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| ChEMBL ligand: CHEMBL1673046 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| phosphoinositide kinase, FYVE-type zinc finger containing/1-phosphatidylinositol 3-phosphate 5-kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1938222] [GtoPdb: 2857] [UniProtKB: Q9Y2I7] | ||||||||
| ChEMBL | Inhibition of PIP5K3 in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| 3-phosphoinositide dependent protein kinase 1/3-phosphoinositide-dependent protein kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2534] [GtoPdb: 1519] [UniProtKB: O15530] | ||||||||
| ChEMBL | Inhibition of PDK1 in human HeLa cells lysate pre incubated for 15 mins followed by ADP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| 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 | Inhibition of AMPKalpha1 in human HeLa cells lysate pre incubated for 15 mins followed by ADP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| protein kinase AMP-activated catalytic subunit alpha 2/5`-AMP-activated protein kinase catalytic subunit alpha-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2116] [GtoPdb: 1542] [UniProtKB: P54646] | ||||||||
| ChEMBL | Inhibition of AMPKalpha2 in human HeLa cells lysate pre incubated for 15 mins followed by ADP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| tyrosine kinase non receptor 2/Activated CDC42 kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4599] [GtoPdb: 2246] [UniProtKB: Q07912] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (KiNativ method in HeLa cells)) EUB0000122b TNK2 | B | 4.74 | pIC50 | 18000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomics Library wave 3 |
| ChEMBL | Inhibition of ACK1 in human HeLa cells lysate pre incubated for 15 mins followed by ADP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.74 | pIC50 | 18000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| Acylglycerol kinase, mitochondrial in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2417354] [UniProtKB: Q53H12] | ||||||||
| ChEMBL | Inhibition of AGK in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| protein kinase AMP-activated catalytic subunit alpha 2/protein kinase AMP-activated catalytic subunit alpha 1/AMPK alpha1/alpha2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3038454] [GtoPdb: 1542, 1541] [UniProtKB: P54646, Q13131] | ||||||||
| ChEMBL | Inhibition of AMPKalpha1/2 in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| ChEMBL | Inhibition of AMPKalpha1/2 in human HeLa cells lysate pre incubated for 15 mins followed by ADP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| aurora kinase A/Aurora kinase A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4722] [GtoPdb: 1936] [UniProtKB: O14965] | ||||||||
| ChEMBL | Inhibition of AURA in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| bromodomain containing 4/Bromodomain-containing protein 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1163125] [GtoPdb: 1945] [UniProtKB: O60885] | ||||||||
| ChEMBL | Inhibition of BRD4 (unknown origin) | B | 5.8 | pKd | 1600 | nM | Kd | Eur J Med Chem (2019) 178: 530-543 [PMID:31212132] |
| ChEMBL | Binding affinity to recombinant human N-terminal hexaHis-tagged BRD4 expressed in Escherichia coli BL21 (DE3) cells by MST assay | B | 6.1 | pKd | 800 | nM | Kd | J Med Chem (2021) 64: 15772-15786 [PMID:34710325] |
| ChEMBL | Binding affinity to recombinant human N-terminal hexaHis-tagged BRD4 expressed in Escherichia coli BL21 (DE3) cells by ITC analysis | B | 6.13 | pKd | 735 | nM | Kd | J Med Chem (2021) 64: 15772-15786 [PMID:34710325] |
| ChEMBL | Binding affinity to recombinant human N-terminal hexaHis-tagged BRD4 expressed in Escherichia coli BL21 (DE3) cells by qPCR assay | B | 6.69 | pKd | 205 | nM | Kd | J Med Chem (2021) 64: 15772-15786 [PMID:34710325] |
| bromodomain testis associated/Bromodomain testis-specific protein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795185] [GtoPdb: 2729] [UniProtKB: Q58F21] | ||||||||
| ChEMBL | Binding affinity to recombinant human N-terminal hexaHis-tagged BRDT expressed in Escherichia coli BL21 (DE3) cells by ITC analysis | B | 5.38 | pKd | 4200 | nM | Kd | J Med Chem (2021) 64: 15772-15786 [PMID:34710325] |
| ChEMBL | Binding affinity to recombinant human N-terminal hexaHis-tagged BRDT expressed in Escherichia coli BL21 (DE3) cells by MST assay | B | 5.46 | pKd | 3500 | nM | Kd | J Med Chem (2021) 64: 15772-15786 [PMID:34710325] |
| ChEMBL | Binding affinity to recombinant human N-terminal hexaHis-tagged BRDT expressed in Escherichia coli BL21 (DE3) cells by qPCR assay | B | 6.17 | pKd | 675 | nM | Kd | J Med Chem (2021) 64: 15772-15786 [PMID:34710325] |
| calcium/calmodulin dependent protein kinase kinase 1/Calcium/calmodulin-dependent protein kinase kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5256] [GtoPdb: 1956] [UniProtKB: Q8N5S9] | ||||||||
| ChEMBL | Inhibition of CAMKK1 in human HeLa cells lysate pre incubated for 15 mins followed by ADP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| calcium/calmodulin dependent protein kinase ID/Calcium/calmodulin-dependent protein kinase type 1D in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5073] [GtoPdb: 1953] [UniProtKB: Q8IU85] | ||||||||
| ChEMBL | Inhibition of CAMK1d in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| ChEMBL | Inhibition of CAMK1d in human HeLa cells lysate pre incubated for 15 mins followed by ADP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| 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 | Inhibition of CAMK2d in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| ChEMBL | Inhibition of CAMK2d in human HeLa cells lysate pre incubated for 15 mins followed by ADP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| 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 | Inhibition of CAMK2g in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| ChEMBL | Inhibition of CAMK2g in human HeLa cells lysate pre incubated for 15 mins followed by ADP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| casein kinase 1 alpha 1/Casein kinase I isoform alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2793] [GtoPdb: 1995] [UniProtKB: P48729] | ||||||||
| ChEMBL | Inhibition of CK1alpha in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| cyclin dependent kinase 1/Cyclin-dependent kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL308] [GtoPdb: 1961] [UniProtKB: P06493] | ||||||||
| ChEMBL | Inhibition of CDC2 in human HeLa cells lysate pre incubated for 15 mins followed by ADP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| cyclin dependent kinase 10/Cyclin-dependent kinase 10 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795191] [GtoPdb: 1962] [UniProtKB: Q15131] | ||||||||
| ChEMBL | Inhibition of CDK10 in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| cyclin dependent kinase 11B/Cyclin-dependent kinase 11B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5808] [GtoPdb: 1964] [UniProtKB: P21127] | ||||||||
