubated at room temperature for 30 minutes, the antibody solution was removed, and each well was washed with 200 μl of wash buffer (PBS containing 0.05% Tween 80) for 5 times.100 μl/well of secondary antibody (anti-mouse IgG) was added. The secondary antibody was diluted at 1:1000 with PBS containing 4% bovine serum albumin, incubated for 30 minutes at room temperature; and the wells were washed again as said above.100 μl/well of TMB substrate solution was used for color development, and the same volume of 0.18 M H2SO4 was added to terminate the color development. Finally, the absorbance at 450 nm or 490 nm was read, and the IC50 was calculated. | B | 8.3 | pIC50 | <5 | nM | IC50 | US-10618884-B2. Deuterated diaminopyrimidine compounds and pharmaceutical compositions comprising such compounds (2020) |
| ChEMBL | The determination of IC50 of the inhibiting effect to kinase ALK: 96-well plates was coated under 37° C. with coating buffer (125 μl/well) overnight, and coating buffer was polypeptide substrate [Poly (4:1 Glu, Tyr) Peptide, available from SignalChem] containing 2.5 μg/well ALK kinase in PBS. Then, each well was washed with 200 μl of buffer (PBS containing 0.05% Tween 80), and placed at 37° C. for at least 2 hours to dryness.Serial diluted test compounds in different concentrations (compounds prepared in any one of Examples 1 to 16, dissolved in DMSO) were added to each well in 5 μl/well, followed by addition of kinase buffer (25 mM Hepes, pH 7.5, 5 mM MnCl2, 5 mM MgCl2), 0.3 mM ATP, and 100 ng/well recombinant human ALK (Abnova Corporation), to a total volume of 100 μl each well. After kept at 30° C. for 15 minutes, the reaction mixture was removed, and washed with 200 μl of wash buffer (PBS containing 0.05% Tween 80) for 5 times.100 μl/well of mouse anti-phosphotyrosine monoclonal antibody (clone 4G10, purchased from EMD Millipore Corporation) were used in the detection of phosphorylated peptide substrate. Monoclonal antibody was diluted at 1:500 with PBS containing 4% bovine serum albumin. After incubated at room temperature for 30 minutes, the antibody solution was removed, and each well was washed with 200 μl of wash buffer (PBS containing 0.05% Tween 80) for 5 times.100 μl/well of secondary antibody (anti-mouse IgG) was added. The secondary antibody was diluted at 1:1000 with PBS containing 4% bovine serum albumin, incubated for 30 minutes at room temperature; and the wells were washed again as said above.100 μl/well of TMB substrate solution was used for color development, and the same volume of 0.18 M H2SO4 was added to terminate the color development. Finally, the absorbance at 450 nm or 490 nm was read, and the IC50 was calculated. | B | 8.3 | pIC50 | <5 | nM | IC50 | US-10618884-B2. Deuterated diaminopyrimidine compounds and pharmaceutical compositions comprising such compounds (2020) |
| ChEMBL | The determination of IC50 of the inhibiting effect to kinase ALK: 96-well plates was coated under 37° C. with coating buffer (125 μl/well) overnight, and coating buffer was polypeptide substrate [Poly (4:1 Glu, Tyr) Peptide, available from SignalChem] containing 2.5 μg/well ALK kinase in PBS. Then, each well was washed with 200 μl of buffer (PBS containing 0.05% Tween 80), and placed at 37° C. for at least 2 hours to dryness.Serial diluted test compounds in different concentrations (compounds prepared in any one of Examples 1 to 16, dissolved in DMSO) were added to each well in 5 μl/well, followed by addition of kinase buffer (25 mM Hepes, pH 7.5, 5 mM MnCl2, 5 mM MgCl2), 0.3 mM ATP, and 100 ng/well recombinant human ALK (Abnova Corporation), to a total volume of 100 μl each well. After kept at 30° C. for 15 minutes, the reaction mixture was removed, and washed with 200 μl of wash buffer (PBS containing 0.05% Tween 80) for 5 times.100 μl/well of mouse anti-phosphotyrosine monoclonal antibody (clone 4G10, purchased from EMD Millipore Corporation) were used in the detection of phosphorylated peptide substrate. Monoclonal antibody was diluted at 1:500 with PBS containing 4% bovine serum albumin. After incubated at room temperature for 30 minutes, the antibody solution was removed, and each well was washed with 200 μl of wash buffer (PBS containing 0.05% Tween 80) for 5 times.100 μl/well of secondary antibody (anti-mouse IgG) was added. The secondary antibody was diluted at 1:1000 with PBS containing 4% bovine serum albumin, incubated for 30 minutes at room temperature; and the wells were washed again as said above.100 μl/well of TMB substrate solution was used for color development, and the same volume of 0.18 M H2SO4 was added to terminate the color development. Finally, the absorbance at 450 nm or 490 nm was read, and the IC50 was calculated. | B | 8.3 | pIC50 | <5 | nM | IC50 | US-10618884-B2. Deuterated diaminopyrimidine compounds and pharmaceutical compositions comprising such compounds (2020) |
| ChEMBL | The determination of IC50 of the inhibiting effect to kinase ALK: 96-well plates was coated under 37° C. with coating buffer (125 μl/well) overnight, and coating buffer was polypeptide substrate [Poly (4:1 Glu, Tyr) Peptide, available from SignalChem] containing 2.5 μg/well ALK kinase in PBS. Then, each well was washed with 200 μl of buffer (PBS containing 0.05% Tween 80), and placed at 37° C. for at least 2 hours to dryness.Serial diluted test compounds in different concentrations (compounds prepared in any one of Examples 1 to 16, dissolved in DMSO) were added to each well in 5 μl/well, followed by addition of kinase buffer (25 mM Hepes, pH 7.5, 5 mM MnCl2, 5 mM MgCl2), 0.3 mM ATP, and 100 ng/well recombinant human ALK (Abnova Corporation), to a total volume of 100 μl each well. After kept at 30° C. for 15 minutes, the reaction mixture was removed, and washed with 200 μl of wash buffer (PBS containing 0.05% Tween 80) for 5 times.100 μl/well of mouse anti-phosphotyrosine monoclonal antibody (clone 4G10, purchased from EMD Millipore Corporation) were used in the detection of phosphorylated peptide substrate. Monoclonal antibody was diluted at 1:500 with PBS containing 4% bovine serum albumin. After incubated at room temperature for 30 minutes, the antibody solution was removed, and each well was washed with 200 μl of wash buffer (PBS containing 0.05% Tween 80) for 5 times.100 μl/well of secondary antibody (anti-mouse IgG) was added. The secondary antibody was diluted at 1:1000 with PBS containing 4% bovine serum albumin, incubated for 30 minutes at room temperature; and the wells were washed again as said above.100 μl/well of TMB substrate solution was used for color development, and the same volume of 0.18 M H2SO4 was added to terminate the color development. Finally, the absorbance at 450 nm or 490 nm was read, and the IC50 was calculated. | B | 8.3 | pIC50 | <5 | nM | IC50 | US-10618884-B2. Deuterated diaminopyrimidine compounds and pharmaceutical compositions comprising such compounds (2020) |
| ChEMBL | The determination of IC50 of the inhibiting effect to kinase ALK: 96-well plates was coated under 37° C. with coating buffer (125 μl/well) overnight, and coating buffer was polypeptide substrate [Poly (4:1 Glu, Tyr) Peptide, available from SignalChem] containing 2.5 μg/well ALK kinase in PBS. Then, each well was washed with 200 μl of buffer (PBS containing 0.05% Tween 80), and placed at 37° C. for at least 2 hours to dryness.Serial diluted test compounds in different concentrations (compounds prepared in any one of Examples 1 to 16, dissolved in DMSO) were added to each well in 5 μl/well, followed by addition of kinase buffer (25 mM Hepes, pH 7.5, 5 mM MnCl2, 5 mM MgCl2), 0.3 mM ATP, and 100 ng/well recombinant human ALK (Abnova Corporation), to a total volume of 100 μl each well. After kept at 30° C. for 15 minutes, the reaction mixture was removed, and washed with 200 μl of wash buffer (PBS containing 0.05% Tween 80) for 5 times.100 μl/well of mouse anti-phosphotyrosine monoclonal antibody (clone 4G10, purchased from EMD Millipore Corporation) were used in the detection of phosphorylated peptide substrate. Monoclonal antibody was diluted at 1:500 with PBS containing 4% bovine serum albumin. After incubated at room temperature for 30 minutes, the antibody solution was removed, and each well was washed with 200 μl of wash buffer (PBS containing 0.05% Tween 80) for 5 times.100 μl/well of secondary antibody (anti-mouse IgG) was added. The secondary antibody was diluted at 1:1000 with PBS containing 4% bovine serum albumin, incubated for 30 minutes at room temperature; and the wells were washed again as said above.100 μl/well of TMB substrate solution was used for color development, and the same volume of 0.18 M H2SO4 was added to terminate the color development. Finally, the absorbance at 450 nm or 490 nm was read, and the IC50 was calculated. | B | 8.3 | pIC50 | <5 | nM | IC50 | US-10618884-B2. Deuterated diaminopyrimidine compounds and pharmaceutical compositions comprising such compounds (2020) |
| ChEMBL | The determination of IC50 of the inhibiting effect to kinase ALK: 96-well plates was coated under 37° C. with coating buffer (125 μl/well) overnight, and coating buffer was polypeptide substrate [Poly (4:1 Glu, Tyr) Peptide, available from SignalChem] containing 2.5 μg/well ALK kinase in PBS. Then, each well was washed with 200 μl of buffer (PBS containing 0.05% Tween 80), and placed at 37° C. for at least 2 hours to dryness.Serial diluted test compounds in different concentrations (compounds prepared in any one of Examples 1 to 16, dissolved in DMSO) were added to each well in 5 μl/well, followed by addition of kinase buffer (25 mM Hepes, pH 7.5, 5 mM MnCl2, 5 mM MgCl2), 0.3 mM ATP, and 100 ng/well recombinant human ALK (Abnova Corporation), to a total volume of 100 μl each well. After kept at 30° C. for 15 minutes, the reaction mixture was removed, and washed with 200 μl of wash buffer (PBS containing 0.05% Tween 80) for 5 times.100 μl/well of mouse anti-phosphotyrosine monoclonal antibody (clone 4G10, purchased from EMD Millipore Corporation) were used in the detection of phosphorylated peptide substrate. Monoclonal antibody was diluted at 1:500 with PBS containing 4% bovine serum albumin. After incubated at room temperature for 30 minutes, the antibody solution was removed, and each well was washed with 200 μl of wash buffer (PBS containing 0.05% Tween 80) for 5 times.100 μl/well of secondary antibody (anti-mouse IgG) was added. The secondary antibody was diluted at 1:1000 with PBS containing 4% bovine serum albumin, incubated for 30 minutes at room temperature; and the wells were washed again as said above.100 μl/well of TMB substrate solution was used for color development, and the same volume of 0.18 M H2SO4 was added to terminate the color development. Finally, the absorbance at 450 nm or 490 nm was read, and the IC50 was calculated. | B | 8.3 | pIC50 | <5 | nM | IC50 | US-10618884-B2. Deuterated diaminopyrimidine compounds and pharmaceutical compositions comprising such compounds (2020) |
| ChEMBL | The determination of IC50 of the inhibiting effect to kinase ALK: 96-well plates was coated under 37° C. with coating buffer (125 μl/well) overnight, and coating buffer was polypeptide substrate [Poly (4:1 Glu, Tyr) Peptide, available from SignalChem] containing 2.5 μg/well ALK kinase in PBS. Then, each well was washed with 200 μl of buffer (PBS containing 0.05% Tween 80), and placed at 37° C. for at least 2 hours to dryness.Serial diluted test compounds in different concentrations (compounds prepared in any one of Examples 1 to 16, dissolved in DMSO) were added to each well in 5 μl/well, followed by addition of kinase buffer (25 mM Hepes, pH 7.5, 5 mM MnCl2, 5 mM MgCl2), 0.3 mM ATP, and 100 ng/well recombinant human ALK (Abnova Corporation), to a total volume of 100 μl each well. After kept at 30° C. for 15 minutes, the reaction mixture was removed, and washed with 200 μl of wash buffer (PBS containing 0.05% Tween 80) for 5 times.100 μl/well of mouse anti-phosphotyrosine monoclonal antibody (clone 4G10, purchased from EMD Millipore Corporation) were used in the detection of phosphorylated peptide substrate. Monoclonal antibody was diluted at 1:500 with PBS containing 4% bovine serum albumin. After incubated at room temperature for 30 minutes, the antibody solution was removed, and each well was washed with 200 μl of wash buffer (PBS containing 0.05% Tween 80) for 5 times.100 μl/well of secondary antibody (anti-mouse IgG) was added. The secondary antibody was diluted at 1:1000 with PBS containing 4% bovine serum albumin, incubated for 30 minutes at room temperature; and the wells were washed again as said above.100 μl/well of TMB substrate solution was used for color development, and the same volume of 0.18 M H2SO4 was added to terminate the color development. Finally, the absorbance at 450 nm or 490 nm was read, and the IC50 was calculated. | B | 8.3 | pIC50 | <5 | nM | IC50 | US-10618884-B2. Deuterated diaminopyrimidine compounds and pharmaceutical compositions comprising such compounds (2020) |
| ChEMBL | The determination of IC50 of the inhibiting effect to kinase ALK: 96-well plates was coated under 37° C. with coating buffer (125 μl/well) overnight, and coating buffer was polypeptide substrate [Poly (4:1 Glu, Tyr) Peptide, available from SignalChem] containing 2.5 μg/well ALK kinase in PBS. Then, each well was washed with 200 μl of buffer (PBS containing 0.05% Tween 80), and placed at 37° C. for at least 2 hours to dryness.Serial diluted test compounds in different concentrations (compounds prepared in any one of Examples 1 to 16, dissolved in DMSO) were added to each well in 5 μl/well, followed by addition of kinase buffer (25 mM Hepes, pH 7.5, 5 mM MnCl2, 5 mM MgCl2), 0.3 mM ATP, and 100 ng/well recombinant human ALK (Abnova Corporation), to a total volume of 100 μl each well. After kept at 30° C. for 15 minutes, the reaction mixture was removed, and washed with 200 μl of wash buffer (PBS containing 0.05% Tween 80) for 5 times.100 μl/well of mouse anti-phosphotyrosine monoclonal antibody (clone 4G10, purchased from EMD Millipore Corporation) were used in the detection of phosphorylated peptide substrate. Monoclonal antibody was diluted at 1:500 with PBS containing 4% bovine serum albumin. After incubated at room temperature for 30 minutes, the antibody solution was removed, and each well was washed with 200 μl of wash buffer (PBS containing 0.05% Tween 80) for 5 times.100 μl/well of secondary antibody (anti-mouse IgG) was added. The secondary antibody was diluted at 1:1000 with PBS containing 4% bovine serum albumin, incubated for 30 minutes at room temperature; and the wells were washed again as said above.100 μl/well of TMB substrate solution was used for color development, and the same volume of 0.18 M H2SO4 was added to terminate the color development. Finally, the absorbance at 450 nm or 490 nm was read, and the IC50 was calculated. | B | 8.3 | pIC50 | <5 | nM | IC50 | US-10618884-B2. Deuterated diaminopyrimidine compounds and pharmaceutical compositions comprising such compounds (2020) |
