infigratinib [Ligand Id: 7877] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1852688 (Bgj-398, BGJ-398, BGJ398, Infigratinib, MVP-BGJ398, NVP-BGJ398) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| ALK receptor tyrosine kinase/ALK tyrosine kinase receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4247] [GtoPdb: 1839] [UniProtKB: Q9UM73] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (Enzymatic assay, microfluidic mobility shift readout, Caliper lifesciences, conc. ATP = Km for each kinase)) EUB0000678a ALK | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Selectivity interaction (Kinase panel (cellular selectivity, Bright-Glo proliferation assay in BaF3 Cell line, Promega)) EUB0000678a ALK | B | 5.51 | pIC50 | 3078 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| calcium/calmodulin-dependent protein kinase II alpha subunit/CaM kinase II alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4147] [GtoPdb: 1555] [UniProtKB: Q9UQM7] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (Enzymatic assay, microfluidic mobility shift readout, Caliper lifesciences, conc. ATP = Km for each kinase)) EUB0000678a CAMK2A | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| protein kinase, cAMP-dependent, catalytic, alpha subunit/cAMP-dependent protein kinase alpha-catalytic subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4101] [GtoPdb: 1476] [UniProtKB: P17612] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (Enzymatic assay, microfluidic mobility shift readout, Caliper lifesciences, conc. ATP = Km for each kinase)) EUB0000678a PRKACA | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| casein kinase 1 gamma 3/Casein kinase I isoform gamma-3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5084] [GtoPdb: 2001] [UniProtKB: Q9Y6M4] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (Enzymatic assay, microfluidic mobility shift readout, Caliper lifesciences, conc. ATP = Km for each kinase)) EUB0000678a CSNK1G3 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| mitogen-activated protein kinase 9/c-Jun N-terminal kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4179] [GtoPdb: 1497] [UniProtKB: P45984] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (Enzymatic assay, microfluidic mobility shift readout, Caliper lifesciences, conc. ATP = Km for each kinase)) EUB0000678a MAPK9 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| mitogen-activated protein kinase 10/c-Jun N-terminal kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2637] [GtoPdb: 1498] [UniProtKB: P53779] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (Enzymatic assay, microfluidic mobility shift readout, Caliper lifesciences, conc. ATP = Km for each kinase)) EUB0000678a MAPK10 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| cyclin dependent kinase 1/Cyclin-dependent kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL308] [GtoPdb: 1961] [UniProtKB: P06493] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (Enzymatic assay, microfluidic mobility shift readout, Caliper lifesciences, conc. ATP = Km for each kinase)) EUB0000678a CDK1 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| cyclin dependent kinase 2/Cyclin-dependent kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL301] [GtoPdb: 1973] [UniProtKB: P24941] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (Enzymatic assay, microfluidic mobility shift readout, Caliper lifesciences, conc. ATP = Km for each kinase)) EUB0000678a CDK2 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| cyclin dependent kinase 4/Cyclin-dependent kinase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL331] [GtoPdb: 1976] [UniProtKB: P11802] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (Enzymatic assay, microfluidic mobility shift readout, Caliper lifesciences, conc. ATP = Km for each kinase)) EUB0000678a CDK4 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| EPH receptor A4/Ephrin type-A receptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3988] [GtoPdb: 1824] [UniProtKB: P54764] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (Enzymatic assay, microfluidic mobility shift readout, Caliper lifesciences, conc. ATP = Km for each kinase)) EUB0000678a EPHA4 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| EPH receptor B1/Ephrin type-B receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5072] [GtoPdb: 1830] [UniProtKB: P54762] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (cellular selectivity, Bright-Glo proliferation assay in BaF3 Cell line, Promega)) EUB0000678a EPHB1 | B | 5.52 | pIC50 | 3039 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| EPH receptor B4/Ephrin type-B receptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5147] [GtoPdb: 1833] [UniProtKB: P54760] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (Enzymatic assay, microfluidic mobility shift readout, Caliper lifesciences, conc. ATP = Km for each kinase)) EUB0000678a EPHB4 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (Enzymatic assay, microfluidic mobility shift readout, Caliper lifesciences, conc. ATP = Km for each kinase)) EUB0000678a EGFR | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| fibroblast growth factor receptor 1/Fibroblast growth factor receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3650] [GtoPdb: 1808] [UniProtKB: P11362] | ||||||||
| ChEMBL | Affinity Phenotypic Cellular interaction: (Proliferation assay (using J82 cancer cells)) EUB0000678a FGFR1 | F | 5.52 | pIC50 | >3000 | nM | IC50 | Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Affinity Phenotypic Cellular interaction: (Proliferation assay (using UMUC3 cancer cells)) EUB0000678a FGFR1 | F | 5.52 | pIC50 | >3000 | nM | IC50 | Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Affinity Phenotypic Cellular interaction: (Proliferation assay (using VMCUB1 cancer cells)) EUB0000678a FGFR1 | F | 5.52 | pIC50 | >3000 | nM | IC50 | Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Selectivity interaction (Kinase panel (cellular selectivity, Bright-Glo proliferation assay in BaF3 Cell line, Promega)) EUB0000678a FGFR1 | B | 5.73 | pIC50 | 1857 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Affinity Phenotypic Cellular interaction: (Proliferation assay (using HT1197 cancer cells)) EUB0000678a FGFR1 | F | 5.94 | pIC50 | 1157 | nM | IC50 | Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Inhibition of FGFR1 V561M mutant (unknown origin) by radiometric kinase activity assay | B | 6.12 | pIC50 | 759.2 | nM | IC50 | J Med Chem (2022) 65: 6017-6038 [PMID:35436119] |
| ChEMBL | Affinity Phenotypic Cellular interaction: (Proliferation assay (using SW780 cancer cells)) EUB0000678a FGFR1 | F | 7.49 | pIC50 | 32 | nM | IC50 | Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Affinity Phenotypic Cellular interaction: (Proliferation assay (using RT4 cancer cells)) EUB0000678a FGFR1 | F | 7.52 | pIC50 | 30 | nM | IC50 | Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Affinity Phenotypic Cellular interaction: (Proliferation assay (using JMSU1 cancer cells)) EUB0000678a FGFR1 | F | 7.82 | pIC50 | 15 | nM | IC50 | Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Affinity Phenotypic Cellular interaction: (Bladder Cancer Cell lines Proliferation Assay in RT112 cells) EUB0000678a FGFR1 | F | 8.3 | pIC50 | 5 | nM | IC50 | Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Selectivity interaction (Cell Capture ELISA Assay (in HEK293 cells)) EUB0000678a FGFR1 | B | 8.34 | pIC50 | 4.6 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Selectivity interaction (Kinase panel (cellular selectivity, Bright-Glo proliferation assay in BaF3 Cell line, Promega)) EUB0000678a FGFR1 | B | 8.54 | pIC50 | 2.9 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Affinity On-target Cellular interaction: (Luciferase bioluminescent assay (Bright-Glo, Promega, proliferation assay in BaF3 Cell line)) EUB0000678a FGFR1 | B | 8.54 | pIC50 | 2.9 | nM | IC50 | Affinity On-target Cellular Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Inhibition of recombinant human FGFR1 using biotin-EQEDEPEGDYFEWLE-amide as substrate preincubated for 5 to 10 mins followed by substrate addition and measured after 1 hr by HTRF assay | B | 8.68 | pIC50 | 2.1 | nM | IC50 | J Med Chem (2022) 65: 15433-15442 [PMID:36356320] |