| ChEMBL | Inhibition of PITSLRE in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| cyclin dependent kinase 12/Cyclin-dependent kinase 12 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3559692] [GtoPdb: 1965] [UniProtKB: Q9NYV4] | ||||||||
| ChEMBL | Inhibition of CRK7 in human HeLa cells lysate pre incubated for 15 mins followed by ADP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| cyclin dependent kinase 13/Cyclin-dependent kinase 13 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795192] [GtoPdb: 1966] [UniProtKB: Q14004] | ||||||||
| ChEMBL | Inhibition of CHED in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| ChEMBL | Inhibition of CHED in human HeLa cells lysate pre incubated for 15 mins followed by ADP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| cyclin dependent kinase 15/Cyclin-dependent kinase 15 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5856] [GtoPdb: 1968] [UniProtKB: Q96Q40] | ||||||||
| ChEMBL | Inhibition of PFTAIRE2 in human HeLa cells lysate pre incubated for 15 mins followed by ADP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| cyclin dependent kinase 16/Cyclin-dependent kinase 16 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4597] [GtoPdb: 1969] [UniProtKB: Q00536] | ||||||||
| ChEMBL | Inhibition of PCTAIRE1 in human HeLa cells lysate pre incubated for 15 mins followed by ADP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| cyclin dependent kinase 2/Cyclin-dependent kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL301] [GtoPdb: 1973] [UniProtKB: P24941] | ||||||||
| ChEMBL | Inhibition of CDK2 K1 site in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| ChEMBL | Inhibition of CDK2 K2 site in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| ChEMBL | Inhibition of CDK2 K1 site in human HeLa cells lysate pre incubated for 15 mins followed by ADP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| ChEMBL | Inhibition of CDK2 K2 site in human HeLa cells lysate pre incubated for 15 mins followed by ADP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| cyclin dependent kinase 5/Cyclin-dependent kinase 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4036] [GtoPdb: 1977] [UniProtKB: Q00535] | ||||||||
| ChEMBL | Inhibition of CDK5 in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| ChEMBL | Inhibition of CDK5 in human HeLa cells lysate pre incubated for 15 mins followed by ADP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| cyclin dependent kinase 7/Cyclin-dependent kinase 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3055] [GtoPdb: 1979] [UniProtKB: P50613] | ||||||||
| ChEMBL | Inhibition of CDK7 in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| cyclin dependent kinase 9/Cyclin-dependent kinase 9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3116] [GtoPdb: 1981] [UniProtKB: P50750] | ||||||||
| ChEMBL | Inhibition of CDK9 in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| ChEMBL | Inhibition of CDK9 in human HeLa cells lysate pre incubated for 15 mins followed by ADP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| protein kinase, DNA-activated, catalytic subunit/DNA-dependent protein kinase catalytic subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3142] [GtoPdb: 2800] [UniProtKB: P78527] | ||||||||
| ChEMBL | Inhibition of PRKDC in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| ChEMBL | Inhibition of PRKDC in human HeLa cells lysate pre incubated for 15 mins followed by ADP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| 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 | Inhibition of MAP2K1 in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| ChEMBL | Inhibition of MAP2K1 in human HeLa cells lysate pre incubated for 15 mins followed by ADP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| 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 | Inhibition of MAP2K3 in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| ChEMBL | Inhibition of MAP2K3 in human HeLa cells lysate pre incubated for 15 mins followed by ADP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| mitogen-activated protein kinase kinase 4/Dual specificity mitogen-activated protein kinase kinase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2897] [GtoPdb: 2065] [UniProtKB: P45985] | ||||||||
| ChEMBL | Inhibition of MAP2K4 in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| ChEMBL | Inhibition of MAP2K4 in human HeLa cells lysate pre incubated for 15 mins followed by ADP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| 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 | Inhibition of MAP2K5 in human HeLa cells lysate pre incubated for 15 mins followed by ADP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| 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 | Inhibition of MAP2K6 in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| ChEMBL | Inhibition of MAP2K6 in human HeLa cells lysate pre incubated for 15 mins followed by ADP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| mitogen-activated protein kinase kinase 7/Dual specificity mitogen-activated protein kinase kinase 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3530] [GtoPdb: 2068] [UniProtKB: O14733] | ||||||||
| ChEMBL | Inhibition of MAP2K7 in human HeLa cells lysate pre incubated for 15 mins followed by ADP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| CDC like kinase 3/Dual specificity protein kinase CLK3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4226] [GtoPdb: 1992] [UniProtKB: P49761] | ||||||||
| ChEMBL | Inhibition of CLK3 in human HeLa cells lysate pre incubated for 15 mins followed by ADP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| eukaryotic translation initiation factor 2 alpha kinase 4/eIF-2-alpha kinase GCN2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5358] [GtoPdb: 2018] [UniProtKB: Q9P2K8] | ||||||||
| ChEMBL | Inhibition of GCN2 in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| TP53 regulating kinase/EKC/KEOPS complex subunit TP53RK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1938223] [GtoPdb: 2248] [UniProtKB: Q96S44] | ||||||||
| ChEMBL | Inhibition of PRPK in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| ChEMBL | Inhibition of PRPK in human HeLa cells lysate pre incubated for 15 mins followed by ADP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| EPH receptor A2/Ephrin type-A receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2068] [GtoPdb: 1822] [UniProtKB: P29317] | ||||||||
| ChEMBL | Inhibition of EphA2 in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| EPH receptor B4/Ephrin type-B receptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5147] [GtoPdb: 1833] [UniProtKB: P54760] | ||||||||