| ChEMBL | The determination of IC50 of the inhibiting effect to kinase ALK: 96-well plates was coated under 37° C. with coating buffer (125 μl/well) overnight, and coating buffer was polypeptide substrate [Poly (4:1 Glu, Tyr) Peptide, available from SignalChem] containing 2.5 μg/well ALK kinase in PBS. Then, each well was washed with 200 μl of buffer (PBS containing 0.05% Tween 80), and placed at 37° C. for at least 2 hours to dryness.Serial diluted test compounds in different concentrations (compounds prepared in any one of Examples 1 to 16, dissolved in DMSO) were added to each well in 5 μl/well, followed by addition of kinase buffer (25 mM Hepes, pH 7.5, 5 mM MnCl2, 5 mM MgCl2), 0.3 mM ATP, and 100 ng/well recombinant human ALK (Abnova Corporation), to a total volume of 100 μl each well. After kept at 30° C. for 15 minutes, the reaction mixture was removed, and washed with 200 μl of wash buffer (PBS containing 0.05% Tween 80) for 5 times.100 μl/well of mouse anti-phosphotyrosine monoclonal antibody (clone 4G10, purchased from EMD Millipore Corporation) were used in the detection of phosphorylated peptide substrate. Monoclonal antibody was diluted at 1:500 with PBS containing 4% bovine serum albumin. After incubated at room temperature for 30 minutes, the antibody solution was removed, and each well was washed with 200 μl of wash buffer (PBS containing 0.05% Tween 80) for 5 times.100 μl/well of secondary antibody (anti-mouse IgG) was added. The secondary antibody was diluted at 1:1000 with PBS containing 4% bovine serum albumin, incubated for 30 minutes at room temperature; and the wells were washed again as said above.100 μl/well of TMB substrate solution was used for color development, and the same volume of 0.18 M H2SO4 was added to terminate the color development. Finally, the absorbance at 450 nm or 490 nm was read, and the IC50 was calculated. | B | 8.3 | pIC50 | <5 | nM | IC50 | US-10618884-B2. Deuterated diaminopyrimidine compounds and pharmaceutical compositions comprising such compounds (2020) |
| ChEMBL | The determination of IC50 of the inhibiting effect to kinase ALK: 96-well plates was coated under 37° C. with coating buffer (125 μl/well) overnight, and coating buffer was polypeptide substrate [Poly (4:1 Glu, Tyr) Peptide, available from SignalChem] containing 2.5 μg/well ALK kinase in PBS. Then, each well was washed with 200 μl of buffer (PBS containing 0.05% Tween 80), and placed at 37° C. for at least 2 hours to dryness.Serial diluted test compounds in different concentrations (compounds prepared in any one of Examples 1 to 16, dissolved in DMSO) were added to each well in 5 μl/well, followed by addition of kinase buffer (25 mM Hepes, pH 7.5, 5 mM MnCl2, 5 mM MgCl2), 0.3 mM ATP, and 100 ng/well recombinant human ALK (Abnova Corporation), to a total volume of 100 μl each well. After kept at 30° C. for 15 minutes, the reaction mixture was removed, and washed with 200 μl of wash buffer (PBS containing 0.05% Tween 80) for 5 times.100 μl/well of mouse anti-phosphotyrosine monoclonal antibody (clone 4G10, purchased from EMD Millipore Corporation) were used in the detection of phosphorylated peptide substrate. Monoclonal antibody was diluted at 1:500 with PBS containing 4% bovine serum albumin. After incubated at room temperature for 30 minutes, the antibody solution was removed, and each well was washed with 200 μl of wash buffer (PBS containing 0.05% Tween 80) for 5 times.100 μl/well of secondary antibody (anti-mouse IgG) was added. The secondary antibody was diluted at 1:1000 with PBS containing 4% bovine serum albumin, incubated for 30 minutes at room temperature; and the wells were washed again as said above.100 μl/well of TMB substrate solution was used for color development, and the same volume of 0.18 M H2SO4 was added to terminate the color development. Finally, the absorbance at 450 nm or 490 nm was read, and the IC50 was calculated. | B | 8.3 | pIC50 | <5 | nM | IC50 | US-10618884-B2. Deuterated diaminopyrimidine compounds and pharmaceutical compositions comprising such compounds (2020) |
| ChEMBL | The determination of IC50 of the inhibiting effect to kinase ALK: 96-well plates was coated under 37° C. with coating buffer (125 μl/well) overnight, and coating buffer was polypeptide substrate [Poly (4:1 Glu, Tyr) Peptide, available from SignalChem] containing 2.5 μg/well ALK kinase in PBS. Then, each well was washed with 200 μl of buffer (PBS containing 0.05% Tween 80), and placed at 37° C. for at least 2 hours to dryness.Serial diluted test compounds in different concentrations (compounds prepared in any one of Examples 1 to 16, dissolved in DMSO) were added to each well in 5 μl/well, followed by addition of kinase buffer (25 mM Hepes, pH 7.5, 5 mM MnCl2, 5 mM MgCl2), 0.3 mM ATP, and 100 ng/well recombinant human ALK (Abnova Corporation), to a total volume of 100 μl each well. After kept at 30° C. for 15 minutes, the reaction mixture was removed, and washed with 200 μl of wash buffer (PBS containing 0.05% Tween 80) for 5 times.100 μl/well of mouse anti-phosphotyrosine monoclonal antibody (clone 4G10, purchased from EMD Millipore Corporation) were used in the detection of phosphorylated peptide substrate. Monoclonal antibody was diluted at 1:500 with PBS containing 4% bovine serum albumin. After incubated at room temperature for 30 minutes, the antibody solution was removed, and each well was washed with 200 μl of wash buffer (PBS containing 0.05% Tween 80) for 5 times.100 μl/well of secondary antibody (anti-mouse IgG) was added. The secondary antibody was diluted at 1:1000 with PBS containing 4% bovine serum albumin, incubated for 30 minutes at room temperature; and the wells were washed again as said above.100 μl/well of TMB substrate solution was used for color development, and the same volume of 0.18 M H2SO4 was added to terminate the color development. Finally, the absorbance at 450 nm or 490 nm was read, and the IC50 was calculated. | B | 8.3 | pIC50 | <5 | nM | IC50 | US-10618884-B2. Deuterated diaminopyrimidine compounds and pharmaceutical compositions comprising such compounds (2020) |
| ChEMBL | In Vitro assay: The determination of IC50 of the inhibiting effect to kinase ALK 96-well plates was coated under 37° C. with coating buffer (125 ul/well) overnight, and coating buffer was polypeptide substrate [Poly (4:1 Glu, Tyr) Peptide, available from SignalChem] containing 2.5 ug/well ALK kinase in PBS. Then, each well was washed with 200 ul of buffer (PBS containing 0.05% Tween 80), and placed at 37° C. for at least 2 hours to dryness. Serial diluted test compounds in different concentrations (compounds prepared in any one of Examples 1 to 16, dissolved in DMSO) were added to each well in 5/well, followed by addition of kinase buffer (25 mM Hepes, pH 7.5, 5 mM MnCl2, 5 mM MgCl2), 0.3 mM ATP, and 100 ng/well recombinant human ALK (Abnova Corporation), to a total volume of 100 ul each well. After kept at 30° C. for 15 minutes, the reaction mixture was removed, and washed with 200 ul of wash buffer (PBS containing 0.05% Tween 80) for 5 times. | B | 8.3 | pIC50 | <5 | nM | IC50 | US-9809572-B2. Deuterated diaminopyrimidine compounds and pharmaceutical compositions comprising such compounds (2017) |
| ChEMBL | In Vitro assay: The determination of IC50 of the inhibiting effect to kinase ALK 96-well plates was coated under 37° C. with coating buffer (125 ul/well) overnight, and coating buffer was polypeptide substrate [Poly (4:1 Glu, Tyr) Peptide, available from SignalChem] containing 2.5 ug/well ALK kinase in PBS. Then, each well was washed with 200 ul of buffer (PBS containing 0.05% Tween 80), and placed at 37° C. for at least 2 hours to dryness. Serial diluted test compounds in different concentrations (compounds prepared in any one of Examples 1 to 16, dissolved in DMSO) were added to each well in 5/well, followed by addition of kinase buffer (25 mM Hepes, pH 7.5, 5 mM MnCl2, 5 mM MgCl2), 0.3 mM ATP, and 100 ng/well recombinant human ALK (Abnova Corporation), to a total volume of 100 ul each well. After kept at 30° C. for 15 minutes, the reaction mixture was removed, and washed with 200 ul of wash buffer (PBS containing 0.05% Tween 80) for 5 times. | B | 8.3 | pIC50 | <5 | nM | IC50 | US-9809572-B2. Deuterated diaminopyrimidine compounds and pharmaceutical compositions comprising such compounds (2017) |
| ChEMBL | In Vitro assay: The determination of IC50 of the inhibiting effect to kinase ALK 96-well plates was coated under 37° C. with coating buffer (125 ul/well) overnight, and coating buffer was polypeptide substrate [Poly (4:1 Glu, Tyr) Peptide, available from SignalChem] containing 2.5 ug/well ALK kinase in PBS. Then, each well was washed with 200 ul of buffer (PBS containing 0.05% Tween 80), and placed at 37° C. for at least 2 hours to dryness. Serial diluted test compounds in different concentrations (compounds prepared in any one of Examples 1 to 16, dissolved in DMSO) were added to each well in 5/well, followed by addition of kinase buffer (25 mM Hepes, pH 7.5, 5 mM MnCl2, 5 mM MgCl2), 0.3 mM ATP, and 100 ng/well recombinant human ALK (Abnova Corporation), to a total volume of 100 ul each well. After kept at 30° C. for 15 minutes, the reaction mixture was removed, and washed with 200 ul of wash buffer (PBS containing 0.05% Tween 80) for 5 times. | B | 8.3 | pIC50 | <5 | nM | IC50 | US-9809572-B2. Deuterated diaminopyrimidine compounds and pharmaceutical compositions comprising such compounds (2017) |
| ChEMBL | In Vitro assay: The determination of IC50 of the inhibiting effect to kinase ALK 96-well plates was coated under 37° C. with coating buffer (125 ul/well) overnight, and coating buffer was polypeptide substrate [Poly (4:1 Glu, Tyr) Peptide, available from SignalChem] containing 2.5 ug/well ALK kinase in PBS. Then, each well was washed with 200 ul of buffer (PBS containing 0.05% Tween 80), and placed at 37° C. for at least 2 hours to dryness. Serial diluted test compounds in different concentrations (compounds prepared in any one of Examples 1 to 16, dissolved in DMSO) were added to each well in 5/well, followed by addition of kinase buffer (25 mM Hepes, pH 7.5, 5 mM MnCl2, 5 mM MgCl2), 0.3 mM ATP, and 100 ng/well recombinant human ALK (Abnova Corporation), to a total volume of 100 ul each well. After kept at 30° C. for 15 minutes, the reaction mixture was removed, and washed with 200 ul of wash buffer (PBS containing 0.05% Tween 80) for 5 times. | B | 8.3 | pIC50 | <5 | nM | IC50 | US-9809572-B2. Deuterated diaminopyrimidine compounds and pharmaceutical compositions comprising such compounds (2017) |
| ChEMBL | In Vitro assay: The determination of IC50 of the inhibiting effect to kinase ALK 96-well plates was coated under 37° C. with coating buffer (125 ul/well) overnight, and coating buffer was polypeptide substrate [Poly (4:1 Glu, Tyr) Peptide, available from SignalChem] containing 2.5 ug/well ALK kinase in PBS. Then, each well was washed with 200 ul of buffer (PBS containing 0.05% Tween 80), and placed at 37° C. for at least 2 hours to dryness. Serial diluted test compounds in different concentrations (compounds prepared in any one of Examples 1 to 16, dissolved in DMSO) were added to each well in 5/well, followed by addition of kinase buffer (25 mM Hepes, pH 7.5, 5 mM MnCl2, 5 mM MgCl2), 0.3 mM ATP, and 100 ng/well recombinant human ALK (Abnova Corporation), to a total volume of 100 ul each well. After kept at 30° C. for 15 minutes, the reaction mixture was removed, and washed with 200 ul of wash buffer (PBS containing 0.05% Tween 80) for 5 times. | B | 8.3 | pIC50 | <5 | nM | IC50 | US-9809572-B2. Deuterated diaminopyrimidine compounds and pharmaceutical compositions comprising such compounds (2017) |
| ChEMBL | In Vitro assay: The determination of IC50 of the inhibiting effect to kinase ALK 96-well plates was coated under 37° C. with coating buffer (125 ul/well) overnight, and coating buffer was polypeptide substrate [Poly (4:1 Glu, Tyr) Peptide, available from SignalChem] containing 2.5 ug/well ALK kinase in PBS. Then, each well was washed with 200 ul of buffer (PBS containing 0.05% Tween 80), and placed at 37° C. for at least 2 hours to dryness. Serial diluted test compounds in different concentrations (compounds prepared in any one of Examples 1 to 16, dissolved in DMSO) were added to each well in 5/well, followed by addition of kinase buffer (25 mM Hepes, pH 7.5, 5 mM MnCl2, 5 mM MgCl2), 0.3 mM ATP, and 100 ng/well recombinant human ALK (Abnova Corporation), to a total volume of 100 ul each well. After kept at 30° C. for 15 minutes, the reaction mixture was removed, and washed with 200 ul of wash buffer (PBS containing 0.05% Tween 80) for 5 times. | B | 8.3 | pIC50 | <5 | nM | IC50 | US-9809572-B2. Deuterated diaminopyrimidine compounds and pharmaceutical compositions comprising such compounds (2017) |
| ChEMBL | In Vitro assay: The determination of IC50 of the inhibiting effect to kinase ALK 96-well plates was coated under 37° C. with coating buffer (125 ul/well) overnight, and coating buffer was polypeptide substrate [Poly (4:1 Glu, Tyr) Peptide, available from SignalChem] containing 2.5 ug/well ALK kinase in PBS. Then, each well was washed with 200 ul of buffer (PBS containing 0.05% Tween 80), and placed at 37° C. for at least 2 hours to dryness. Serial diluted test compounds in different concentrations (compounds prepared in any one of Examples 1 to 16, dissolved in DMSO) were added to each well in 5/well, followed by addition of kinase buffer (25 mM Hepes, pH 7.5, 5 mM MnCl2, 5 mM MgCl2), 0.3 mM ATP, and 100 ng/well recombinant human ALK (Abnova Corporation), to a total volume of 100 ul each well. After kept at 30° C. for 15 minutes, the reaction mixture was removed, and washed with 200 ul of wash buffer (PBS containing 0.05% Tween 80) for 5 times. | B | 8.3 | pIC50 | <5 | nM | IC50 | US-9809572-B2. Deuterated diaminopyrimidine compounds and pharmaceutical compositions comprising such compounds (2017) |
| ChEMBL | In Vitro assay: The determination of IC50 of the inhibiting effect to kinase ALK 96-well plates was coated under 37° C. with coating buffer (125 ul/well) overnight, and coating buffer was polypeptide substrate [Poly (4:1 Glu, Tyr) Peptide, available from SignalChem] containing 2.5 ug/well ALK kinase in PBS. Then, each well was washed with 200 ul of buffer (PBS containing 0.05% Tween 80), and placed at 37° C. for at least 2 hours to dryness. Serial diluted test compounds in different concentrations (compounds prepared in any one of Examples 1 to 16, dissolved in DMSO) were added to each well in 5/well, followed by addition of kinase buffer (25 mM Hepes, pH 7.5, 5 mM MnCl2, 5 mM MgCl2), 0.3 mM ATP, and 100 ng/well recombinant human ALK (Abnova Corporation), to a total volume of 100 ul each well. After kept at 30° C. for 15 minutes, the reaction mixture was removed, and washed with 200 ul of wash buffer (PBS containing 0.05% Tween 80) for 5 times. | B | 8.3 | pIC50 | <5 | nM | IC50 | US-9809572-B2. Deuterated diaminopyrimidine compounds and pharmaceutical compositions comprising such compounds (2017) |
| ChEMBL | In Vitro assay: The determination of IC50 of the inhibiting effect to kinase ALK 96-well plates was coated under 37° C. with coating buffer (125 ul/well) overnight, and coating buffer was polypeptide substrate [Poly (4:1 Glu, Tyr) Peptide, available from SignalChem] containing 2.5 ug/well ALK kinase in PBS. Then, each well was washed with 200 ul of buffer (PBS containing 0.05% Tween 80), and placed at 37° C. for at least 2 hours to dryness. Serial diluted test compounds in different concentrations (compounds prepared in any one of Examples 1 to 16, dissolved in DMSO) were added to each well in 5/well, followed by addition of kinase buffer (25 mM Hepes, pH 7.5, 5 mM MnCl2, 5 mM MgCl2), 0.3 mM ATP, and 100 ng/well recombinant human ALK (Abnova Corporation), to a total volume of 100 ul each well. After kept at 30° C. for 15 minutes, the reaction mixture was removed, and washed with 200 ul of wash buffer (PBS containing 0.05% Tween 80) for 5 times. | B | 8.3 | pIC50 | <5 | nM | IC50 | US-9809572-B2. Deuterated diaminopyrimidine compounds and pharmaceutical compositions comprising such compounds (2017) |