| ChEMBL | Inhibition of recombinant FGFR1 (unknown origin) using peptidic substrates in presence of ATP by Kinase-Glo luminescent kinase assay | B | 9 | pIC50 | 1 | nM | IC50 | Eur J Med Chem (2017) 126: 476-490 [PMID:27914362] |
| ChEMBL | Biochemical Kinase Assay : Recombinant FGFR1 (2.5 nM), or FGFR4 (12 nM) was prepared as a mixture with substrate KKKSPGEYVNIEFG (SEQ ID NO:1) (20 ÎĽM, FGFR1 substrate); Poly [E,Y]4:1 (0.2 mg/ml, FGFR2,3,4 substrate)] in kinase reaction buffer (20 mM HEPES-HCl, pH 7.5, 10 mM MgCl2, 2 mM MnCl2, 1 mM EGTA, 0.02% Brij35, 0.1 mM Na3VO4, 0.02 mg/ml BSA, 2 mM DTT, and 1% DMSO). Compound was added to the enzyme/substrate mixture using acoustic technology and pre-incubated for 0, 15, or 60 minutes at room temperature. After compound pre-incubation, 33P-Îł-ATP was added at a final concentration of 10 ÎĽM to initiate kinase reactions. Reactions were incubated for 120 minutes at room temperature. | B | 9 | pIC50 | 1 | nM | IC50 | US-9434697-B2. Pyrimidine FGFR4 inhibitors (2016) |
| ChEMBL | Affinity Biochemical interaction: (Microfluidic mobility shift readout (Caliper lifesciences, conc. ATP = Km)) EUB0000678a FGFR1 | B | 9.05 | pIC50 | 0.9 | nM | IC50 | Affinity Biochemical Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Inhibition of FGFR1 (unknown origin) | B | 9.05 | pIC50 | 0.9 | nM | IC50 | Eur J Med Chem (2021) 220: 113499-113499 [PMID:33940465] |
| ChEMBL | Selectivity interaction (Kinase panel (Enzymatic assay, microfluidic mobility shift readout, Caliper lifesciences, conc. ATP = Km for each kinase)) EUB0000678a FGFR1 | B | 9.05 | pIC50 | 0.9 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| GtoPdb | - | - | 9.05 | pIC50 | 0.9 | nM | IC50 | J Med Chem (2011) 54: 7066-83 [PMID:21936542] |
| ChEMBL | Selectivity interaction (Kinase panel (cellular selectivity, Bright-Glo proliferation assay in BaF3 Cell line, Promega)) EUB0000678a FGFR1 | B | 9.15 | pIC50 | 0.7 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Inhibition of N-terminal GST-tagged human FGFR1 cytoplasmic domain (398-822 AA) expressed in baculovirus using FAM-labelled peptide as substrate pre-incubated for 10 mins followed by substrate addition by mobility shift assay | B | 9.23 | pIC50 | 0.59 | nM | IC50 | Eur J Med Chem (2020) 187: 111943-111943 [PMID:31846829] |
| ChEMBL | Inhibition of wild-type FGFR1 (unknown origin) by radiometric kinase activity assay | B | 9.3 | pIC50 | <0.5 | nM | IC50 | J Med Chem (2022) 65: 6017-6038 [PMID:35436119] |
| fibroblast growth factor receptor 2/Fibroblast growth factor receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4142] [GtoPdb: 1809] [UniProtKB: P21802] | ||||||||
| ChEMBL | Affinity Phenotypic Cellular interaction: (Proliferation assay (using VMCUB1 cancer cells)) EUB0000678a FGFR2 | F | 5.52 | pIC50 | >3000 | nM | IC50 | Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Affinity Phenotypic Cellular interaction: (Proliferation assay (using J82 cancer cells)) EUB0000678a FGFR2 | F | 5.52 | pIC50 | >3000 | nM | IC50 | Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Affinity Phenotypic Cellular interaction: (Proliferation assay (using UMUC3 cancer cells)) EUB0000678a FGFR2 | F | 5.52 | pIC50 | >3000 | nM | IC50 | Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Selectivity interaction (Kinase panel (cellular selectivity, Bright-Glo proliferation assay in BaF3 Cell line, Promega)) EUB0000678a FGFR2 | B | 5.73 | pIC50 | 1857 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Affinity Phenotypic Cellular interaction: (Proliferation assay (using HT1197 cancer cells)) EUB0000678a FGFR2 | F | 5.94 | pIC50 | 1157 | nM | IC50 | Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Affinity Phenotypic Cellular interaction: (Proliferation assay (using SW780 cancer cells)) EUB0000678a FGFR2 | F | 7.49 | pIC50 | 32 | nM | IC50 | Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Affinity Phenotypic Cellular interaction: (Proliferation assay (using RT4 cancer cells)) EUB0000678a FGFR2 | F | 7.52 | pIC50 | 30 | nM | IC50 | Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Affinity Phenotypic Cellular interaction: (Proliferation assay (using JMSU1 cancer cells)) EUB0000678a FGFR2 | F | 7.82 | pIC50 | 15 | nM | IC50 | Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Affinity Phenotypic Cellular interaction: (Bladder Cancer Cell lines Proliferation Assay in RT112 cells) EUB0000678a FGFR2 | F | 8.3 | pIC50 | 5 | nM | IC50 | Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Selectivity interaction (Cell Capture ELISA Assay (in HEK293 cells)) EUB0000678a FGFR2 | B | 8.31 | pIC50 | 4.9 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Selectivity interaction (Kinase panel (cellular selectivity, Bright-Glo proliferation assay in BaF3 Cell line, Promega)) EUB0000678a FGFR2 | B | 8.7 | pIC50 | 2 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Affinity On-target Cellular interaction: (Luciferase bioluminescent assay (Bright-Glo, Promega, proliferation assay in BaF3 Cell line)) EUB0000678a FGFR2 | B | 8.7 | pIC50 | 2 | nM | IC50 | Affinity On-target Cellular Literature for EUbOPEN Chemogenomic Library |
| GtoPdb | - | - | 8.85 | pIC50 | 1.4 | nM | IC50 | J Med Chem (2011) 54: 7066-83 [PMID:21936542] |
| ChEMBL | Inhibition of FGFR2 (unknown origin) | B | 8.85 | pIC50 | 1.4 | nM | IC50 | Eur J Med Chem (2021) 220: 113499-113499 [PMID:33940465] |
| ChEMBL | Affinity Biochemical interaction: (Microfluidic mobility shift readout (Caliper lifesciences, conc. ATP = Km)) EUB0000678a FGFR2 | B | 8.85 | pIC50 | 1.4 | nM | IC50 | Affinity Biochemical Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Selectivity interaction (Kinase panel (Enzymatic assay, microfluidic mobility shift readout, Caliper lifesciences, conc. ATP = Km for each kinase)) EUB0000678a FGFR2 | B | 8.85 | pIC50 | 1.4 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Inhibition of recombinant FGFR2 (unknown origin) using peptidic substrates in presence of ATP by Kinase-Glo luminescent kinase assay | B | 9 | pIC50 | 1 | nM | IC50 | Eur J Med Chem (2017) 126: 476-490 [PMID:27914362] |
| ChEMBL | Inhibition of FGFR2 N549H mutant (unknown origin) by radiometric kinase activity assay | B | 9.17 | pIC50 | 0.68 | nM | IC50 | J Med Chem (2022) 65: 6017-6038 [PMID:35436119] |
| ChEMBL | Inhibition of wild-type FGFR2 (unknown origin) by radiometric kinase activity assay | B | 9.3 | pIC50 | <0.5 | nM | IC50 | J Med Chem (2022) 65: 6017-6038 [PMID:35436119] |
| fibroblast growth factor receptor 3/Fibroblast growth factor receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2742] [GtoPdb: 1810] [UniProtKB: P22607] | ||||||||
| ChEMBL | Affinity Phenotypic Cellular interaction: (Proliferation assay (using J82 cancer cells)) EUB0000678a FGFR3 | F | 5.52 | pIC50 | >3000 | nM | IC50 | Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Affinity Phenotypic Cellular interaction: (Proliferation assay (using VMCUB1 cancer cells)) EUB0000678a FGFR3 | F | 5.52 | pIC50 | >3000 | nM | IC50 | Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Affinity Phenotypic Cellular interaction: (Proliferation assay (using UMUC3 cancer cells)) EUB0000678a FGFR3 | F | 5.52 | pIC50 | >3000 | nM | IC50 | Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Selectivity interaction (Kinase panel (cellular selectivity, Bright-Glo proliferation assay in BaF3 Cell line, Promega)) EUB0000678a FGFR3 | B | 5.73 | pIC50 | 1857 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Affinity Phenotypic Cellular interaction: (Proliferation assay (using HT1197 cancer cells)) EUB0000678a FGFR3 | F | 5.94 | pIC50 | 1157 | nM | IC50 | Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Inhibition of FGFR3 V555M mutant (unknown origin) by radiometric kinase activity assay | B | 6.3 | pIC50 | 505.9 | nM | IC50 | J Med Chem (2022) 65: 6017-6038 [PMID:35436119] |