| ChEMBL | Inhibition of EphB4 in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| ChEMBL | Inhibition of EphB4 in human HeLa cells lysate pre incubated for 15 mins followed by ADP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| epidermal growth factor receptor/Epidermal growth factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533] | ||||||||
| ChEMBL | Inhibition of EGFR in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| ChEMBL | Inhibition of EGFR in human HeLa cells lysate pre incubated for 15 mins followed by ADP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| eukaryotic elongation factor 2 kinase/Eukaryotic elongation factor 2 kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5026] [GtoPdb: 2014] [UniProtKB: O00418] | ||||||||
| ChEMBL | Inhibition of EEF2K in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| eukaryotic translation initiation factor 2 alpha kinase 3/Eukaryotic translation initiation factor 2-alpha kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6030] [GtoPdb: 2017] [UniProtKB: Q9NZJ5] | ||||||||
| ChEMBL | Inhibition of PEK in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| protein tyrosine kinase 2/Focal adhesion kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2695] [GtoPdb: 2180] [UniProtKB: Q05397] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (KiNativ method in HeLa cells)) EUB0000122b PTK2 | B | 4.41 | pIC50 | 39000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomics Library wave 3 |
| ChEMBL | Inhibition of FAK in human HeLa cells lysate pre incubated for 15 mins followed by ADP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.41 | pIC50 | 39000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| glycogen synthase kinase 3 alpha/Glycogen synthase kinase-3 alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2850] [GtoPdb: 2029] [UniProtKB: P49840] | ||||||||
| ChEMBL | Inhibition of GSK3A in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| glycogen synthase kinase 3 beta/Glycogen synthase kinase-3 beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL262] [GtoPdb: 2030] [UniProtKB: P49841] | ||||||||
| ChEMBL | Inhibition of GSK3B isoform 2 in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| ChEMBL | Inhibition of GSK3B isoform 2 in human HeLa cells lysate pre incubated for 15 mins followed by ADP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| MET proto-oncogene, receptor tyrosine kinase/Hepatocyte growth factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3717] [GtoPdb: 1815] [UniProtKB: P08581] | ||||||||
| ChEMBL | Inhibition of MET in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| inhibitor of nuclear factor kappa B kinase subunit epsilon/TANK binding kinase 1/IKK epsilon/TBK1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3038486] [GtoPdb: 2040, 2237] [UniProtKB: Q14164, Q9UHD2] | ||||||||
| ChEMBL | Inhibition of IKKE/TBK1 in human HeLa cells lysate pre incubated for 15 mins followed by ADP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| component of inhibitor of nuclear factor kappa B kinase complex/Inhibitor of nuclear factor kappa-B kinase subunit alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3476] [GtoPdb: 1989] [UniProtKB: O15111] | ||||||||
| ChEMBL | Inhibition of IKKA in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| inhibitor of nuclear factor kappa B kinase subunit beta/Inhibitor of nuclear factor kappa-B kinase subunit beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1991] [GtoPdb: 2039] [UniProtKB: O14920] | ||||||||
| ChEMBL | Inhibition of IKKB in human HeLa cells lysate pre incubated for 15 mins followed by ADP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| 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 | Inhibition of IGF1R in human HeLa cells lysate pre incubated for 15 mins followed by ADP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| Insulin receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1981] [GtoPdb: 1800] [UniProtKB: P06213] | ||||||||
| ChEMBL | Inhibition of INSR in human HeLa cells lysate pre incubated for 15 mins followed by ADP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| integrin linked kinase/Integrin-linked protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5247] [GtoPdb: 2041] [UniProtKB: Q13418] | ||||||||
| ChEMBL | Inhibition of ILK in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| eukaryotic translation initiation factor 2 alpha kinase 2/Interferon-induced, double-stranded RNA-activated protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5785] [GtoPdb: 2016] [UniProtKB: P19525] | ||||||||
| ChEMBL | Inhibition of PKR in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| ChEMBL | Inhibition of PKR in human HeLa cells lysate pre incubated for 15 mins followed by ADP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| 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 | Inhibition of IRAK1 in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| 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 | Inhibition of IRAK4 in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| ChEMBL | Inhibition of IRAK4 in human HeLa cells lysate pre incubated for 15 mins followed by ADP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| leucine rich repeat kinase 2/Leucine-rich repeat serine/threonine-protein kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075104] [GtoPdb: 2059] [UniProtKB: Q5S007] | ||||||||
| ChEMBL | Inhibition of LRRK2 G2019S mutant (unknown origin) using LRRKtide as substrate incubated for 1 hrs in presence of ATP by Adapta TR-FRET assay | B | 7.23 | pIC50 | 59 | nM | IC50 | Eur J Med Chem (2013) 70: 758-767 [PMID:24239623] |
| ChEMBL | Inhibition of recombinant human GST-tagged LRRK2 catalytic domain (970 to 2527 residues) expressed in baculovirus expression system using LRRKtide as substrate measured after 1 hr by Alexa fluor-647 ADP tracer-based ADAPTA assay | B | 7.34 | pIC50 | 46 | nM | IC50 | J Med Chem (2020) 63: 7817-7826 [PMID:32530623] |
| macrophage stimulating 1 receptor/Macrophage-stimulating protein receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2689] [GtoPdb: 1816] [UniProtKB: Q04912] | ||||||||
| ChEMBL | Inhibition of RON in human HeLa cells lysate pre incubated for 15 mins followed by ADP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| microtubule affinity regulating kinase 3/MAP/microtubule affinity-regulating kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5600] [GtoPdb: 2099] [UniProtKB: P27448] | ||||||||
| ChEMBL | Inhibition of MARK3 in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| ChEMBL | Inhibition of MARK3 in human HeLa cells lysate pre incubated for 15 mins followed by ADP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| Microtubule associated serine/threonine kinase 3/Microtubule-associated serine/threonine-protein kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2417352] [GtoPdb: 1512] [UniProtKB: O60307] | ||||||||