| ChEMBL | In Vitro assay: The determination of IC50 of the inhibiting effect to kinase ALK 96-well plates was coated under 37° C. with coating buffer (125 ul/well) overnight, and coating buffer was polypeptide substrate [Poly (4:1 Glu, Tyr) Peptide, available from SignalChem] containing 2.5 ug/well ALK kinase in PBS. Then, each well was washed with 200 ul of buffer (PBS containing 0.05% Tween 80), and placed at 37° C. for at least 2 hours to dryness. Serial diluted test compounds in different concentrations (compounds prepared in any one of Examples 1 to 16, dissolved in DMSO) were added to each well in 5/well, followed by addition of kinase buffer (25 mM Hepes, pH 7.5, 5 mM MnCl2, 5 mM MgCl2), 0.3 mM ATP, and 100 ng/well recombinant human ALK (Abnova Corporation), to a total volume of 100 ul each well. After kept at 30° C. for 15 minutes, the reaction mixture was removed, and washed with 200 ul of wash buffer (PBS containing 0.05% Tween 80) for 5 times. | B | 8.3 | pIC50 | <5 | nM | IC50 | US-9809572-B2. Deuterated diaminopyrimidine compounds and pharmaceutical compositions comprising such compounds (2017) |
| ChEMBL | In Vitro assay: The determination of IC50 of the inhibiting effect to kinase ALK 96-well plates was coated under 37° C. with coating buffer (125 ul/well) overnight, and coating buffer was polypeptide substrate [Poly (4:1 Glu, Tyr) Peptide, available from SignalChem] containing 2.5 ug/well ALK kinase in PBS. Then, each well was washed with 200 ul of buffer (PBS containing 0.05% Tween 80), and placed at 37° C. for at least 2 hours to dryness. Serial diluted test compounds in different concentrations (compounds prepared in any one of Examples 1 to 16, dissolved in DMSO) were added to each well in 5/well, followed by addition of kinase buffer (25 mM Hepes, pH 7.5, 5 mM MnCl2, 5 mM MgCl2), 0.3 mM ATP, and 100 ng/well recombinant human ALK (Abnova Corporation), to a total volume of 100 ul each well. After kept at 30° C. for 15 minutes, the reaction mixture was removed, and washed with 200 ul of wash buffer (PBS containing 0.05% Tween 80) for 5 times. | B | 8.3 | pIC50 | <5 | nM | IC50 | US-9809572-B2. Deuterated diaminopyrimidine compounds and pharmaceutical compositions comprising such compounds (2017) |
| ChEMBL | In Vitro assay: The determination of IC50 of the inhibiting effect to kinase ALK 96-well plates was coated under 37° C. with coating buffer (125 ul/well) overnight, and coating buffer was polypeptide substrate [Poly (4:1 Glu, Tyr) Peptide, available from SignalChem] containing 2.5 ug/well ALK kinase in PBS. Then, each well was washed with 200 ul of buffer (PBS containing 0.05% Tween 80), and placed at 37° C. for at least 2 hours to dryness. Serial diluted test compounds in different concentrations (compounds prepared in any one of Examples 1 to 16, dissolved in DMSO) were added to each well in 5/well, followed by addition of kinase buffer (25 mM Hepes, pH 7.5, 5 mM MnCl2, 5 mM MgCl2), 0.3 mM ATP, and 100 ng/well recombinant human ALK (Abnova Corporation), to a total volume of 100 ul each well. After kept at 30° C. for 15 minutes, the reaction mixture was removed, and washed with 200 ul of wash buffer (PBS containing 0.05% Tween 80) for 5 times. | B | 8.3 | pIC50 | <5 | nM | IC50 | US-9809572-B2. Deuterated diaminopyrimidine compounds and pharmaceutical compositions comprising such compounds (2017) |
| ChEMBL | Inhibition of recombinant human N-terminal GST-tagged ALK cytoplasmic domain (1058 to 1620 residues) S1206Y mutant expressed in baculovirus expression system using peptide substrate after 1 hr by mobility shift assay | B | 8.34 | pIC50 | 4.6 | nM | IC50 | Eur J Med Chem (2018) 143: 123-136 [PMID:29174809] |
| ChEMBL | Inhibition of crizotinib-resistant ALK C1156Y mutant (unknown origin) using peptide substrate incubated for 30 mins in presence of ATP by fluorescence assay | B | 8.38 | pIC50 | 4.2 | nM | IC50 | Bioorg Med Chem (2016) 24: 207-219 [PMID:26712094] |
| ChEMBL | Inhibition of ALK (unknown origin) by TR-FRET assay | B | 8.4 | pIC50 | 3.94 | nM | IC50 | J Med Chem (2019) 62: 10927-10954 [PMID:31419130] |
| ChEMBL | Inhibition of recombinant human N-terminal GST-tagged ALK (1058 to 1620 residues) expressed in baculovirus expression system using Srctide as substrate incubated for 1 hr by mobility shift assay | B | 8.46 | pIC50 | 3.5 | nM | IC50 | Eur J Med Chem (2021) 214: 113259-113259 [PMID:33581554] |
| ChEMBL | Inhibition of wild type ALK (unknown origin) | B | 8.46 | pIC50 | 3.5 | nM | IC50 | Bioorg Med Chem Lett (2022) 75: 128990-128990 [PMID:36113668] |
| ChEMBL | Inhibition of recombinant ALK (unknown origin) using poly (Glu,Tyr) 4:1 as substrate incubated for 60 mins by ELISA | B | 8.47 | pIC50 | 3.4 | nM | IC50 | Eur J Med Chem (2018) 144: 386-397 [PMID:29288940] |
| ChEMBL | Inhibition of purified ALK (unknown origin) after 60 mins by ELISA kinase assay | B | 8.47 | pIC50 | 3.4 | nM | IC50 | Eur J Med Chem (2014) 86: 438-448 [PMID:25200979] |
| ChEMBL | Inhibition of recombinant human N-terminal GST-tagged ALK cytoplasmic domain (1058 to 1620 residues) G1269A mutant expressed in baculovirus expression system using peptide substrate after 1 hr by mobility shift assay | B | 8.47 | pIC50 | 3.4 | nM | IC50 | Eur J Med Chem (2018) 143: 123-136 [PMID:29174809] |
| ChEMBL | Inhibition of ALK G1202R mutant (unknown origin) | B | 8.48 | pIC50 | 3.3 | nM | IC50 | Eur J Med Chem (2021) 224: 113672-113672 [PMID:34237620] |
| ChEMBL | Inhibition of N-terminal GST-tagged human wild type ALK (1058 to 1620 residues) cytoplasmic domain expressed in baculovirus infected Sf21 cells incubated for 1 hrs in the presence of ATP by mobility shift assay | B | 8.49 | pIC50 | 3.2 | nM | IC50 | Eur J Med Chem (2022) 238: 114493-114493 [PMID:35691173] |
| ChEMBL | Inhibition of human N-terminal GST-fused ALK cytoplasmic domain (1058 to 1620 residues) expressed in baculovirus infected Sf21 insect cells using Srctide as substrate measured after 1 hr by mobility shift assay | B | 8.49 | pIC50 | 3.2 | nM | IC50 | Bioorg Med Chem (2021) 37: 116108-116108 [PMID:33756437] |
| ChEMBL | Inhibition of recombinant human N-terminal GST-tagged ALK (1058 to 1620 residues) cytoplasmic domain L1196M mutant expressed in baculovirus expression system using srctide as substrate incubated for 1 hr by mobility shift assay | B | 8.51 | pIC50 | 3.1 | nM | IC50 | Bioorg Med Chem (2019) 27: 115051-115051 [PMID:31492532] |
| ChEMBL | Inhibition of human ALK assessed as decreased enzymatic reactions measured after 1 hr by mobility shift assay | B | 8.51 | pIC50 | 3.1 | nM | IC50 | Bioorg Med Chem (2021) 47: 116396-116396 [PMID:34534734] |
| ChEMBL | Inhibition of recombinant human N-terminal GST-tagged ALK cytoplasmic domain (1058 to 1620 residues) C1156Y mutant expressed in baculovirus expression system using peptide substrate after 1 hr by mobility shift assay | B | 8.54 | pIC50 | 2.9 | nM | IC50 | Eur J Med Chem (2018) 143: 123-136 [PMID:29174809] |
| ChEMBL | Inhibition of recombinant human N-terminal GST-tagged ALK cytoplasmic domain (1058 to 1620 residues) expressed in baculovirus expression system using peptide substrate after 1 hr by mobility shift assay | B | 8.54 | pIC50 | 2.9 | nM | IC50 | Eur J Med Chem (2018) 143: 123-136 [PMID:29174809] |
| ChEMBL | Inhibition of ALK (unknown origin) using peptide substrate incubated for 60 mins in presence of ATP by HTRF assay | B | 8.54 | pIC50 | 2.9 | nM | IC50 | Bioorg Med Chem (2020) 28: 115719-115719 [PMID:33069075] |
| ChEMBL | Inhibition of wild type ALK (unknown origin) | B | 8.54 | pIC50 | 2.9 | nM | IC50 | J Med Chem (2024) 67: 14702-14722 [PMID:39143914] |
| ChEMBL | Inhibition of recombinant human N-terminal GST-tagged ALK (1058 to 1620 residues) cytoplasmic domain expressed in baculovirus expression system using srctide as substrate incubated for 1 hr by mobility shift assay | B | 8.57 | pIC50 | 2.7 | nM | IC50 | Bioorg Med Chem (2019) 27: 115051-115051 [PMID:31492532] |
| ChEMBL | Inhibition of ALK (unknown origin) incubated for 1 hr and measured by mobility shift assay | B | 8.59 | pIC50 | 2.6 | nM | IC50 | Eur J Med Chem (2022) 241: 114626-114626 [PMID:35939995] |
| ChEMBL | Inhibition of recombinant human N-terminal GST-tagged ALK cytoplasmic domain (1058 to 1620 residues) T1151 insertion mutant expressed in baculovirus expression system using peptide substrate after 1 hr by mobility shift assay | B | 8.6 | pIC50 | 2.5 | nM | IC50 | Eur J Med Chem (2018) 143: 123-136 [PMID:29174809] |
| ChEMBL | Inhibition of crizotinib-resistant ALK F1174L mutant (unknown origin) using peptide substrate incubated for 30 mins in presence of ATP by fluorescence assay | B | 8.62 | pIC50 | 2.4 | nM | IC50 | Bioorg Med Chem (2016) 24: 207-219 [PMID:26712094] |
| ChEMBL | Inhibition of wild-type ALK (unknown origin) incubated for 1 hr | B | 8.62 | pIC50 | 2.4 | nM | IC50 | Bioorg Med Chem (2020) 28: 115715-115715 [PMID:33069079] |
| ChEMBL | Inhibition of ALK (unknown origin) using peptide as substrate after 60 mins by HTRF assay | B | 8.64 | pIC50 | 2.3 | nM | IC50 | Eur J Med Chem (2016) 123: 80-89 [PMID:27474925] |
| ChEMBL | Inhibition of N-terminal GST-tagged human ALK cytoplasmic domain (1058 to 1620 residues) expressed in Baculovirus expression system using srctide as substrate incubated for 1 hr by mobility shift assay | B | 8.64 | pIC50 | 2.3 | nM | IC50 | Eur J Med Chem (2019) 171: 297-309 [PMID:30927566] |
| ChEMBL | Inhibition of EML4-fused ALK (unknown origin) by cell-based assay | B | 8.66 | pIC50 | 2.2 | nM | IC50 | J Med Chem (2013) 56: 5675-5690 [PMID:23742252] |
| ChEMBL | Inhibition of crizotinib-resistant ALK G1269A mutant (unknown origin) using peptide substrate incubated for 30 mins in presence of ATP by fluorescence assay | B | 8.68 | pIC50 | 2.1 | nM | IC50 | Bioorg Med Chem (2016) 24: 207-219 [PMID:26712094] |
| ChEMBL | Inhibition of ALK C1156Y mutant (unknown origin) using peptide as substrate measured after 30 mins by fluorescence assay | B | 8.7 | pIC50 | 2 | nM | IC50 | Eur J Med Chem (2017) 126: 536-549 [PMID:27915169] |
| ChEMBL | Inhibition of N-terminal GST-tagged human ALK L1196M mutant cytoplasmic domain (1058 to 1620 residues) expressed in baculovirus expression system using srctide as substrate incubated for 1 hr by mobility shift assay | B | 8.7 | pIC50 | 2 | nM | IC50 | Eur J Med Chem (2019) 171: 297-309 [PMID:30927566] |
| ChEMBL | Inhibition of human ALK G1269A mutant expressed Sf9 cells pre-incubated for 30 mins before addition of Ulight-CKKSRGDYMTMQIG substrate and measured after 90 mins by fluorescence based assay | B | 8.72 | pIC50 | 1.9 | nM | IC50 | J Med Chem (2020) 63: 13994-14016 [PMID:33185101] |
| ChEMBL | Inhibition of human ALK S1206Y mutant expressed Sf9 cells pre-incubated for 30 mins before addition of Ulight-CKKSRGDYMTMQIG substrate and measured after 90 mins by fluorescence based assay | B | 8.8 | pIC50 | 1.6 | nM | IC50 | J Med Chem (2020) 63: 13994-14016 [PMID:33185101] |
| ChEMBL | Inhibition of ALK F1174L mutant (unknown origin) using peptide as substrate measured after 30 mins by fluorescence assay | B | 8.82 | pIC50 | 1.5 | nM | IC50 | Eur J Med Chem (2017) 126: 536-549 [PMID:27915169] |
| ChEMBL | Inhibition of ALK G1269A mutant (unknown origin) using peptide as substrate measured after 30 mins by fluorescence assay | B | 8.85 | pIC50 | 1.4 | nM | IC50 | Eur J Med Chem (2017) 126: 536-549 [PMID:27915169] |
| ChEMBL | Inhibition of wild type N-terminal GST tagged ALK cytoplasmic domain (1058 to 1620 end residues) (unknown origin) expressed in Sf21 cells incubated for 1 hr in presence of ATP | B | 8.92 | pIC50 | 1.2 | nM | IC50 | Bioorg Med Chem (2022) 66: 116794-116794 [PMID:35576654] |
| ChEMBL | Inhibition of human ALK L1196M mutant expressed Sf9 cells pre-incubated for 30 mins before addition of Ulight-CKKSRGDYMTMQIG substrate and measured after 90 mins by fluorescence based assay | B | 8.96 | pIC50 | 1.1 | nM | IC50 | J Med Chem (2020) 63: 13994-14016 [PMID:33185101] |
| ChEMBL | Inhibitory Activity Against Anaplastic Lymphoma Kinase (ALK): A proliferation inhibitory activity against the ALK of the compound represented by Chemical Formula 1 according to the present invention at an enzyme level, the following experiment was performed.In order to measure the inhibitory activity against the ALK, the compounds (2 ÎĽl) prepared in Examples 1 to 106 were added to Greiner 96 well round bottom plates, respectively, and the ALK enzyme (1 ÎĽl) and biotin-adhered peptide substrate (2 ÎĽl) were mixed for 15 minutes, and then, the plates were cultured. An ATP solution (5 ÎĽl) was added thereto, and then, a kinase reaction was performed at room temperature for 30 minutes. Streptavidin-adhered XL 665 (5 ÎĽl) and europium (Eu3+)-adhered anti-phosphotyrosine antibody (5 ÎĽl) dissolved in ethylenediaminetetraacetic acid solution was added to the reaction solution to stop the reaction, and cultured for 1 hour, and analyzed by using homogeneous time-resolved fluorescence (HTRF, Cisbio) The compounds were read in a wavelength range of 615/665 nm using a Wallac Envision 2103 instrument. The IC50 of each of the test compounds subjected to the above experiment was implemented using prism (version 5.01, GraphPad) software.Accordingly, IC50 of each of the compounds that reduce an ALK enzyme activity and a cell activity of L1196M (a non-small cell lung cancer cell including an ALK enzyme) to 50% was calculated, and as a result, it was found that all of the compounds prepared in Examples 1 to 106 according to the present invention had IC50 values of 0.01 ÎĽM or less. | B | 9 | pIC50 | 1 | nM | IC50 | US-10053458-B2. Pyrimidine-2,4-diamine derivative and anticancer pharmaceutical composition comprising same as effective ingredient (2018) |
| ChEMBL | Inhibition of ALK (unknown origin) preincubated for 10 mins followed by addition of substrate and ATP for 25 mins by caliper EZ reader method | B | 9 | pIC50 | <1 | nM | IC50 | Eur J Med Chem (2021) 224: 113672-113672 [PMID:34237620] |
| ChEMBL | Inhibition of wild type N-terminal GST tagged ALK L1196M mutant cytoplasmic domain (1058 to 1620 end residues) (unknown origin) expressed in Sf21 cells incubated for 1 hr in presence of ATP | B | 9.08 | pIC50 | 0.83 | nM | IC50 | Bioorg Med Chem (2022) 66: 116794-116794 [PMID:35576654] |
| ChEMBL | Inhibition of N-terminal GST tagged wild-type human ALK cytoplasmic domain (1058-1620 amino acids) expressed Sf9 cells pre-incubated for 30 mins before addition of Ulight-CKKSRGDYMTMQIG substrate and measured after 90 mins by fluorescence based assay | B | 9.21 | pIC50 | 0.61 | nM | IC50 | J Med Chem (2020) 63: 13994-14016 [PMID:33185101] |
| ChEMBL | Inhibition of ALK L1196M mutant (unknown origin) | B | 9.6 | pIC50 | 0.25 | nM | IC50 | Eur J Med Chem (2021) 224: 113672-113672 [PMID:34237620] |
| ChEMBL | Inhibition of ALK (unknown origin) | B | 9.7 | pIC50 | 0.2 | nM | IC50 | J Med Chem (2022) 65: 5149-5183 [PMID:35311289] |
| ChEMBL | Inhibition of ALK (unknown origin) after 60 mins | B | 9.7 | pIC50 | 0.2 | nM | IC50 | J Med Chem (2013) 56: 5675-5690 [PMID:23742252] |
| ChEMBL | Inhibition of ALK (unknown origin) | B | 9.7 | pIC50 | 0.2 | nM | IC50 | J Med Chem (2013) 56: 5673-5674 [PMID:23837797] |
| GtoPdb | - | - | 9.7 | pIC50 | 0.2 | nM | IC50 | J Med Chem (2013) 56: 5675-90 [PMID:23742252] |
| ChEMBL | Inhibition of ALK L1152R mutant in human DFCI076 cells assessed as reduction in cell viability after 72 hrs by MTS assay | B | 5.46 | pEC50 | 3490 | nM | EC50 | Eur J Med Chem (2017) 136: 497-510 [PMID:28528303] |