| ChEMBL | Inhibition of recombinant human FGFR3 V555M mutant using biotin-EQEDEPEGDYFEWLE-amide as substrate preincubated for 5 to 10 mins followed by substrate addition and measured after 1 hr by HTRF assay | B | 6.45 | pIC50 | 352 | nM | IC50 | J Med Chem (2022) 65: 15433-15442 [PMID:36356320] |
| ChEMBL | Selectivity interaction (Kinase panel (cellular selectivity, Bright-Glo proliferation assay in BaF3 Cell line, Promega)) EUB0000678a FGFR3 | B | 7.28 | pIC50 | 52.2 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Inhibition of FGFR3 K650M mutant (unknown origin) by radiometric kinase activity assay | B | 7.35 | pIC50 | 44.4 | nM | IC50 | J Med Chem (2022) 65: 6017-6038 [PMID:35436119] |
| ChEMBL | Affinity Phenotypic Cellular interaction: (Proliferation assay (using SW780 cancer cells)) EUB0000678a FGFR3 | F | 7.49 | pIC50 | 32 | nM | IC50 | Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Affinity Phenotypic Cellular interaction: (Proliferation assay (using RT4 cancer cells)) EUB0000678a FGFR3 | F | 7.52 | pIC50 | 30 | nM | IC50 | Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Affinity Phenotypic Cellular interaction: (Proliferation assay (using JMSU1 cancer cells)) EUB0000678a FGFR3 | F | 7.82 | pIC50 | 15 | nM | IC50 | Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Selectivity interaction (Cell Capture ELISA Assay (in HEK293 cells)) EUB0000678a FGFR3 | B | 8.3 | pIC50 | 5 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Affinity Phenotypic Cellular interaction: (Bladder Cancer Cell lines Proliferation Assay in RT112 cells) EUB0000678a FGFR3 | F | 8.3 | pIC50 | 5 | nM | IC50 | Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Selectivity interaction (Cell Capture ELISA Assay (in HEK293 cells)) EUB0000678a FGFR3 | B | 8.3 | pIC50 | 5 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Selectivity interaction (Kinase panel (Enzymatic assay, microfluidic mobility shift readout, Caliper lifesciences, conc. ATP = Km for each kinase)) EUB0000678a FGFR3 | B | 8.31 | pIC50 | 4.9 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Inhibition of N-terminal His-Avi tagged recombinant human FGFR3 (447 to 761 residues) expressed in an Sf9 infected baculovirus expression system using biotin-EQEDEPEGDYFEWLE-amide as substrate preincubated for 5 to 10 mins followed by substrate addition and measured after 1 hr by HTRF assay | B | 8.57 | pIC50 | 2.7 | nM | IC50 | J Med Chem (2022) 65: 15433-15442 [PMID:36356320] |
| ChEMBL | Selectivity interaction (Kinase panel (cellular selectivity, Bright-Glo proliferation assay in BaF3 Cell line, Promega)) EUB0000678a FGFR3 | B | 8.7 | pIC50 | 2 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| GtoPdb | - | - | 9 | pIC50 | 1 | nM | IC50 | J Med Chem (2011) 54: 7066-83 [PMID:21936542] |
| ChEMBL | Inhibition of FGFR3 (unknown origin) | B | 9 | pIC50 | 1 | nM | IC50 | Eur J Med Chem (2021) 220: 113499-113499 [PMID:33940465] |
| ChEMBL | Affinity Biochemical interaction: (Microfluidic mobility shift readout (Caliper lifesciences, conc. ATP = Km)) EUB0000678a FGFR3 | B | 9 | pIC50 | 1 | nM | IC50 | Affinity Biochemical Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Selectivity interaction (Kinase panel (Enzymatic assay, microfluidic mobility shift readout, Caliper lifesciences, conc. ATP = Km for each kinase)) EUB0000678a FGFR3 | B | 9 | pIC50 | 1 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Inhibition of recombinant GST fused FGFR3 (unknown origin) using poly(EY) 4:1 as substrate in presence of [gamma-32P]ATP after 10 mins by scintillation counting method | B | 9 | pIC50 | 1 | nM | IC50 | Eur J Med Chem (2017) 126: 476-490 [PMID:27914362] |