| ChEMBL | Inhibition of MAST3 in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| mitogen-activated protein kinase 1/Mitogen-activated protein kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4040] [GtoPdb: 1495] [UniProtKB: P28482] | ||||||||
| ChEMBL | Inhibition of ERK2 in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| mitogen-activated protein kinase 14/Mitogen-activated protein kinase 14 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL260] [GtoPdb: 1499] [UniProtKB: Q16539] | ||||||||
| ChEMBL | Inhibition of P38a in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| ChEMBL | Inhibition of P38a interaction site in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| mitogen-activated protein kinase 3/Mitogen-activated protein kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3385] [GtoPdb: 1494] [UniProtKB: P27361] | ||||||||
| ChEMBL | Inhibition of ERK1 in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| ChEMBL | Inhibition of ERK1 in human HeLa cells lysate pre incubated for 15 mins followed by ADP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| mitogen-activated protein kinase 4/Mitogen-activated protein kinase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5759] [GtoPdb: 2091] [UniProtKB: P31152] | ||||||||
| ChEMBL | Inhibition of ERK4 in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| mitogen-activated protein kinase 7/Mitogen-activated protein kinase 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5332] [GtoPdb: 2093] [UniProtKB: Q13164] | ||||||||
| ChEMBL | In vitro Erk5 : In vitro Erk5 binding assay: Ambit Kd values in nanomolar. Kd values generated by Ambit binding assay over a concentration range of the compound. | B | 7.1 | pKd | 80 | nM | Kd | US-9266890-B2. Pyrimido-diazepinone kinase scaffold compounds and methods of treating disorders (2016) |
| ChEMBL | Affinity Biochemical interaction (ATP-binding displacement assay) EUB0000122b MAPK7 | B | 7.1 | pKd | 80 | nM | Kd | Affinity Biochemical Literature for EUbOPEN Chemogenomics Library wave 3 |
| ChEMBL | Selectivity interaction (Kinase panel (ATP-site competition binding assay)) EUB0000122b MAPK7 | B | 7.1 | pKd | 80 | nM | Kd | Selectivity Literature for EUbOPEN Chemogenomics Library wave 3 |
| ChEMBL | Binding affinity to ERK5 (unknown origin) assessed as dissociation constant by ATP-competition binding assay | B | 7.1 | pKd | 80 | nM | Kd | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| GtoPdb | - | - | 7.1 | pKd | 80 | nM | Kd | Cancer Cell (2010) 18: 258-67 [PMID:20832753] |
| ChEMBL | Inhibition of ERK5 in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 5.82 | pIC50 | 1500 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| ChEMBL | Affinity On-target Cellular interaction (KiNativ assay (HeLa cell lysate)) EUB0000122b MAPK7 | B | 5.82 | pIC50 | 1500 | nM | IC50 | Affinity On-target Cellular Literature for EUbOPEN Chemogenomics Library wave 3 |
| ChEMBL | Inhibition of N-terminal 6His-tagged human ERK5 expressed in baculovirus infected Sf21 cells co-expressing HA-tagged human MEK5-DD using ARKKRRHPSGPPTA peptide as substrate incubated for 20 mins in presence of [gamma-32P]-ATP by radiochemical assay | B | 6.44 | pIC50 | 364 | nM | IC50 | Eur J Med Chem (2013) 70: 758-767 [PMID:24239623] |
| ChEMBL | Inhibition of ERK5 in human HeLa cells incubated for 15 mins prior to ATP addition by KiNativ profiling method | B | 6.52 | pIC50 | 300 | nM | IC50 | Eur J Med Chem (2019) 178: 530-543 [PMID:31212132] |
| ChEMBL | Inhibition of ERK5 (unknown origin) | B | 6.62 | pIC50 | 240 | nM | IC50 | J Med Chem (2023) 66: 4491-4502 [PMID:37002872] |
| ChEMBL | Inhibition of EGF-induced BMK1 autophosphorylation in human HeLa cells by SDS-PAGE analysis | B | 6.62 | pIC50 | 240 | nM | IC50 | ACS Med Chem Lett (2011) 2: 195-200 [PMID:21412406] |
| ChEMBL | Inhibition of His-tagged MAP2K5 activated N-terminal GST-tagged recombinant human ERK5 (1 to 398 residues) expressed in Escherichia coli using biotin-Ahx-PPGDYSTTPGGTLFSTTPGGTRI peptide as substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins in presence of ATP by TR-FRET assay | B | 6.7 | pIC50 | 200 | nM | IC50 | J Med Chem (2019) 62: 928-940 [PMID:30563338] |
| ChEMBL | Inhibition of ERK5 (unknown origin) by ADP-Glo kinase assay | B | 7.28 | pIC50 | 52.3 | nM | IC50 | J Med Chem (2023) 66: 13568-13586 [PMID:37751283] |
| ChEMBL | Affinity Phenotypic Cellular interaction (Reduction of BMK1-dependent transactivating activity of MEF2C) EUB0000122b MAPK7 | B | 5.3 | pEC50 | <5000 | nM | EC50 | Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomics Library wave 3 |
| ChEMBL | Inhibition of EGF-stimulated ERK5 autophosphorylation in human HeLa cells preincubated with compound for 1 hrs followed by EGF stimulation for 17 mins by SDS-PAGE analysis | B | 6.62 | pEC50 | 240 | nM | EC50 | Eur J Med Chem (2013) 70: 758-767 [PMID:24239623] |
| 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 | Inhibition of MAP3K1 in human HeLa cells lysate pre incubated for 15 mins followed by ADP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| 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 | Inhibition of MLK3 in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| 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 | Inhibition of MAP3K2 in human HeLa cells lysate pre incubated for 15 mins followed by ADP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| 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 | Inhibition of ZAK in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| 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 | Inhibition of MAP3K4 in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| 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 | Inhibition of MAP3K5 in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| mitogen-activated protein kinase kinase kinase 7/Mitogen-activated protein kinase kinase kinase 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5776] [GtoPdb: 2082] [UniProtKB: O43318] | ||||||||
| ChEMBL | Inhibition of TAK1 in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| mitogen-activated protein kinase kinase kinase 8/Mitogen-activated protein kinase kinase kinase 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4899] [GtoPdb: 2083] [UniProtKB: P41279] | ||||||||
| ChEMBL | Inhibition of COT in human HeLa cells lysate pre incubated for 15 mins followed by ADP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| 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 | Inhibition of GCK in human HeLa cells lysate pre incubated for 15 mins followed by ADP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| mixed lineage kinase domain like pseudokinase/Mixed lineage kinase domain-like protein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1938217] [GtoPdb: 2106] [UniProtKB: Q8NB16] | ||||||||
| ChEMBL | Inhibition of MLKL in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| ChEMBL | Inhibition of MLKL in human HeLa cells lysate pre incubated for 15 mins followed by ADP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| tyrosine kinase non receptor 1/Non-receptor tyrosine-protein kinase TNK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5334] [GtoPdb: 2245] [UniProtKB: Q13470] | ||||||||