| ChEMBL | Inhibition of ALK L1152R mutant in human DFCI076 cells assessed as reduction in cell viability after 72 hrs by MTS assay in presence of osimertinib | B | 5.49 | pEC50 | 3210 | nM | EC50 | Eur J Med Chem (2017) 136: 497-510 [PMID:28528303] |
| AP2 associated kinase 1/AP2-associated protein kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3830] [GtoPdb: 1921] [UniProtKB: Q2M2I8] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ATP-dependent 6-phosphofructokinase, platelet type in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2972] [UniProtKB: Q01813] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ATP-dependent RNA helicase DDX1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2010634] [UniProtKB: Q92499] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ATP-dependent RNA helicase DDX3X in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5553] [UniProtKB: O00571] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ATP-dependent RNA helicase DDX42 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105782] [UniProtKB: Q86XP3] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ATP-dependent RNA helicase DHX30 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105814] [UniProtKB: Q7L2E3] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ABCB1/ATP-dependent translocase ABCB1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4302] [GtoPdb: 768] [UniProtKB: P08183] | ||||||||
| ChEMBL | Inhibition of ABCB1 in human A2780/ADR cells assessed as potentiation of daunorubicin-induced cytotoxicity measured after 72 hrs by MTT assay | B | 7.05 | pEC50 | 89 | nM | EC50 | Eur J Med Chem (2019) 164: 193-213 [PMID:30594677] |
| coenzyme Q8A/Atypical kinase COQ8A, mitochondrial in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5550] [GtoPdb: 1927] [UniProtKB: Q8NI60] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| aurora kinase A/Aurora kinase A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4722] [GtoPdb: 1936] [UniProtKB: O14965] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| aurora kinase B/Aurora kinase B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2185] [GtoPdb: 1937] [UniProtKB: Q96GD4] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| neurotrophic receptor tyrosine kinase 2/BDNF/NT-3 growth factors receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4898] [GtoPdb: 1818] [UniProtKB: Q16620] | ||||||||
| ChEMBL | Inhibition of TEL-fused TRKB (unknown origin) by cell-based assay | B | 5.74 | pIC50 | 1829 | nM | IC50 | J Med Chem (2013) 56: 5675-5690 [PMID:23742252] |
| beta adrenergic receptor kinase 1/Beta-adrenergic receptor kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4079] [GtoPdb: 1466] [UniProtKB: P25098] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Bifunctional phosphoribosylaminoimidazole carboxylase/phosphoribosylaminoimidazole succinocarboxamide synthetase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5922] [UniProtKB: P22234] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| BMP2 inducible kinase/BMP-2-inducible protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4522] [GtoPdb: 1941] [UniProtKB: Q9NSY1] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| bone morphogenetic protein receptor type IA/Bone morphogenetic protein receptor type-1A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5275] [GtoPdb: 1786] [UniProtKB: P36894] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| bone morphogenetic protein receptor type IB/Bone morphogenetic protein receptor type-1B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5476] [GtoPdb: 1789] [UniProtKB: O00238] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| bone morphogenetic protein receptor type 2/Bone morphogenetic protein receptor type-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5467] [GtoPdb: 1794] [UniProtKB: Q13873] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| BCR activator of RhoGEF and GTPase/Breakpoint cluster region protein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5146] [GtoPdb: 2755] [UniProtKB: P11274] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| calcium/calmodulin dependent protein kinase kinase 2/Calcium/calmodulin-dependent protein kinase kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5284] [GtoPdb: 1957] [UniProtKB: Q96RR4] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 5.27 | pKd | 5429 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| calcium/calmodulin-dependent protein kinase II delta subunit/Calcium/calmodulin-dependent protein kinase type II subunit delta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2801] [GtoPdb: 1558] [UniProtKB: Q13557] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| calcium/calmodulin-dependent protein kinase II gamma subunit/Calcium/calmodulin-dependent protein kinase type II subunit gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3829] [GtoPdb: 1557] [UniProtKB: Q13555] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| calcium/calmodulin dependent protein kinase IV/Calcium/calmodulin-dependent protein kinase type IV in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2494] [GtoPdb: 1955] [UniProtKB: Q16566] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 6.2 | pKd | 635 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| protein kinase, cAMP-dependent, catalytic, alpha subunit/cAMP-dependent protein kinase catalytic subunit alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4101] [GtoPdb: 1476] [UniProtKB: P17612] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| protein kinase, cAMP-dependent, catalytic, beta subunit/cAMP-dependent protein kinase catalytic subunit beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2918] [GtoPdb: 1477] [UniProtKB: P22694] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| protein kinase, cAMP-dependent, catalytic, gamma subunit/cAMP-dependent protein kinase catalytic subunit gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2743] [GtoPdb: 1478] [UniProtKB: P22612] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| protein kinase, cAMP-dependent, regulatory, type II, alpha subunit/cAMP-dependent protein kinase type II-alpha regulatory subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2221] [GtoPdb: 1474] [UniProtKB: P13861] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| casein kinase 1 alpha 1/Casein kinase I isoform alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2793] [GtoPdb: 1995] [UniProtKB: P48729] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| casein kinase 1 delta/Casein kinase I isoform delta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2828] [GtoPdb: 1997] [UniProtKB: P48730] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| casein kinase 1 epsilon/Casein kinase I isoform epsilon in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4937] [GtoPdb: 1998] [UniProtKB: P49674] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| casein kinase 1 gamma 1/Casein kinase I isoform gamma-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2426] [GtoPdb: 1999] [UniProtKB: Q9HCP0] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| casein kinase 1 gamma 2/Casein kinase I isoform gamma-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2543] [GtoPdb: 2000] [UniProtKB: P78368] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| casein kinase 1 gamma 3/Casein kinase I isoform gamma-3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5084] [GtoPdb: 2001] [UniProtKB: Q9Y6M4] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| casein kinase 2, alpha prime polypeptide subunit/Casein kinase II subunit alpha` in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4070] [GtoPdb: 1550] [UniProtKB: P19784] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Protein kinase G (PKG) 1/cGMP-dependent protein kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4273] [GtoPdb: 1492] [UniProtKB: Q13976] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Chromodomain-helicase-DNA-binding protein 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105742] [UniProtKB: Q14839] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| citron rho-interacting serine/threonine kinase/Citron Rho-interacting kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5579] [GtoPdb: 1509] [UniProtKB: O14578] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| cyclin dependent kinase 1/Cyclin-dependent kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL308] [GtoPdb: 1961] [UniProtKB: P06493] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| cyclin dependent kinase 12/Cyclin-dependent kinase 12 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3559692] [GtoPdb: 1965] [UniProtKB: Q9NYV4] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| cyclin dependent kinase 13/Cyclin-dependent kinase 13 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795192] [GtoPdb: 1966] [UniProtKB: Q14004] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| cyclin dependent kinase 16/Cyclin-dependent kinase 16 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4597] [GtoPdb: 1969] [UniProtKB: Q00536] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| cyclin dependent kinase 17/Cyclin-dependent kinase 17 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5790] [GtoPdb: 1970] [UniProtKB: Q00537] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| cyclin dependent kinase 2/Cyclin-dependent kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL301] [GtoPdb: 1973] [UniProtKB: P24941] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Inhibition of CDK2 (unknown origin) after 60 mins | B | 5.4 | pIC50 | 3970 | nM | IC50 | J Med Chem (2013) 56: 5675-5690 [PMID:23742252] |
| cyclin dependent kinase 3/Cyclin-dependent kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4442] [GtoPdb: 1975] [UniProtKB: Q00526] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| cyclin dependent kinase 4/Cyclin-dependent kinase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL331] [GtoPdb: 1976] [UniProtKB: P11802] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Inhibition of CDK4 (unknown origin) after 60 mins | B | 5.33 | pIC50 | 4720 | nM | IC50 | J Med Chem (2013) 56: 5675-5690 [PMID:23742252] |
| cyclin dependent kinase 5/Cyclin-dependent kinase 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4036] [GtoPdb: 1977] [UniProtKB: Q00535] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| cyclin dependent kinase 6/Cyclin-dependent kinase 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2508] [GtoPdb: 1978] [UniProtKB: Q00534] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| cyclin dependent kinase 7/Cyclin-dependent kinase 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3055] [GtoPdb: 1979] [UniProtKB: P50613] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| cyclin dependent kinase 9/Cyclin-dependent kinase 9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3116] [GtoPdb: 1981] [UniProtKB: P50750] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| cyclin-dependent kinase like 5/Cyclin-dependent kinase-like 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1163112] [GtoPdb: 1986] [UniProtKB: O76039] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| cyclin G associated kinase/Cyclin-G-associated kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4355] [GtoPdb: 2027] [UniProtKB: O14976] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Cysteine--tRNA ligase, cytoplasmic in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105937] [UniProtKB: P49589] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Cytochrome c1, heme protein, mitochondrial in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105975] [UniProtKB: P08574] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| dCTP pyrophosphatase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3769292] [UniProtKB: Q9H773] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Delta(24)-sterol reductase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2331059] [UniProtKB: Q15392] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Deoxycytidine kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2447] [UniProtKB: P27707] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| discoidin domain receptor tyrosine kinase 2/Discoidin domain-containing receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5122] [GtoPdb: 1844] [UniProtKB: Q16832] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| DnaJ homolog subfamily A member 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2189122] [UniProtKB: P31689] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| DNA replication licensing factor MCM4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105745] [UniProtKB: P33991] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| DNA topoisomerase II alpha/DNA topoisomerase 2-alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1806] [GtoPdb: 2637] [UniProtKB: P11388] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| DNA topoisomerase 2-beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3396] [UniProtKB: Q02880] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| mitogen-activated protein kinase kinase 1/Dual specificity mitogen-activated protein kinase kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3587] [GtoPdb: 2062] [UniProtKB: Q02750] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| mitogen-activated protein kinase kinase 2/Dual specificity mitogen-activated protein kinase kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2964] [GtoPdb: 2063] [UniProtKB: P36507] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| mitogen-activated protein kinase kinase 3/Dual specificity mitogen-activated protein kinase kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2109] [GtoPdb: 2064] [UniProtKB: P46734] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| mitogen-activated protein kinase kinase 5/Dual specificity mitogen-activated protein kinase kinase 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4948] [GtoPdb: 2066] [UniProtKB: Q13163] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| mitogen-activated protein kinase kinase 6/Dual specificity mitogen-activated protein kinase kinase 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2171] [GtoPdb: 2067] [UniProtKB: P52564] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| CDC like kinase 1/Dual specificity protein kinase CLK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4224] [GtoPdb: 1990] [UniProtKB: P49759] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 5.98 | pKd | 1059 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| CDC like kinase 2/Dual specificity protein kinase CLK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4225] [GtoPdb: 1991] [UniProtKB: P49760] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| TTK protein kinase/Dual specificity protein kinase TTK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3983] [GtoPdb: 2264] [UniProtKB: P33981] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| testis associated actin remodelling kinase 1/Dual specificity testis-specific protein kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5604] [GtoPdb: 2239] [UniProtKB: Q15569] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| dual specificity tyrosine phosphorylation regulated kinase 1A/Dual specificity tyrosine-phosphorylation-regulated kinase 1A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2292] [GtoPdb: 2009] [UniProtKB: Q13627] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| dual specificity tyrosine phosphorylation regulated