| ChEMBL | Affinity On-target Cellular interaction: (Luciferase bioluminescent assay (Bright-Glo, Promega, proliferation assay in BaF3 Cell line)) EUB0000678a FGFR3 | B | 9.15 | pIC50 | 0.7 | nM | IC50 | Affinity On-target Cellular Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Inhibition of wild-type FGFR3 (unknown origin) by radiometric kinase activity assay | B | 9.18 | pIC50 | 0.66 | nM | IC50 | J Med Chem (2022) 65: 6017-6038 [PMID:35436119] |
| ChEMBL | Inhibition of FGFR3 K650E mutant (unknown origin) by radiometric kinase activity assay | B | 9.3 | pIC50 | <0.5 | nM | IC50 | J Med Chem (2022) 65: 6017-6038 [PMID:35436119] |
| fibroblast growth factor receptor 4/Fibroblast growth factor receptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3973] [GtoPdb: 1811] [UniProtKB: P22455] | ||||||||
| ChEMBL | Selectivity interaction (Cell Capture ELISA Assay (in HEK293 cells)) EUB0000678a FGFR4 | B | 6.77 | pIC50 | 168 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Inhibition of recombinant human FGFR4 (460 to 802 residues) using biotin-EQEDEPEGDYFEWLE-amide as substrate preincubated for 5 to 10 mins followed by substrate addition and measured after 1 hr by HTRF assay | B | 6.94 | pIC50 | 115 | nM | IC50 | J Med Chem (2022) 65: 15433-15442 [PMID:36356320] |
| ChEMBL | Inhibition of recombinant non-phosphorylated FGFR4 kinase domain (442 to 753) (unknown origin) expressed in Sf9 insect cells using 5-Fluo-Ahx-KKKKEEIYFFFG-NH2 peptide as substrate in presence of ATP measured after 60 mins by caliper microfluidic mobility shift assay | B | 7.15 | pIC50 | 71 | nM | IC50 | J Med Chem (2020) 63: 12542-12573 [PMID:32930584] |
| ChEMBL | Inhibition of phosphorylated FGFR4 (388 to 802 residues) (unknown origin) using 5-Fluo-Ahx-KKKKEEIYFFFG-NH2 as substrate after 60 mins by microfluidic mobility shift assay | B | 7.15 | pIC50 | 71 | nM | IC50 | Medchemcomm (2017) 8: 1604-1613 [PMID:30108871] |
| ChEMBL | Inhibition of non-phosphorylated N-terminal His6-tagged FGFR4 C477A mutant (G442 to E753 residues) (unknown origin) expressed in sf9 cells using 5-Fluo-Ahx-KKKKEEIYFFFG-NH2 as substrate after 60 mins by microfluidic mobility shift assay | B | 7.19 | pIC50 | 64 | nM | IC50 | Medchemcomm (2017) 8: 1604-1613 [PMID:30108871] |
| ChEMBL | Inhibition of wild type non-phosphorylated N-terminal His6-tagged FGFR4 (G442 to E753 residues) (unknown origin) expressed in sf9 cells using 5-Fluo-Ahx-KKKKEEIYFFFG-NH2 as substrate after 60 mins by microfluidic mobility shift assay | B | 7.21 | pIC50 | 62 | nM | IC50 | Medchemcomm (2017) 8: 1604-1613 [PMID:30108871] |
| GtoPdb | - | - | 7.22 | pIC50 | 60 | nM | IC50 | J Med Chem (2011) 54: 7066-83 [PMID:21936542] |
| ChEMBL | Inhibition of FGFR4 (unknown origin) | B | 7.22 | pIC50 | 60 | nM | IC50 | Eur J Med Chem (2021) 220: 113499-113499 [PMID:33940465] |
| ChEMBL | Inhibition of recombinant FGFR4 (unknown origin) using peptidic substrates in presence of ATP by Kinase-Glo luminescent kinase assay | B | 7.22 | pIC50 | 60 | nM | IC50 | Eur J Med Chem (2017) 126: 476-490 [PMID:27914362] |
| ChEMBL | Inhibition of wild-type FGFR4 (unknown origin) by radiometric kinase activity assay | B | 7.22 | pIC50 | 60 | nM | IC50 | J Med Chem (2022) 65: 6017-6038 [PMID:35436119] |
| ChEMBL | Selectivity interaction (Kinase panel (Enzymatic assay, microfluidic mobility shift readout, Caliper lifesciences, conc. ATP = Km for each kinase)) EUB0000678a FGFR4 | B | 7.22 | pIC50 | 60 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Biochemical Kinase Assay : Recombinant FGFR1 (2.5 nM), or FGFR4 (12 nM) was prepared as a mixture with substrate KKKSPGEYVNIEFG (SEQ ID NO:1) (20 ÎĽM, FGFR1 substrate); Poly [E,Y]4:1 (0.2 mg/ml, FGFR2,3,4 substrate)] in kinase reaction buffer (20 mM HEPES-HCl, pH 7.5, 10 mM MgCl2, 2 mM MnCl2, 1 mM EGTA, 0.02% Brij35, 0.1 mM Na3VO4, 0.02 mg/ml BSA, 2 mM DTT, and 1% DMSO). Compound was added to the enzyme/substrate mixture using acoustic technology and pre-incubated for 0, 15, or 60 minutes at room temperature. After compound pre-incubation, 33P-Îł-ATP was added at a final concentration of 10 ÎĽM to initiate kinase reactions. Reactions were incubated for 120 minutes at room temperature. | B | 7.89 | pIC50 | 13 | nM | IC50 | US-9434697-B2. Pyrimidine FGFR4 inhibitors (2016) |