| GtoPdb | - | - | 6.05 | pKd | 890 | nM | Kd | Cancer Cell (2010) 18: 258-67 [PMID:20832753] |
| ChEMBL | Selectivity interaction (Kinase panel (ATP-site competition binding assay)) EUB0000122b TNK1 | B | 6.05 | pKd | 890 | nM | Kd | Selectivity Literature for EUbOPEN Chemogenomics Library wave 3 |
| ChEMBL | Binding affinity to TNK1 (unknown origin) assessed as dissociation constant by ATP-competition binding assay | B | 6.05 | pKd | 890 | nM | Kd | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| ChEMBL | Selectivity interaction (Kinase panel (KiNativ method in HeLa cells)) EUB0000122b TNK1 | B | 5 | pIC50 | 10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomics Library wave 3 |
| ChEMBL | Inhibition of TNK1 in human HeLa cells lysate pre incubated for 15 mins followed by ADP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 5 | pIC50 | 10000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| PAN2-PAN3 deadenylation complex subunit PAN3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105985] [UniProtKB: Q58A45] | ||||||||
| ChEMBL | Inhibition of PAN3 in human HeLa cells lysate pre incubated for 15 mins followed by ADP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| calcium/calmodulin dependent serine protein kinase/Peripheral plasma membrane protein CASK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1908381] [GtoPdb: 1959] [UniProtKB: O14936] | ||||||||
| ChEMBL | Inhibition of CASK in human HeLa cells lysate pre incubated for 15 mins followed by ADP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| phosphatidylinositol 3-kinase catalytic subunit type 3/Phosphatidylinositol 3-kinase catalytic subunit type 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075165] [GtoPdb: 2152] [UniProtKB: Q8NEB9] | ||||||||
| ChEMBL | Inhibition of PIK3C3 in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| phosphatidylinositol 4-kinase alpha/Phosphatidylinositol 4-kinase alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3667] [GtoPdb: 2148] [UniProtKB: P42356] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (KiNativ method in HeLa cells)) EUB0000122b PI4KA | B | 4.44 | pIC50 | 36000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomics Library wave 3 |
| ChEMBL | Inhibition of PIK4CA in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.44 | pIC50 | 36000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| phosphatidylinositol 4-kinase beta/Phosphatidylinositol 4-kinase beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3268] [GtoPdb: 2149] [UniProtKB: Q9UBF8] | ||||||||
| ChEMBL | Inhibition of PIK4CB in human HeLa cells lysate pre incubated for 15 mins followed by ADP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| ChEMBL | Inhibition of PIK4CB in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.47 | pIC50 | 34000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| phosphatidylinositol-4-phosphate 3-kinase catalytic subunit type 2 beta/Phosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5554] [GtoPdb: 2151] [UniProtKB: O00750] | ||||||||
| ChEMBL | Inhibition of PIK3C2B in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| 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 | Inhibition of PIP5K2A in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| ChEMBL | Inhibition of PIP5K2A LIP1 labeling site in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| ChEMBL | Inhibition of PIP5K2A in human HeLa cells lysate pre incubated for 15 mins followed by ADP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| ChEMBL | Inhibition of PIP5K2A LIP1 site in human HeLa cells lysate pre incubated for 15 mins followed by ADP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| phosphatidylinositol-5-phosphate 4-kinase type 2 beta/Phosphatidylinositol 5-phosphate 4-kinase type-2 beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5667] [GtoPdb: 2162] [UniProtKB: P78356] | ||||||||
| ChEMBL | Inhibition of PIP5K2B in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| 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 | Inhibition of PIP5K2C in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| 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 | Inhibition of PHKg2 in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| ChEMBL | Inhibition of PHKg2 in human HeLa cells lysate pre incubated for 15 mins followed by ADP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| protein kinase C iota/Protein kinase C iota type in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2598] [GtoPdb: 1490] [UniProtKB: P41743] | ||||||||
| ChEMBL | Inhibition of PKCiota in human HeLa cells lysate pre incubated for 15 mins followed by ADP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| protein kinase C theta/Protein kinase C theta type in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3920] [GtoPdb: 1488] [UniProtKB: Q04759] | ||||||||
| ChEMBL | Inhibition of PKCtheta in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| protein kinase C zeta/Protein kinase C zeta type in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3438] [GtoPdb: 1491] [UniProtKB: Q05513] | ||||||||
| ChEMBL | Inhibition of PKCzeta in human HeLa cells lysate pre incubated for 15 mins followed by ADP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| AKT serine/threonine kinase 1/RAC-alpha serine/threonine-protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4282] [GtoPdb: 1479] [UniProtKB: P31749] | ||||||||
| ChEMBL | Inhibition of AKT1 in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| ribosomal protein S6 kinase A1/Ribosomal protein S6 kinase alpha-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2553] [GtoPdb: 1527] [UniProtKB: Q15418] | ||||||||
| ChEMBL | Inhibition of RSK1 domain 1 in human HeLa cells lysate pre incubated for 15 mins followed by ADP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| ChEMBL | Inhibition of RSK1 domain 2 K2 site in human HeLa cells lysate pre incubated for 15 mins followed by ADP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.51 | pIC50 | 31000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| ChEMBL | Inhibition of RSK1 domain 2 K1 site in human HeLa cells lysate pre incubated for 15 mins followed by ADP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.54 | pIC50 | 29000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| ChEMBL | Inhibition of RSK1 domain 2 in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.59 | pIC50 | 26000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| ribosomal protein S6 kinase A2/Ribosomal protein S6 kinase alpha-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3906] [GtoPdb: 1529] [UniProtKB: Q15349] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (KiNativ method in HeLa cells)) EUB0000122b RPS6KA1 | B | 4.54 | pIC50 | 29000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomics Library wave 3 |