kinase 1B/Dual specificity tyrosine-phosphorylation-regulated kinase 1B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5543] [GtoPdb: 2010] [UniProtKB: Q9Y463] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Dynamin-like GTPase OPA1, mitochondrial in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105705] [UniProtKB: O60313] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| TP53 regulating kinase/EKC/KEOPS complex subunit TP53RK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1938223] [GtoPdb: 2248] [UniProtKB: Q96S44] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Elongation factor Tu, mitochondrial in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105970] [UniProtKB: P49411] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| EPH receptor A1/Ephrin type-A receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5810] [GtoPdb: 1821] [UniProtKB: P21709] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| EPH receptor A2/Ephrin type-A receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2068] [GtoPdb: 1822] [UniProtKB: P29317] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| EPH receptor A4/Ephrin type-A receptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3988] [GtoPdb: 1824] [UniProtKB: P54764] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| EPH receptor A5/Ephrin type-A receptor 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3987] [GtoPdb: 1825] [UniProtKB: P54756] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| EPH receptor A7/Ephrin type-A receptor 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4602] [GtoPdb: 1827] [UniProtKB: Q15375] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| EPH receptor B2/Ephrin type-B receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3290] [GtoPdb: 1831] [UniProtKB: P29323] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| EPH receptor B3/Ephrin type-B receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4901] [GtoPdb: 1832] [UniProtKB: P54753] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| EPH receptor B4/Ephrin type-B receptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5147] [GtoPdb: 1833] [UniProtKB: P54760] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| EPH receptor B6/Ephrin type-B receptor 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5836] [GtoPdb: 1834] [UniProtKB: O15197] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| epidermal growth factor receptor/Epidermal growth factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Inhibition of human N-terminal GST-tagged EGFR cytoplasmic domain (669 to 1210 residues) expressed in baculovirus expression system after 1 hr by mobility shift assay | B | 3 | pIC50 | >1000000 | nM | IC50 | Eur J Med Chem (2018) 158: 322-333 [PMID:30223120] |
| ChEMBL | Inhibition of wild type GST-tagged human EGFR cytoplasmic domain (668 to 1210 residues) expressed in baculovirus expression system using Poly G:T (4:1) as substrate after 30 mins by Z-LYTE assay | B | 5.67 | pIC50 | 2156 | nM | IC50 | Eur J Med Chem (2017) 136: 497-510 [PMID:28528303] |
| ChEMBL | Inhibition of recombinant human N-terminal GST-tagged EGFR cytoplasmic domain (669 to 1210 residues) expressed in baculovirus expression system using peptide substrate after 1 hr by mobility shift assay | B | 6 | pIC50 | >1000 | nM | IC50 | Eur J Med Chem (2018) 143: 123-136 [PMID:29174809] |
| ChEMBL | Inhibition of N-terminal GST-tagged human EGFR cytoplasmic domain (669 to 1210 residues) expressed in Baculovirus expression system using srctide as substrate incubated for 1 hr by mobility shift assay | B | 6 | pIC50 | >1000 | nM | IC50 | Eur J Med Chem (2019) 171: 297-309 [PMID:30927566] |
| ChEMBL | Inhibition of EGFR (unknown origin) | B | 6 | pIC50 | >1000 | nM | IC50 | Bioorg Med Chem Lett (2022) 75: 128990-128990 [PMID:36113668] |
| ChEMBL | Inhibition of human EGFR (669 to 1210 residues) cytoplasmic domain expressed in baculovirus infected Sf21 cells incubated for 1 hrs in the presence of ATP by mobility shift assay | B | 6 | pIC50 | >1000 | nM | IC50 | Eur J Med Chem (2022) 238: 114493-114493 [PMID:35691173] |
| ChEMBL | Inhibition of recombinant human N-terminal GST-tagged EGFR (669 to 1210 residues) cytoplasmic domain expressed in baculovirus expression system using Srctide as substrate incubated for 1 hr by mobility shift assay | B | 6 | pIC50 | >1000 | nM | IC50 | Bioorg Med Chem (2019) 27: 115051-115051 [PMID:31492532] |
| ChEMBL | Inhibition of N-terminal GST-tagged human EGFR cytoplasmic domain (669 to 1210 residues) expressed in baculovirus infected Sf21 insect cells using Srctide as substrate measured after 1 hr by mobility shift assay | B | 6 | pIC50 | >1000 | nM | IC50 | Bioorg Med Chem (2021) 37: 116108-116108 [PMID:33756437] |
| ChEMBL | Inhibition of EGFR (unknown origin) incubated for 1 hr and measured by mobility shift assay | B | 6 | pIC50 | >1000 | nM | IC50 | Eur J Med Chem (2022) 241: 114626-114626 [PMID:35939995] |
| ChEMBL | Inhibition of recombinant human N-terminal GST-tagged EGFR (669 to 1210 residues) expressed in baculovirus expression system using Srctide as substrate incubated for 1 hr by mobility shift assay | B | 6 | pIC50 | >1000 | nM | IC50 | Eur J Med Chem (2021) 214: 113259-113259 [PMID:33581554] |
| ChEMBL | Inhibition of EGFR (unknown origin) using peptide as substrate after 60 mins by HTRF assay | B | 6 | pIC50 | >1000 | nM | IC50 | Eur J Med Chem (2016) 123: 80-89 [PMID:27474925] |
| ChEMBL | Inhibition of EGFR (unknown origin) after 60 mins | B | 6.05 | pIC50 | 900 | nM | IC50 | J Med Chem (2013) 56: 5675-5690 [PMID:23742252] |
| ChEMBL | Inhibition of GST-tagged human EGFR T790M mutant cytoplasmic domain (668 to 1210 residues) expressed in baculovirus expression system using Poly G:T (4:1) as substrate after 30 mins by Z-LYTE assay | B | 7.55 | pIC50 | 28 | nM | IC50 | Eur J Med Chem (2017) 136: 497-510 [PMID:28528303] |
| ChEMBL | Inhibition of GST-tagged human EGFR T790M/L858R double mutant cytoplasmic domain (668 to 1210 residues) expressed in baculovirus expression system using Poly G:T (4:1) as substrate after 30 mins by Z-LYTE assay | B | 7.72 | pIC50 | 19 | nM | IC50 | Eur J Med Chem (2017) 136: 497-510 [PMID:28528303] |
| ChEMBL | Inhibition of EGFR L858R mutant (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay | B | 5.52 | pEC50 | 3000 | nM | EC50 | Eur J Med Chem (2017) 136: 497-510 [PMID:28528303] |
| ChEMBL | Inhibition of wild type EGFR (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay | B | 5.52 | pEC50 | >3000 | nM | EC50 | Eur J Med Chem (2017) 136: 497-510 [PMID:28528303] |
| ChEMBL | Inhibition of EGFR T790M exon19 deletion double mutant (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay | B | 5.58 | pEC50 | 2660 | nM | EC50 | Eur J Med Chem (2017) 136: 497-510 [PMID:28528303] |
| ChEMBL | Inhibition of EGFR exon19 deletion mutant (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay | B | 5.6 | pEC50 | 2500 | nM | EC50 | Eur J Med Chem (2017) 136: 497-510 [PMID:28528303] |
| ChEMBL | Inhibition of EGFR T790M/L858R double mutant (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay | B | 5.6 | pEC50 | 2500 | nM | EC50 | Eur J Med Chem (2017) 136: 497-510 [PMID:28528303] |
| discoidin domain receptor tyrosine kinase 1/Epithelial discoidin domain-containing receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5319] [GtoPdb: 1843] [UniProtKB: Q08345] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| eukaryotic translation initiation factor 2 alpha kinase 1/Eukaryotic translation initiation factor 2-alpha kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6029] [GtoPdb: 2015] [UniProtKB: Q9BQI3] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Exosome RNA helicase MTR4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105889] [UniProtKB: P42285] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Ferrochelatase, mitochondrial in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3879831] [UniProtKB: P22830] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| fibroblast growth factor receptor 1/Fibroblast growth factor receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3650] [GtoPdb: 1808] [UniProtKB: P11362] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| fibroblast growth factor receptor 2/Fibroblast growth factor receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4142] [GtoPdb: 1809] [UniProtKB: P21802] | ||||||||
| ChEMBL | Inhibition of FGFR2 (unknown origin) after 60 mins | B | 6.59 | pIC50 | 260 | nM | IC50 | J Med Chem (2013) 56: 5675-5690 [PMID:23742252] |
| fibroblast growth factor receptor 3/Fibroblast growth factor receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2742] [GtoPdb: 1810] [UniProtKB: P22607] | ||||||||
| ChEMBL | Inhibition of TEL-fused FGFR3 (unknown origin) by cell-based assay | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2013) 56: 5675-5690 [PMID:23742252] |
| ChEMBL | Inhibition of FGFR3 (unknown origin) after 60 mins | B | 6.37 | pIC50 | 430 | nM | IC50 | J Med Chem (2013) 56: 5675-5690 [PMID:23742252] |
| fibroblast growth factor receptor 4/Fibroblast growth factor receptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3973] [GtoPdb: 1811] [UniProtKB: P22455] | ||||||||
| ChEMBL | Inhibition of FGFR4 (unknown origin) after 60 mins | B | 6.02 | pIC50 | 950 | nM | IC50 | J Med Chem (2013) 56: 5675-5690 [PMID:23742252] |
| protein tyrosine kinase 2/Focal adhesion kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2695] [GtoPdb: 2180] [UniProtKB: Q05397] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 6.66 | pKd | 218 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| General transcription and DNA repair factor IIH helicase subunit XPD in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105743] [UniProtKB: P18074] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Glycine--tRNA ligase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105815] [UniProtKB: P41250] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Glycogen phosphorylase, brain form in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3856] [UniProtKB: P11216] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Glycogen phosphorylase, liver form in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2568] [UniProtKB: P06737] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| glycogen synthase kinase 3 alpha/Glycogen synthase kinase-3 alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2850] [GtoPdb: 2029] [UniProtKB: P49840] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| glycogen synthase kinase 3 beta/Glycogen synthase kinase-3 beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL262] [GtoPdb: 2030] [UniProtKB: P49841] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Inhibition of GSK3beta (unknown origin) after 60 mins | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2013) 56: 5675-5690 [PMID:23742252] |
| G protein-coupled receptor kinase 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6144] [GtoPdb: 1470] [UniProtKB: P43250] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| GTP-binding nuclear protein Ran in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1741190] [UniProtKB: P62826] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| GTP-binding protein 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105780] [UniProtKB: Q9BZE4] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Guanine nucleotide-binding protein G(i) subunit alpha-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105887] [UniProtKB: P04899] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Haem oxygenase 2/Heme oxygenase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2546] [GtoPdb: 1442] [UniProtKB: P30519] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| MET proto-oncogene, receptor tyrosine kinase/Hepatocyte growth factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3717] [GtoPdb: 1815] [UniProtKB: P08581] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Inhibition of cMET (unknown origin) after 60 mins | B | 5.5 | pIC50 | 3170 | nM | IC50 | J Med Chem (2013) 56: 5675-5690 [PMID:23742252] |
| ChEMBL | Inhibition of TEL-fused MET (unknown origin) by cell-based assay | B | 5.87 | pIC50 | 1339 | nM | IC50 | J Med Chem (2013) 56: 5675-5690 [PMID:23742252] |
| ChEMBL | Inhibition of recombinant human N-terminal GST-tagged c-MET cytoplasmic domain (956 to 1390 residues) expressed in baculovirus expression system using peptide substrate after 1 hr by mobility shift assay | B | 6 | pIC50 | >1000 | nM | IC50 | Eur J Med Chem (2018) 143: 123-136 [PMID:29174809] |
| ChEMBL | Inhibition of c-Met (unknown origin) using peptide as substrate after 60 mins by HTRF assay | B | 6 | pIC50 | >1000 | nM | IC50 | Eur J Med Chem (2016) 123: 80-89 [PMID:27474925] |
| ChEMBL | Inhibition of c-MET (unknown origin) | B | 6 | pIC50 | >1000 | nM | IC50 | Bioorg Med Chem Lett (2022) 75: 128990-128990 [PMID:36113668] |
| ChEMBL | Inhibition of c-Met (unknown origin) using peptide substrate incubated for 60 mins in presence of ATP by HTRF assay | B | 6 | pIC50 | >1000 | nM | IC50 | Bioorg Med Chem (2020) 28: 115719-115719 [PMID:33069075] |
| ChEMBL | Inhibition of recombinant human N-terminal GST-tagged MET (956 to 1390 residues) cytoplasmic domain expressed in baculovirus expression system using Srctide as substrate incubated for 1 hr by mobility shift assay | B | 6.57 | pIC50 | 271 | nM | IC50 | Bioorg Med Chem (2019) 27: 115051-115051 [PMID:31492532] |
| neurotrophic receptor tyrosine kinase 1/High affinity nerve growth factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2815] [GtoPdb: 1817] [UniProtKB: P04629] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Inhibition of TEL-fused TRKA (unknown origin) by cell-based assay | B | 5.56 | pIC50 | 2727 | nM | IC50 | J Med Chem (2013) 56: 5675-5690 [PMID:23742252] |
| inhibitor of nuclear factor kappa B kinase subunit epsilon/Inhibitor of nuclear factor kappa-B kinase subunit epsilon in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3529] [GtoPdb: 2040] [UniProtKB: Q14164] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Insulin-like growth factor I receptor/Insulin-like growth factor 1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1957] [GtoPdb: 1801] [UniProtKB: P08069] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.72 | pKd | 19217 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Inhibition of TEL-fused IGF1 receptor (unknown origin) by cell-based assay | B | 6.39 | pIC50 | 410 | nM | IC50 | J Med Chem (2013) 56: 5675-5690 [PMID:23742252] |
| ChEMBL | Inhibition of IGF1 receptor (unknown origin) after 60 mins | B | 8.1 | pIC50 | 8 | nM | IC50 | J Med Chem (2013) 56: 5675-5690 [PMID:23742252] |
| GtoPdb | - | - | 8.1 | pIC50 | 8 | nM | IC50 | J Med Chem (2013) 56: 5675-90 [PMID:23742252] |
| Insulin receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1981] [GtoPdb: 1800] [UniProtKB: P06213] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 5.41 | pKd | 3887 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Inhibition of TEL-fused insulin receptor (unknown origin) expressed in mouse BAF3 cells after 2 to 3 days by luciferase reporter gene assay | B | 6.5 | pIC50 | 319.5 | nM | IC50 | J Med Chem (2013) 56: 5675-5690 [PMID:23742252] |
| ChEMBL | Inhibition of Tel fused InsR (unknown origin) expressed in mouse BaF3 cells assessed as reduction in cell proliferation incubated for 2 to 3 days by Bright-Glo luciferase assay | B | 6.5 | pIC50 | 319 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 1090-1096 [PMID:26750252] |
| ChEMBL | Inhibition of insulin receptor (unknown origin) by homogeneous time resolved fluorescence assay | B | 7.03 | pIC50 | 93 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 3992-3998 [PMID:26235945] |
| ChEMBL | Inhibition of insulin receptor kinase (unknown origin) using TK as substrate after 30 mins by HTRF assay | B | 7.62 | pIC50 | 24 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 2185-2191 [PMID:28385505] |
| GtoPdb | - | - | 8.15 | pIC50 | 7 | nM | IC50 | J Med Chem (2013) 56: 5675-90 [PMID:23742252] |
| ChEMBL | Inhibition of insulin receptor (unknown origin) after 60 mins | B | 8.15 | pIC50 | 7 | nM | IC50 | J Med Chem (2013) 56: 5675-5690 [PMID:23742252] |
| integrin linked kinase/Integrin-linked protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5247] [GtoPdb: 2041] [UniProtKB: Q13418] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| interleukin 1 receptor associated kinase 1/Interleukin-1 receptor-associated kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3357] [GtoPdb: 2042] [UniProtKB: P51617] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| interleukin 1 receptor associated kinase 3/Interleukin-1 receptor-associated kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5081] [GtoPdb: 2044] [UniProtKB: Q9Y616] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| interleukin 1 receptor associated kinase 4/Interleukin-1 receptor-associated kinase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3778] [GtoPdb: 2045] [UniProtKB: Q9NWZ3] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| LIM domain kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3836] [GtoPdb: 2054] [UniProtKB: P53667] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| LIM domain kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5932] [GtoPdb: 2055] [UniProtKB: P53671] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Long-chain-fatty-acid--CoA ligase 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105818] [UniProtKB: Q9ULC5] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| macrophage stimulating 1 receptor/Macrophage-stimulating protein receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2689] [GtoPdb: 1816] [UniProtKB: Q04912] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| MAPK activated protein kinase 2/MAP kinase-activated protein kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2208] [GtoPdb: 2094] [UniProtKB: P49137] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| MAPK activated protein kinase 3/MAP kinase-activated protein kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4670] [GtoPdb: 2095] [UniProtKB: Q16644] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| MAPK activated protein kinase 5/MAP kinase-activated protein kinase 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3094] [GtoPdb: 2096] [UniProtKB: Q8IW41] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| MAPK interacting serine/threonine kinase 2/MAP kinase-interacting serine/threonine-protein kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4204] [GtoPdb: 2105] [UniProtKB: Q9HBH9] | ||||||||
| ChEMBL | Inhibition of MKNK2 (unknown origin) after 60 mins | B | 5.65 | pIC50 | 2240 | nM | IC50 | J Med Chem (2013) 56: 5675-5690 [PMID:23742252] |
| microtubule affinity regulating kinase 3/MAP/microtubule affinity-regulating kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5600] [GtoPdb: 2099] [UniProtKB: P27448] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| microtubule affinity regulating kinase 4/MAP/microtubule affinity-regulating kinase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5754] [GtoPdb: 2100] [UniProtKB: Q96L34] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| KIT proto-oncogene, receptor tyrosine kinase/Mast/stem cell growth factor receptor Kit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1936] [GtoPdb: 1805] [UniProtKB: P10721] | ||||||||
| ChEMBL | Inhibition of TEL-fused cKIT (unknown origin) by cell-based assay | B | 5.54 | pIC50 | 2855 | nM | IC50 | J Med Chem (2013) 56: 5675-5690 [PMID:23742252] |
| ChEMBL | Inhibition of cKIT (unknown origin) after 60 mins | B | 5.89 | pIC50 | 1280 | nM | IC50 | J Med Chem (2013) 56: 5675-5690 [PMID:23742252] |
| maternal embryonic leucine zipper kinase/Maternal embryonic leucine zipper kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4578] [GtoPdb: 2102] [UniProtKB: Q14680] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| protein kinase, membrane associated tyrosine/threonine 1/Membrane-associated tyrosine- and threonine-specific cdc2-inhibitory kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3984] [GtoPdb: 2167] [UniProtKB: Q99640] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Midasin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105779] [UniProtKB: Q9NU22] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| misshapen like kinase 1/Misshapen-like kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5518] [GtoPdb: 2103] [UniProtKB: Q8N4C8] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| mitogen-activated protein kinase 1/Mitogen-activated protein kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4040] [GtoPdb: 1495] [UniProtKB: P28482] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| mitogen-activated protein kinase 10/Mitogen-activated protein kinase 10 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2637] [GtoPdb: 1498] [UniProtKB: P53779] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| mitogen-activated protein kinase 11/Mitogen-activated protein kinase 11 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3961] [GtoPdb: 1500] [UniProtKB: Q15759] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| mitogen-activated protein kinase 14/Mitogen-activated protein kinase 14 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL260] [GtoPdb: 1499] [UniProtKB: Q16539] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| mitogen-activated protein kinase 15/Mitogen-activated protein kinase 15 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5198] [GtoPdb: 2090] [UniProtKB: Q8TD08] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| mitogen-activated protein kinase 3/Mitogen-activated protein kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3385] [GtoPdb: 1494] [UniProtKB: P27361] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| mitogen-activated protein kinase 7/Mitogen-activated protein kinase 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5332] [GtoPdb: 2093] [UniProtKB: Q13164] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 5.01 | pKd | 9851 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| mitogen-activated protein kinase 8/Mitogen-activated protein kinase 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2276] [GtoPdb: 1496] [UniProtKB: P45983] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| mitogen-activated protein kinase 9/Mitogen-activated protein kinase 9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4179] [GtoPdb: 1497] [UniProtKB: P45984] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| mitogen-activated protein kinase kinase kinase 1/Mitogen-activated protein kinase kinase kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3956] [GtoPdb: 2069] [UniProtKB: Q13233] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| mitogen-activated protein kinase kinase kinase 11/Mitogen-activated protein kinase kinase kinase 11 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2708] [GtoPdb: 2071] [UniProtKB: Q16584] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| mitogen-activated protein kinase kinase kinase 2/Mitogen-activated protein kinase kinase kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5914] [GtoPdb: 2077] [UniProtKB: Q9Y2U5] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ZAK sterile alpha motif and leucine zipper containing kinase AZK/Mitogen-activated protein kinase kinase kinase 20 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3886] [GtoPdb: 2289] [UniProtKB: Q9NYL2] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| mitogen-activated protein kinase kinase kinase 3/Mitogen-activated protein kinase kinase kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5970] [GtoPdb: 2078] [UniProtKB: Q99759] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| mitogen-activated protein kinase kinase kinase 4/Mitogen-activated protein kinase kinase kinase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4853] [GtoPdb: 2079] [UniProtKB: Q9Y6R4] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| mitogen-activated protein kinase kinase kinase 5/Mitogen-activated protein kinase kinase kinase 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5285] [GtoPdb: 2080] [UniProtKB: Q99683] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| mitogen-activated protein kinase kinase kinase 6/Mitogen-activated protein kinase kinase kinase 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1163123] [GtoPdb: 2081] [UniProtKB: O95382] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| mitogen-activated protein kinase kinase kinase kinase 1/Mitogen-activated protein kinase kinase kinase kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5749] [GtoPdb: 2085] [UniProtKB: Q92918] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| mitogen-activated protein kinase kinase kinase kinase 2/Mitogen-activated protein kinase kinase kinase kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5330] [GtoPdb: 2086] [UniProtKB: Q12851] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| mitogen-activated protein kinase kinase kinase kinase 3/Mitogen-activated protein kinase kinase kinase kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5432] [GtoPdb: 2087] [UniProtKB: Q8IVH8] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| mitogen-activated protein kinase kinase kinase kinase 4/Mitogen-activated protein kinase kinase kinase kinase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6166] [GtoPdb: 2088] [UniProtKB: O95819] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| mitogen-activated protein kinase kinase kinase kinase 5/Mitogen-activated protein kinase kinase kinase kinase 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4852] [GtoPdb: 2089] [UniProtKB: Q9Y4K4] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| BUB1 mitotic checkpoint serine/threonine kinase/Mitotic checkpoint serine/threonine-protein kinase BUB1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1772932] [GtoPdb: 1949] [UniProtKB: O43683] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Myosin-14 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105888] [UniProtKB: Q7Z406] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| myosin light chain kinase 3/Myosin light chain kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4627] [GtoPdb: 2110] [UniProtKB: Q32MK0] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| myosin light chain kinase/Myosin light chain kinase, smooth muscle in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2428] [GtoPdb: 1552] [UniProtKB: Q15746] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| NADH dehydrogenase [ubiquinone] 1 alpha subcomplex subunit 13 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105781] [UniProtKB: Q9P0J0] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| tyrosine kinase non receptor 1/Non-receptor tyrosine-protein kinase TNK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5334] [GtoPdb: 2245] [UniProtKB: Q13470] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 7.57 | pKd | 27 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| tyrosine kinase 2/Non-receptor tyrosine-protein kinase TYK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3553] [GtoPdb: 2269] [UniProtKB: P29597] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| NUAK family, SNF1-like kinase, 2/NUAK family SNF1-like kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5698] [GtoPdb: 2130] [UniProtKB: Q9H093] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Peroxisomal acyl-coenzyme A oxidase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105748] [UniProtKB: Q15067] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Peroxisomal acyl-coenzyme A oxidase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105817] [UniProtKB: O15254] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Phenylalanine--tRNA ligase beta subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105969] [UniProtKB: Q9NSD9] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Phosphatidylethanolamine-binding protein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105856] [UniProtKB: P30086] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| phosphatidylinositol-5-phosphate 4-kinase type 2 alpha/Phosphatidylinositol 5-phosphate 4-kinase type-2 alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795194] [GtoPdb: 2858] [UniProtKB: P48426] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| phosphatidylinositol-5-phosphate 4-kinase type 2 gamma/Phosphatidylinositol 5-phosphate 4-kinase type-2 gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1770034] [GtoPdb: 2163] [UniProtKB: Q8TBX8] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| phosphorylase kinase catalytic subunit gamma 2/Phosphorylase b kinase gamma catalytic chain, liver/testis isoform in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2349] [GtoPdb: 2147] [UniProtKB: P15735] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| platelet derived growth factor receptor alpha/Platelet-derived growth factor receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2007] [GtoPdb: 1803] [UniProtKB: P16234] | ||||||||
| ChEMBL | Inhibition of PDGFRalpha (unknown origin) after 60 mins | B | 5.94 | pIC50 | 1140 | nM | IC50 | J Med Chem (2013) 56: 5675-5690 [PMID:23742252] |
| platelet derived growth factor receptor beta/Platelet-derived growth factor receptor beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1913] [GtoPdb: 1804] [UniProtKB: P09619] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Probable ATP-dependent RNA helicase DDX6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105783] [UniProtKB: P26196] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| protein kinase C alpha/Protein kinase C alpha type in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL299] [GtoPdb: 1482] [UniProtKB: P17252] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| protein kinase C beta/Protein kinase C beta type in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3045] [GtoPdb: 1483] [UniProtKB: P05771] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| protein kinase C delta/Protein kinase C delta type in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2996] [GtoPdb: 1485] [UniProtKB: Q05655] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| protein kinase C iota/Protein kinase C iota type in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2598] [GtoPdb: 1490] [UniProtKB: P41743] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| protein kinase C theta/Protein kinase C theta type in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3920] [GtoPdb: 1488] [UniProtKB: Q04759] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| protein kinase C zeta/Protein kinase C zeta type in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3438] [GtoPdb: 1491] [UniProtKB: Q05513] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| protein tyrosine kinase 2 beta/Protein-tyrosine kinase 2-beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5469] [GtoPdb: 2181] [UniProtKB: Q14289] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.74 | pKd | 18357 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| protein tyrosine kinase 6/Protein-tyrosine kinase 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4601] [GtoPdb: 2182] [UniProtKB: Q13882] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ret proto-oncogene/Proto-oncogene tyrosine-protein kinase receptor Ret in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2041] [GtoPdb: 2185] [UniProtKB: P07949] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Inhibition of TEL-fused RET (unknown origin) by cell-based assay | B | 5.64 | pIC50 | 2304 | nM | IC50 | J Med Chem (2013) 56: 5675-5690 [PMID:23742252] |