| ribosomal protein S6 kinase A3/Ribosomal protein S6 kinase alpha-3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2345] [GtoPdb: 1528] [UniProtKB: P51812] | ||||||||
| ChEMBL | Inhibition of RSK2 in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| ChEMBL | Inhibition of RSK2 domain 1 in human HeLa cells lysate pre incubated for 15 mins followed by ADP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| ChEMBL | Inhibition of RSK2 domain 2 in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.31 | pIC50 | 49000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| ChEMBL | Selectivity interaction (Kinase panel (KiNativ method in HeLa cells)) EUB0000122b RPS6KA3 | B | 4.33 | pIC50 | 47000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomics Library wave 3 |
| ChEMBL | Inhibition of RSK2 domain 2 K2 site in human HeLa cells lysate pre incubated for 15 mins followed by ADP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.33 | pIC50 | 47000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| ribosomal protein S6 kinase A5/Ribosomal protein S6 kinase alpha-5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4237] [GtoPdb: 1523] [UniProtKB: O75582] | ||||||||
| ChEMBL | Inhibition of MSK1 in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| ChEMBL | Inhibition of MSK1 domain 1 K2 site in human HeLa cells lysate pre incubated for 15 mins followed by ADP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| ChEMBL | Inhibition of MSK1 domain 1 K1 site in human HeLa cells lysate pre incubated for 15 mins followed by ADP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| ribosomal protein S6 kinase B1/Ribosomal protein S6 kinase beta-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4501] [GtoPdb: 1525] [UniProtKB: P23443] | ||||||||
| ChEMBL | Inhibition of P70S6K in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| ribosomal protein S6 kinase B2/Ribosomal protein S6 kinase beta-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3111] [GtoPdb: 1526] [UniProtKB: Q9UBS0] | ||||||||
| ChEMBL | Inhibition of P70S6KB in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| ATM serine/threonine kinase/Serine-protein kinase ATM in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3797] [GtoPdb: 1934] [UniProtKB: Q13315] | ||||||||
| ChEMBL | Inhibition of ATM in human HeLa cells lysate pre incubated for 15 mins followed by ADP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| serine/threonine kinase 10/Serine/threonine-protein kinase 10 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3981] [GtoPdb: 2211] [UniProtKB: O94804] | ||||||||
| ChEMBL | Inhibition of LOK in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| ChEMBL | Inhibition of LOK in human HeLa cells lysate pre incubated for 15 mins followed by ADP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| serine/threonine kinase 16/Serine/threonine-protein kinase 16 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3938] [GtoPdb: 2213] [UniProtKB: O75716] | ||||||||
| ChEMBL | Inhibition of MPSK1 in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| serine/threonine kinase 24/Serine/threonine-protein kinase 24 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5082] [GtoPdb: 2217] [UniProtKB: Q9Y6E0] | ||||||||
| ChEMBL | Inhibition of MST3 in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| ChEMBL | Inhibition of MST3 in human HeLa cells lysate pre incubated for 15 mins followed by ADP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| serine/threonine kinase 3/Serine/threonine-protein kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4708] [GtoPdb: 2219] [UniProtKB: Q13188] | ||||||||
| ChEMBL | Inhibition of MST2 in human HeLa cells lysate pre incubated for 15 mins followed by ADP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| Serine/threonine kinase 38/Serine/threonine-protein kinase 38 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075155] [GtoPdb: 1517] [UniProtKB: Q15208] | ||||||||
| ChEMBL | Inhibition of NDR1 in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| Serine/threonine kinase 38 like/Serine/threonine-protein kinase 38-like in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4851] [GtoPdb: 1518] [UniProtKB: Q9Y2H1] | ||||||||
| ChEMBL | Inhibition of NDR2 in human HeLa cells lysate pre incubated for 15 mins followed by ADP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| serine/threonine kinase 4/Serine/threonine-protein kinase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4598] [GtoPdb: 2225] [UniProtKB: Q13043] | ||||||||
| ChEMBL | Inhibition of MST1 in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| ChEMBL | Inhibition of MST1 in human HeLa cells lysate pre incubated for 15 mins followed by ADP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| 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 | Inhibition of ARAF in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| ATR checkpoint kinase/Serine/threonine-protein kinase ATR in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5024] [GtoPdb: 1935] [UniProtKB: Q13535] | ||||||||
| ChEMBL | Inhibition of ATR in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| 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 | Inhibition of BRAF in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| ChEMBL | Inhibition of BRAF in human HeLa cells lysate pre incubated for 15 mins followed by ADP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| checkpoint kinase 1/Serine/threonine-protein kinase Chk1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4630] [GtoPdb: 1987] [UniProtKB: O14757] | ||||||||
| ChEMBL | Inhibition of CHK1 in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| ChEMBL | Inhibition of CHK1 inactive site in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| checkpoint kinase 2/Serine/threonine-protein kinase Chk2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2527] [GtoPdb: 1988] [UniProtKB: O96017] | ||||||||
| ChEMBL | Inhibition of CHK2 in human HeLa cells lysate pre incubated for 15 mins followed by ADP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| protein kinase D2/Serine/threonine-protein kinase D2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4900] [GtoPdb: 2173] [UniProtKB: Q9BZL6] | ||||||||
| ChEMBL | Inhibition of PKD2 in human HeLa cells lysate pre incubated for 15 mins followed by ADP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| protein kinase D3/Serine/threonine-protein kinase D3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2595] [GtoPdb: 2174] [UniProtKB: O94806] | ||||||||
| ChEMBL | Inhibition of PKD3 in human HeLa cells lysate pre incubated for 15 mins followed by ADP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| doublecortin like kinase 1/Serine/threonine-protein kinase DCLK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5683] [GtoPdb: 2005] [UniProtKB: O15075] | ||||||||