| ChEMBL | Inhibition of RET (unknown origin) after 60 mins | B | 6.4 | pIC50 | 400 | nM | IC50 | J Med Chem (2013) 56: 5675-5690 [PMID:23742252] |
| c-ros oncogene 1, receptor tyrosine kinase/Proto-oncogene tyrosine-protein kinase ROS in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5568] [GtoPdb: 1840] [UniProtKB: P08922] | ||||||||
| ChEMBL | Inhibition of ROS1 G2032R mutant (unknown origin) | B | 6.64 | pKi | 230 | nM | Ki | Eur J Med Chem (2017) 134: 348-356 [PMID:28431340] |
| ChEMBL | Binding affinity to recombinant human ROS1 G2032R mutant assessed as inhibition constant in presence of ATP by microfluidic mobility shift assay | B | 6.64 | pKi | 230 | nM | Ki | Proc Natl Acad Sci U S A (2015) 112: 3493-3498 [PMID:25733882] |
| ChEMBL | Inhibition of wild type ROS1 (unknown origin) | B | 9.15 | pKi | 0.7 | nM | Ki | Eur J Med Chem (2017) 134: 348-356 [PMID:28431340] |
| ChEMBL | Binding affinity to recombinant human ROS1 assessed as inhibition constant in presence of ATP by microfluidic mobility shift assay | B | 9.15 | pKi | 0.7 | nM | Ki | Proc Natl Acad Sci U S A (2015) 112: 3493-3498 [PMID:25733882] |
| ChEMBL | Inhibition of ROS1 L2026M mutant (unknown origin) | B | 9.4 | pKi | 0.4 | nM | Ki | Eur J Med Chem (2017) 134: 348-356 [PMID:28431340] |
| ChEMBL | Binding affinity to recombinant human ROS1 L2026M mutant assessed as inhibition constant in presence of ATP by microfluidic mobility shift assay | B | 9.4 | pKi | 0.4 | nM | Ki | Proc Natl Acad Sci U S A (2015) 112: 3493-3498 [PMID:25733882] |
| ChEMBL | Inhibition of human N-terminal GST-tagged ROS cytoplasmic domain (1883 to 2347 residues) expressed in baculovirus expression system after 1 hr by mobility shift assay | B | 5.7 | pIC50 | 2000 | nM | IC50 | Eur J Med Chem (2018) 158: 322-333 [PMID:30223120] |
| ChEMBL | Inhibition of TEL-fused ROS (unknown origin) by cell-based assay | B | 6.85 | pIC50 | 141.8 | nM | IC50 | J Med Chem (2013) 56: 5675-5690 [PMID:23742252] |
| ChEMBL | Inhibition of wild-type ROS1 (unknown origin) | B | 7.52 | pIC50 | 30 | nM | IC50 | Eur J Med Chem (2023) 257: 115477-115477 [PMID:37210839] |
| ChEMBL | Inhibition of recombinant human N-terminal GST-tagged ROS (1883 to 2347 residues) cytoplasmic domain expressed in baculovirus expression system using IRS1 as substrate incubated for 1 hr by mobility shift assay | B | 8.37 | pIC50 | 4.3 | nM | IC50 | Bioorg Med Chem (2019) 27: 115051-115051 [PMID:31492532] |
| ChEMBL | Inhibition of N-terminal GST-tagged human ROS1 cytoplasmic domain (1883 to 2347 residues) expressed in Baculovirus expression system using IRS1 as substrate incubated for 1 hr by mobility shift assay | B | 8.51 | pIC50 | 3.1 | nM | IC50 | Eur J Med Chem (2019) 171: 297-309 [PMID:30927566] |
| ChEMBL | Inhibition of recombinant human N-terminal GST-tagged ROS1 (1883 to 2347 residues) expressed in baculovirus expression system using IRS1 as substrate incubated for 1 hr by mobility shift assay | B | 8.66 | pIC50 | 2.2 | nM | IC50 | Eur J Med Chem (2021) 214: 113259-113259 [PMID:33581554] |
| ChEMBL | Inhibition of recombinant human N-terminal GST-tagged ROS1 cytoplasmic domain (1883 to 2347 residues) expressed in baculovirus expression system using peptide substrate after 1 hr by mobility shift assay | B | 8.7 | pIC50 | 2 | nM | IC50 | Eur J Med Chem (2018) 143: 123-136 [PMID:29174809] |
| ChEMBL | Inhibition of ROS1 (unknown origin) using peptide substrate incubated for 60 mins in presence of ATP by HTRF assay | B | 8.7 | pIC50 | 2 | nM | IC50 | Bioorg Med Chem (2020) 28: 115719-115719 [PMID:33069075] |
| ChEMBL | Inhibition of ROS1 (unknown origin) using peptide as substrate after 60 mins by HTRF assay | B | 8.7 | pIC50 | 2 | nM | IC50 | Eur J Med Chem (2016) 123: 80-89 [PMID:27474925] |
| SRC proto-oncogene, non-receptor tyrosine kinase/Proto-oncogene tyrosine-protein kinase Src in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL267] [GtoPdb: 2206] [UniProtKB: P12931] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Inhibition of TEL-fused SRC (unknown origin) by cell-based assay | B | 5.77 | pIC50 | 1694 | nM | IC50 | J Med Chem (2013) 56: 5675-5690 [PMID:23742252] |
| Putative heat shock protein HSP 90-beta 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105858] [UniProtKB: Q58FF8] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Pyridoxal kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075181] [UniProtKB: O00764] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Rab-like protein 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105853] [UniProtKB: Q5HYI8] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| AKT serine/threonine kinase 1/RAC-alpha serine/threonine-protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4282] [GtoPdb: 1479] [UniProtKB: P31749] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| AKT serine/threonine kinase 2/RAC-beta serine/threonine-protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2431] [GtoPdb: 1480] [UniProtKB: P31751] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| AKT serine/threonine kinase 3/RAC-gamma serine/threonine-protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4816] [GtoPdb: 2286] [UniProtKB: Q9Y243] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Ras-related protein Rab-10 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105971] [UniProtKB: P61026] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| RAB27A, member RAS oncogene family/Ras-related protein Rab-27A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105702] [GtoPdb: 2916] [UniProtKB: P51159] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Ras-related protein Rab-6A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105703] [UniProtKB: P20340] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| receptor interacting serine/threonine kinase 2/Receptor-interacting serine/threonine-protein kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5014] [GtoPdb: 2190] [UniProtKB: O43353] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| receptor interacting serine/threonine kinase 3/Receptor-interacting serine/threonine-protein kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795199] [GtoPdb: 2191] [UniProtKB: Q9Y572] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| fms related receptor tyrosine kinase 3/Receptor-type tyrosine-protein kinase FLT3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 5.37 | pKd | 4255 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Inhibition of TEL-fused FLT3 (unknown origin) by cell-based assay | B | 5.5 | pIC50 | 3143 | nM | IC50 | J Med Chem (2013) 56: 5675-5690 [PMID:23742252] |
| ChEMBL | Inhibition of N-terminal GST-tagged human FLT3 cytoplasmic domain (564 to 993 residues) expressed in baculovirus infected Sf21 insect cells using Srctide as substrate measured after 1 hr by mobility shift assay | B | 7.06 | pIC50 | 86.4 | nM | IC50 | Bioorg Med Chem (2021) 37: 116108-116108 [PMID:33756437] |
| GtoPdb | - | - | 7.22 | pIC50 | 60 | nM | IC50 | J Med Chem (2013) 56: 5675-90 [PMID:23742252] |
| ChEMBL | Inhibition of FLT3 (unknown origin) after 60 mins | B | 7.22 | pIC50 | 60 | nM | IC50 | J Med Chem (2013) 56: 5675-5690 [PMID:23742252] |
| Rho associated coiled-coil containing protein kinase 1/Rho-associated protein kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3231] [GtoPdb: 1503] [UniProtKB: Q13464] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Rho associated coiled-coil containing protein kinase 2/Rho-associated protein kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2973] [GtoPdb: 1504] [UniProtKB: O75116] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Inhibition of ROCK2 (unknown origin) after 60 mins | B | 5.9 | pIC50 | 1270 | nM | IC50 | J Med Chem (2013) 56: 5675-5690 [PMID:23742252] |
| ribosomal protein S6 kinase A1/Ribosomal protein S6 kinase alpha-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2553] [GtoPdb: 1527] [UniProtKB: Q15418] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.67 | pKd | 21402 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ribosomal protein S6 kinase A3/Ribosomal protein S6 kinase alpha-3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2345] [GtoPdb: 1528] [UniProtKB: P51812] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ribosomal protein S6 kinase A4/Ribosomal protein S6 kinase alpha-4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3125] [GtoPdb: 1524] [UniProtKB: O75676] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ribosomal protein S6 kinase A5/Ribosomal protein S6 kinase alpha-5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4237] [GtoPdb: 1523] [UniProtKB: O75582] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ribosomal protein S6 kinase A6/Ribosomal protein S6 kinase alpha-6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4924] [GtoPdb: 1530] [UniProtKB: Q9UK32] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ribosomal protein S6 kinase B1/Ribosomal protein S6 kinase beta-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4501] [GtoPdb: 1525] [UniProtKB: P23443] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Ribosyldihydronicotinamide dehydrogenase [quinone] in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3959] [UniProtKB: P16083] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| RNA cytidine acetyltransferase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105935] [UniProtKB: Q9H0A0] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| S-adenosylmethionine synthase isoform type-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3313835] [UniProtKB: P31153] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Septin-9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105891] [UniProtKB: Q9UHD8] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| serine/threonine kinase 10/Serine/threonine-protein kinase 10 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3981] [GtoPdb: 2211] [UniProtKB: O94804] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| serine/threonine kinase 16/Serine/threonine-protein kinase 16 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3938] [GtoPdb: 2213] [UniProtKB: O75716] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| serine/threonine-protein kinase MST4/Serine/threonine-protein kinase 26 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5941] [GtoPdb: 2287] [UniProtKB: Q9P289] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| serine/threonine kinase 3/Serine/threonine-protein kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4708] [GtoPdb: 2219] [UniProtKB: Q13188] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Serine/threonine kinase 38/Serine/threonine-protein kinase 38 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075155] [GtoPdb: 1517] [UniProtKB: Q15208] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Serine/threonine kinase 38 like/Serine/threonine-protein kinase 38-like in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4851] [GtoPdb: 1518] [UniProtKB: Q9Y2H1] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| serine/threonine kinase 4/Serine/threonine-protein kinase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4598] [GtoPdb: 2225] [UniProtKB: Q13043] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| A-Raf proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase A-Raf in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1169596] [GtoPdb: 1933] [UniProtKB: P10398] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ATR checkpoint kinase/Serine/threonine-protein kinase ATR in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5024] [GtoPdb: 1935] [UniProtKB: Q13535] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| B-Raf proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase B-raf in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5145] [GtoPdb: 1943] [UniProtKB: P15056] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| checkpoint kinase 1/Serine/threonine-protein kinase Chk1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4630] [GtoPdb: 1987] [UniProtKB: O14757] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| protein kinase D2/Serine/threonine-protein kinase D2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4900] [GtoPdb: 2173] [UniProtKB: Q9BZL6] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| protein kinase D3/Serine/threonine-protein kinase D3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2595] [GtoPdb: 2174] [UniProtKB: O94806] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| endoplasmic reticulum to nucleus signaling 1/Serine/threonine-protein kinase/endoribonuclease IRE1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1163101] [GtoPdb: 2020] [UniProtKB: O75460] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| endoplasmic reticulum to nucleus signaling 2/Serine/threonine-protein kinase/endoribonuclease IRE2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105932] [GtoPdb: 2021] [UniProtKB: Q76MJ5] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ciliogenesis associated kinase 1/Serine/threonine-protein kinase ICK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1163126] [GtoPdb: 2038] [UniProtKB: Q9UPZ9] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| large tumor suppressor kinase 1/Serine/threonine-protein kinase LATS1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6167] [GtoPdb: 1515] [UniProtKB: O95835] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| microtubule affinity regulating kinase 2/Serine/threonine-protein kinase MARK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3831] [GtoPdb: 2098] [UniProtKB: Q7KZI7] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| CDC42 binding protein kinase alpha/Serine/threonine-protein kinase MRCK alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4516] [GtoPdb: 1507] [UniProtKB: Q5VT25] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| CDC42 binding protein kinase beta/Serine/threonine-protein kinase MRCK beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5052] [GtoPdb: 1508] [UniProtKB: Q9Y5S2] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| CDC42 binding protein kinase gamma/Serine/threonine-protein kinase MRCK gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5615] [GtoPdb: 1506] [UniProtKB: Q6DT37] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| protein kinase N1/Serine/threonine-protein kinase N1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3384] [GtoPdb: 1520] [UniProtKB: Q16512] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| protein kinase N2/Serine/threonine-protein kinase N2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3032] [GtoPdb: 1521] [UniProtKB: Q16513] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| protein kinase N3/Serine/threonine-protein kinase N3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3627581] [GtoPdb: 1522] [UniProtKB: Q6P5Z2] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| NIMA related kinase 1/Serine/threonine-protein kinase Nek1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5855] [GtoPdb: 2114] [UniProtKB: Q96PY6] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| NIMA related kinase 2/Serine/threonine-protein kinase Nek2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3835] [GtoPdb: 2117] [UniProtKB: P51955] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| NIMA related kinase 3/Serine/threonine-protein kinase Nek3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5679] [GtoPdb: 2118] [UniProtKB: P51956] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| NIMA related kinase 7/Serine/threonine-protein kinase Nek7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4849] [GtoPdb: 2122] [UniProtKB: Q8TDX7] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| NIMA related kinase 9/Serine/threonine-protein kinase Nek9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5257] [GtoPdb: 2124] [UniProtKB: Q8TD19] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| nemo like kinase/Serine/threonine-protein kinase NLK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5364] [GtoPdb: 2125] [UniProtKB: Q9UBE8] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| p21 (RAC1) activated kinase 2/Serine/threonine-protein kinase PAK 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4487] [GtoPdb: 2134] [UniProtKB: Q13177] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Inhibition of PAK2 (unknown origin) after 60 mins | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2013) 56: 5675-5690 [PMID:23742252] |