| ChEMBL | Inhibition of recombinant human N-terminal His6-tagged DCLK1 (G351 to H689 residues) expressed in Escherichia coli BL21 DE3 using 5-FAM-KKLRRTLSVA-COOH as substrate measured after 2 hrs by mobility shift assay | B | 6.15 | pIC50 | 716 | nM | IC50 | J Med Chem (2020) 63: 7817-7826 [PMID:32530623] |
| doublecortin like kinase 2/Serine/threonine-protein kinase DCLK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5519] [GtoPdb: 2006] [UniProtKB: Q8N568] | ||||||||
| GtoPdb | - | - | 6.72 | pKd | 190 | nM | Kd | Cancer Cell (2010) 18: 258-67 [PMID:20832753] |
| ChEMBL | Selectivity interaction (Kinase panel (ATP-site competition binding assay)) EUB0000122b DCLK2 | B | 6.72 | pKd | 190 | nM | Kd | Selectivity Literature for EUbOPEN Chemogenomics Library wave 3 |
| ChEMBL | Binding affinity to DCAMKL2 (unknown origin) assessed as dissociation constant by ATP-competition binding assay | B | 6.72 | pKd | 190 | nM | Kd | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| 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 | Inhibition of IRE1 in human HeLa cells lysate pre incubated for 15 mins followed by ADP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| Microtubule associated serine/threonine kinase-like/Serine/threonine-protein kinase greatwall in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105826] [GtoPdb: 1514] [UniProtKB: Q96GX5] | ||||||||
| ChEMBL | Inhibition of MASTL in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| large tumor suppressor kinase 1/Serine/threonine-protein kinase LATS1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6167] [GtoPdb: 1515] [UniProtKB: O95835] | ||||||||
| ChEMBL | Inhibition of LATS1 in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| large tumor suppressor kinase 2/Serine/threonine-protein kinase LATS2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5907] [GtoPdb: 1516] [UniProtKB: Q9NRM7] | ||||||||
| ChEMBL | Inhibition of LATS2 in human HeLa cells lysate pre incubated for 15 mins followed by ADP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| microtubule affinity regulating kinase 1/Serine/threonine-protein kinase MARK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5940] [GtoPdb: 2097] [UniProtKB: Q9P0L2] | ||||||||
| ChEMBL | Inhibition of MARK1 in human HeLa cells lysate pre incubated for 15 mins followed by ADP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| microtubule affinity regulating kinase 2/Serine/threonine-protein kinase MARK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3831] [GtoPdb: 2098] [UniProtKB: Q7KZI7] | ||||||||
| ChEMBL | Inhibition of MARK2 in human HeLa cells lysate pre incubated for 15 mins followed by ADP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| CDC42 binding protein kinase beta/Serine/threonine-protein kinase MRCK beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5052] [GtoPdb: 1508] [UniProtKB: Q9Y5S2] | ||||||||
| ChEMBL | Inhibition of MRCKB in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| mechanistic target of rapamycin kinase/Serine/threonine-protein kinase mTOR in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2842] [GtoPdb: 2109] [UniProtKB: P42345] | ||||||||
| ChEMBL | Inhibition of FRAP in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| protein kinase N2/Serine/threonine-protein kinase N2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3032] [GtoPdb: 1521] [UniProtKB: Q16513] | ||||||||
| ChEMBL | Inhibition of PKN2 in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| NIMA related kinase 1/Serine/threonine-protein kinase Nek1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5855] [GtoPdb: 2114] [UniProtKB: Q96PY6] | ||||||||
| ChEMBL | Inhibition of NEK1 in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| NIMA related kinase 3/Serine/threonine-protein kinase Nek3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5679] [GtoPdb: 2118] [UniProtKB: P51956] | ||||||||
| ChEMBL | Inhibition of NEK3 in human HeLa cells lysate pre incubated for 15 mins followed by ADP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| NIMA related kinase 4/Serine/threonine-protein kinase Nek4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5819] [GtoPdb: 2119] [UniProtKB: P51957] | ||||||||
| ChEMBL | Inhibition of NEK4 in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| NIMA related kinase 7/Serine/threonine-protein kinase Nek7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4849] [GtoPdb: 2122] [UniProtKB: Q8TDX7] | ||||||||
| ChEMBL | Inhibition of NEK7 in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| ChEMBL | Inhibition of NEK7 in human HeLa cells lysate pre incubated for 15 mins followed by ADP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| NIMA related kinase 8/Serine/threonine-protein kinase Nek8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2417353] [GtoPdb: 2123] [UniProtKB: Q86SG6] | ||||||||
| ChEMBL | Inhibition of NEK8 in human HeLa cells lysate pre incubated for 15 mins followed by ADP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| NIMA related kinase 9/Serine/threonine-protein kinase Nek9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5257] [GtoPdb: 2124] [UniProtKB: Q8TD19] | ||||||||
| ChEMBL | Inhibition of NEK9 in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| ChEMBL | Inhibition of NEK9 in human HeLa cells lysate pre incubated for 15 mins followed by ADP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| polo like kinase 1/Serine/threonine-protein kinase PLK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3024] [GtoPdb: 2168] [UniProtKB: P53350] | ||||||||
| ChEMBL | Inhibition of PLK1 K1 site in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| ChEMBL | Inhibition of PLK1 K2 site in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| ChEMBL | Inhibition of PLK1 in human HeLa cells lysate pre incubated for 15 mins followed by ADP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| ChEMBL | Inhibition of PLK1 splice variant in human HeLa cells lysate pre incubated for 15 mins followed by ADP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| polo like kinase 4/Serine/threonine-protein kinase PLK4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3788] [GtoPdb: 2171] [UniProtKB: O00444] | ||||||||
| GtoPdb | - | - | 6.22 | pKd | 600 | nM | Kd | Cancer Cell (2010) 18: 258-67 [PMID:20832753] |
| ChEMBL | Selectivity interaction (Kinase panel (ATP-site competition binding assay)) EUB0000122b PLK4 | B | 6.22 | pKd | 600 | nM | Kd | Selectivity Literature for EUbOPEN Chemogenomics Library wave 3 |
| ChEMBL | Binding affinity to PLK4 (unknown origin) assessed as dissociation constant by ATP-competition binding assay | B | 6.22 | pKd | 600 | nM | Kd | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| pre-mRNA processing factor kinase PRP4K/Serine/threonine-protein kinase PRP4 homolog in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1908382] [GtoPdb: 2177] [UniProtKB: Q13523] | ||||||||