| p21 (RAC1) activated kinase 4/Serine/threonine-protein kinase PAK 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4482] [GtoPdb: 2136] [UniProtKB: O96013] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| p21 (RAC1) activated kinase 6/Serine/threonine-protein kinase PAK 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4311] [GtoPdb: 2137] [UniProtKB: Q9NQU5] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Pim-1 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase pim-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2147] [GtoPdb: 2158] [UniProtKB: P11309] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Pim-2 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase pim-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523] [GtoPdb: 2159] [UniProtKB: Q9P1W9] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| polo like kinase 1/Serine/threonine-protein kinase PLK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3024] [GtoPdb: 2168] [UniProtKB: P53350] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| polo like kinase 4/Serine/threonine-protein kinase PLK4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3788] [GtoPdb: 2171] [UniProtKB: O00444] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 5.15 | pKd | 7100 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| salt inducible kinase 2/Serine/threonine-protein kinase SIK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5699] [GtoPdb: 2198] [UniProtKB: Q9H0K1] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| SIK family kinase 3/Serine/threonine-protein kinase SIK3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6149] [GtoPdb: 2199] [UniProtKB: Q9Y2K2] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| serine/threonine kinase 11/Serine/threonine-protein kinase STK11 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5606] [GtoPdb: 2212] [UniProtKB: Q15831] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| TAO kinase 1/Serine/threonine-protein kinase TAO1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5261] [GtoPdb: 2233] [UniProtKB: Q7L7X3] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| TAO kinase 2/Serine/threonine-protein kinase TAO2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075195] [GtoPdb: 2234] [UniProtKB: Q9UL54] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| TAO kinase 3/Serine/threonine-protein kinase TAO3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5701] [GtoPdb: 2235] [UniProtKB: Q9H2K8] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| TANK binding kinase 1/Serine/threonine-protein kinase TBK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5408] [GtoPdb: 2237] [UniProtKB: Q9UHD2] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| unc-51 like autophagy activating kinase 1/Serine/threonine-protein kinase ULK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6006] [GtoPdb: 2271] [UniProtKB: O75385] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| unc-51 like kinase 3/Serine/threonine-protein kinase ULK3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5047] [GtoPdb: 2273] [UniProtKB: Q6PHR2] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Signal recognition particle receptor subunit alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105934] [UniProtKB: P08240] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| STE20 like kinase/STE20-like serine/threonine-protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4202] [GtoPdb: 2200] [UniProtKB: Q9H2G2] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| STE20 related adaptor alpha/STE20-related kinase adapter protein alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795198] [GtoPdb: 2227] [UniProtKB: Q7RTN6] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Structural maintenance of chromosomes protein 1A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105747] [UniProtKB: Q14683] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Structural maintenance of chromosomes protein 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105890] [UniProtKB: O95347] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Succinate--CoA ligase [ADP-forming] subunit beta, mitochondrial in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105973] [UniProtKB: Q9P2R7] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| testis specific serine kinase 1B/Testis-specific serine/threonine-protein kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6003] [GtoPdb: 2257] [UniProtKB: Q9BXA7] | ||||||||
| ChEMBL | Inhibition of STK22D (unknown origin) after 60 mins | B | 7.64 | pIC50 | 23 | nM | IC50 | J Med Chem (2013) 56: 5675-5690 [PMID:23742252] |
| GtoPdb | - | - | 7.64 | pIC50 | 23 | nM | IC50 | J Med Chem (2013) 56: 5675-90 [PMID:23742252] |
| transforming growth factor beta receptor 1/TGF-beta receptor type-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4439] [GtoPdb: 1788] [UniProtKB: P36897] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| transforming growth factor beta receptor 2/TGF-beta receptor type-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4267] [GtoPdb: 1795] [UniProtKB: P37173] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Thyroid hormone receptor-associated protein 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105820] [UniProtKB: Q9Y2W1] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| TRAF2 and NCK interacting kinase/TRAF2 and NCK-interacting protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4527] [GtoPdb: 2244] [UniProtKB: Q9UKE5] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Transcription factor ETV6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2401606] [UniProtKB: P41212] | ||||||||
| ChEMBL | Inhibition of wild-type TEL (unknown origin) by cell-based assay | B | 5.49 | pIC50 | 3250 | nM | IC50 | J Med Chem (2013) 56: 5675-5690 [PMID:23742252] |
| ABL proto-oncogene 1, non-receptor tyrosine kinase/Tyrosine-protein kinase ABL1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1862] [GtoPdb: 1923] [UniProtKB: P00519] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Inhibition of ABL (unknown origin) after 60 mins | B | 5.9 | pIC50 | 1250 | nM | IC50 | J Med Chem (2013) 56: 5675-5690 [PMID:23742252] |
| ABL proto-oncogene 2, non-receptor tyrosine kinase/Tyrosine-protein kinase ABL2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4014] [GtoPdb: 1924] [UniProtKB: P42684] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Bruton tyrosine kinase/Tyrosine-protein kinase BTK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5251] [GtoPdb: 1948] [UniProtKB: Q06187] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Inhibition of BTK (unknown origin) after 60 mins | B | 5.47 | pIC50 | 3360 | nM | IC50 | J Med Chem (2013) 56: 5675-5690 [PMID:23742252] |
| C-terminal Src kinase/Tyrosine-protein kinase CSK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2634] [GtoPdb: 1994] [UniProtKB: P41240] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| FER tyrosine kinase/Tyrosine-protein kinase Fer in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3982] [GtoPdb: 2022] [UniProtKB: P16591] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 6.67 | pKd | 214 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| FES proto-oncogene, tyrosine kinase/Tyrosine-protein kinase Fes/Fps in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5455] [GtoPdb: 2023] [UniProtKB: P07332] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 5.76 | pKd | 1742 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| FGR proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase Fgr in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4454] [GtoPdb: 2024] [UniProtKB: P09769] | ||||||||
| ChEMBL | Inhibition of TEL-fused FGR (unknown origin) by cell-based assay | B | 5.71 | pIC50 | 1947 | nM | IC50 | J Med Chem (2013) 56: 5675-5690 [PMID:23742252] |
| fyn related Src family tyrosine kinase/Tyrosine-protein kinase FRK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4223] [GtoPdb: 2025] [UniProtKB: P42685] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| FYN proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase Fyn in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1841] [GtoPdb: 2026] [UniProtKB: P06241] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| HCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase HCK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3234] [GtoPdb: 2032] [UniProtKB: P08631] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Janus kinase 1/Tyrosine-protein kinase JAK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2835] [GtoPdb: 2047] [UniProtKB: P23458] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Inhibition of JAK1 (unknown origin) after 60 mins | B | 5.43 | pIC50 | 3730 | nM | IC50 | J Med Chem (2013) 56: 5675-5690 [PMID:23742252] |
| Janus kinase 2/Tyrosine-protein kinase JAK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2971] [GtoPdb: 2048] [UniProtKB: O60674] | ||||||||
| ChEMBL | Inhibition of TEL-fused JAK2 (unknown origin) by cell-based assay | B | 5.67 | pIC50 | 2160 | nM | IC50 | J Med Chem (2013) 56: 5675-5690 [PMID:23742252] |
| ChEMBL | Inhibition of JAK2 (unknown origin) after 60 mins | B | 6.21 | pIC50 | 610 | nM | IC50 | J Med Chem (2013) 56: 5675-5690 [PMID:23742252] |
| Janus kinase 3/Tyrosine-protein kinase JAK3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2148] [GtoPdb: 2049] [UniProtKB: P52333] | ||||||||
| ChEMBL | Inhibition of JAK3 (unknown origin) after 60 mins | B | 5.1 | pIC50 | 7920 | nM | IC50 | J Med Chem (2013) 56: 5675-5690 [PMID:23742252] |
| LCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase Lck in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL258] [GtoPdb: 2053] [UniProtKB: P06239] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Inhibition of TEL-fused LCK (unknown origin) by cell-based assay | B | 6.17 | pIC50 | 672 | nM | IC50 | J Med Chem (2013) 56: 5675-5690 [PMID:23742252] |
| ChEMBL | Inhibition of LCK (unknown origin) after 60 mins | B | 6.25 | pIC50 | 560 | nM | IC50 | J Med Chem (2013) 56: 5675-5690 [PMID:23742252] |
| LYN proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase Lyn in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3905] [GtoPdb: 2060] [UniProtKB: P07948] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Inhibition of TEL-fused LYN (unknown origin) by cell-based assay | B | 5.64 | pIC50 | 2306 | nM | IC50 | J Med Chem (2013) 56: 5675-5690 [PMID:23742252] |
| ChEMBL | Inhibition of LYN (unknown origin) after 60 mins | B | 6.08 | pIC50 | 840 | nM | IC50 | J Med Chem (2013) 56: 5675-5690 [PMID:23742252] |
| MER proto-oncogene, tyrosine kinase/Tyrosine-protein kinase Mer in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5331] [GtoPdb: 1837] [UniProtKB: Q12866] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| spleen associated tyrosine kinase/Tyrosine-protein kinase SYK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2599] [GtoPdb: 2230] [UniProtKB: P43405] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Inhibition of SYK (unknown origin) after 60 mins | B | 5.52 | pIC50 | 3050 | nM | IC50 | J Med Chem (2013) 56: 5675-5690 [PMID:23742252] |
| tec protein tyrosine kinase/Tyrosine-protein kinase Tec in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4246] [GtoPdb: 2238] [UniProtKB: P42680] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| YES proto-oncogene 1, Src family tyrosine kinase/Tyrosine-protein kinase Yes in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2073] [GtoPdb: 2284] [UniProtKB: P07947] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| zeta chain of T cell receptor associated protein kinase 70/Tyrosine-protein kinase ZAP-70 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2803] [GtoPdb: 2285] [UniProtKB: P43403] | ||||||||
| ChEMBL | Inhibition of ZAP70 (unknown origin) after 60 mins | B | 5.01 | pIC50 | 9700 | nM | IC50 | J Med Chem (2013) 56: 5675-5690 [PMID:23742252] |
| Tyrosine--tRNA ligase, cytoplasmic in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3179] [UniProtKB: P54577] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| U5 small nuclear ribonucleoprotein 200 kDa helicase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105972] [UniProtKB: O75643] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| aarF domain containing kinase 5/Uncharacterized aarF domain-containing protein kinase 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105886] [GtoPdb: 1929] [UniProtKB: Q3MIX3] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Uncharacterized protein FLJ45252 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105933] [UniProtKB: Q6ZSR9] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| kinase insert domain receptor/Vascular endothelial growth factor receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL279] [GtoPdb: 1813] [UniProtKB: P35968] | ||||||||
| ChEMBL | Inhibition of TEL-fused KDR (unknown origin) by cell-based assay | B | 5.38 | pIC50 | 4210 | nM | IC50 | J Med Chem (2013) 56: 5675-5690 [PMID:23742252] |
| Very long-chain specific acyl-CoA dehydrogenase, mitochondrial in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105892] [UniProtKB: P49748] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Kv11.1/Voltage-gated inwardly rectifying potassium channel KCNH2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
| ChEMBL | Inhibition of human ERG by patch-clamp technique | B | 4.34 | pIC50 | 46000 | nM | IC50 | J Med Chem (2013) 56: 5675-5690 [PMID:23742252] |
| ChEMBL | Inhibition of human ERG by patch clamp method | B | 4.34 | pIC50 | 46000 | nM | IC50 | J Med Chem (2013) 56: 5673-5674 [PMID:23837797] |
| ChEMBL | Inhibition of human ERG by dofetilide binding assay | B | 5.9 | pIC50 | 1250 | nM | IC50 | J Med Chem (2013) 56: 5675-5690 [PMID:23742252] |
| WEE1 G2 checkpoint kinase/Wee1-like protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5491] [GtoPdb: 2278] [UniProtKB: P30291] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
ChEMBL data shown on this page come from version 36:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]