| ChEMBL | Inhibition of PRP4 in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| serum/glucocorticoid regulated kinase 1/Serine/threonine-protein kinase Sgk1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2343] [GtoPdb: 1534] [UniProtKB: O00141] | ||||||||
| ChEMBL | Inhibition of SGK1 in human HeLa cells lysate pre incubated for 15 mins followed by ADP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| serum/glucocorticoid regulated kinase family member 3/Serine/threonine-protein kinase Sgk3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6186] [GtoPdb: 1536] [UniProtKB: Q96BR1] | ||||||||
| ChEMBL | Inhibition of SGK3 K1 site in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| ChEMBL | Inhibition of SGK3 K2 site in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| ChEMBL | Inhibition of SGK3 in human HeLa cells lysate pre incubated for 15 mins followed by ADP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| SMG1 nonsense mediated mRNA decay associated PI3K related kinase/Serine/threonine-protein kinase SMG1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795195] [GtoPdb: 2201] [UniProtKB: Q96Q15] | ||||||||
| ChEMBL | Inhibition of SMG1 in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| TAO kinase 2/Serine/threonine-protein kinase TAO2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075195] [GtoPdb: 2234] [UniProtKB: Q9UL54] | ||||||||
| ChEMBL | Inhibition of TAO2 in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| TAO kinase 3/Serine/threonine-protein kinase TAO3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5701] [GtoPdb: 2235] [UniProtKB: Q9H2K8] | ||||||||
| ChEMBL | Inhibition of TAO3 in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| tousled like kinase 1/Serine/threonine-protein kinase tousled-like 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5388] [GtoPdb: 2242] [UniProtKB: Q9UKI8] | ||||||||
| ChEMBL | Inhibition of TLK1 in human HeLa cells lysate pre incubated for 15 mins followed by ADP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| tousled like kinase 2/Serine/threonine-protein kinase tousled-like 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5404] [GtoPdb: 2243] [UniProtKB: Q86UE8] | ||||||||
| ChEMBL | Inhibition of TLK2 in human HeLa cells lysate pre incubated for 15 mins followed by ADP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| unc-51 like autophagy activating kinase 2/Serine/threonine-protein kinase ULK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5435] [GtoPdb: 2272] [UniProtKB: Q8IYT8] | ||||||||
| ChEMBL | Inhibition of ULK2 in human HeLa cells lysate pre incubated for 15 mins followed by ADP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| unc-51 like kinase 3/Serine/threonine-protein kinase ULK3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5047] [GtoPdb: 2273] [UniProtKB: Q6PHR2] | ||||||||
| ChEMBL | Inhibition of ULK3 in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| ChEMBL | Inhibition of ULK3 in human HeLa cells lysate pre incubated for 15 mins followed by ADP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| WNK lysine deficient protein kinase 1/Serine/threonine-protein kinase WNK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075173] [GtoPdb: 2280] [UniProtKB: Q9H4A3] | ||||||||
| ChEMBL | Inhibition of Wnk1 in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| SRSF protein kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4375] [GtoPdb: 2208] [UniProtKB: Q96SB4] | ||||||||
| ChEMBL | Inhibition of SRPK1 in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| STE20 like kinase/STE20-like serine/threonine-protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4202] [GtoPdb: 2200] [UniProtKB: Q9H2G2] | ||||||||
| ChEMBL | Inhibition of SLK in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| ChEMBL | Inhibition of SLK in human HeLa cells lysate pre incubated for 15 mins followed by ADP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| STE20 related adaptor beta/STE20-related kinase adapter protein beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105756] [GtoPdb: 2228] [UniProtKB: Q9C0K7] | ||||||||
| ChEMBL | Inhibition of ALS2CR2 in human HeLa cells lysate pre incubated for 15 mins followed by ADP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| tripartite motif containing 28/Transcription intermediary factor 1-beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3769297] [GtoPdb: 2253] [UniProtKB: Q13263] | ||||||||
| ChEMBL | Inhibition of TIF1b in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| C-terminal Src kinase/Tyrosine-protein kinase CSK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2634] [GtoPdb: 1994] [UniProtKB: P41240] | ||||||||
| ChEMBL | Inhibition of CSK in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| ChEMBL | Inhibition of CSK in human HeLa cells lysate pre incubated for 15 mins followed by ADP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| FER tyrosine kinase/Tyrosine-protein kinase Fer in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3982] [GtoPdb: 2022] [UniProtKB: P16591] | ||||||||
| ChEMBL | Inhibition of FER in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| FYN proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase Fyn in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1841] [GtoPdb: 2026] [UniProtKB: P06241] | ||||||||
| ChEMBL | Inhibition of FYN in human HeLa cells lysate pre incubated for 15 mins followed by ADP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| Janus kinase 1/Tyrosine-protein kinase JAK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2835] [GtoPdb: 2047] [UniProtKB: P23458] | ||||||||
| ChEMBL | Inhibition of JAK1 domain 2 in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| ChEMBL | Inhibition of JAK1 domain 2 in human HeLa cells lysate pre incubated for 15 mins followed by ADP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| LYN proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase Lyn in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3905] [GtoPdb: 2060] [UniProtKB: P07948] | ||||||||
| ChEMBL | Inhibition of LYN in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| AXL receptor tyrosine kinase/Tyrosine-protein kinase receptor UFO in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4895] [GtoPdb: 1835] [UniProtKB: P30530] | ||||||||
| ChEMBL | Inhibition of AXL in human HeLa cells lysate pre incubated for 15 mins followed by ADP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
| WEE1 G2 checkpoint kinase/Wee1-like protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5491] [GtoPdb: 2278] [UniProtKB: P30291] | ||||||||
| ChEMBL | Inhibition of Wee1 in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC-MS/MS analysis | B | 4.3 | pIC50 | >50000 | nM | IC50 | Cancer Cell (2010) 18: 258-267 [PMID:20832753] |
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]