| ChEMBL | Inhibition of non-phosphorylated N-terminal His6-tagged FGFR4 C552A mutant (G442 to E753 residues) (unknown origin) expressed in sf9 cells using 5-Fluo-Ahx-KKKKEEIYFFFG-NH2 as substrate after 60 mins by microfluidic mobility shift assay | B | 9.09 | pIC50 | 0.82 | nM | IC50 | Medchemcomm (2017) 8: 1604-1613 [PMID:30108871] |
| fibroblast growth factor receptor 4/Fibroblast growth factor receptor 4 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3839] [GtoPdb: 1811] [UniProtKB: Q03142] | ||||||||
| ChEMBL | Inhibition of FGFR4 in mouse BAF3 cells assessed as reduction in cell viability incubated for 2 days by cell proliferation assay | B | 6.24 | pIC50 | 581 | nM | IC50 | J Med Chem (2020) 63: 12542-12573 [PMID:32930584] |
| ChEMBL | Inhibition of FGFR4 in mouse BAF3 cells assessed as decrease in FGFR4 phosphorylation incubated for 40 mins | B | 6.27 | pIC50 | 541 | nM | IC50 | J Med Chem (2020) 63: 12542-12573 [PMID:32930584] |
| 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 (Enzymatic assay, microfluidic mobility shift readout, Caliper lifesciences, conc. ATP = Km for each kinase)) EUB0000678a PTK2 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| glycogen synthase kinase 3 beta/Glycogen synthase kinase-3 beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL262] [GtoPdb: 2030] [UniProtKB: P49841] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (Enzymatic assay, microfluidic mobility shift readout, Caliper lifesciences, conc. ATP = Km for each kinase)) EUB0000678a GSK3B | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| MET proto-oncogene, receptor tyrosine kinase/Hepatocyte growth factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3717] [GtoPdb: 1815] [UniProtKB: P08581] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (Enzymatic assay, microfluidic mobility shift readout, Caliper lifesciences, conc. ATP = Km for each kinase)) EUB0000678a MET | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Selectivity interaction (Kinase panel (cellular selectivity, Bright-Glo proliferation assay in BaF3 Cell line, Promega)) EUB0000678a MET | B | 5.52 | pIC50 | 3011 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| Insulin-like growth factor I receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1957] [GtoPdb: 1801] [UniProtKB: P08069] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (Enzymatic assay, microfluidic mobility shift readout, Caliper lifesciences, conc. ATP = Km for each kinase)) EUB0000678a IGF1R | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| Insulin receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1981] [GtoPdb: 1800] [UniProtKB: P06213] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (Enzymatic assay, microfluidic mobility shift readout, Caliper lifesciences, conc. ATP = Km for each kinase)) EUB0000678a INSR | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Selectivity interaction (Kinase panel (cellular selectivity, Bright-Glo proliferation assay in BaF3 Cell line, Promega)) EUB0000678a INSR | B | 5.47 | pIC50 | 3371 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| 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 | Selectivity interaction (Kinase panel (Enzymatic assay, microfluidic mobility shift readout, Caliper lifesciences, conc. ATP = Km for each kinase)) EUB0000678a IRAK4 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| macrophage stimulating 1 receptor/Macrophage-stimulating protein receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2689] [GtoPdb: 1816] [UniProtKB: Q04912] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (Enzymatic assay, microfluidic mobility shift readout, Caliper lifesciences, conc. ATP = Km for each kinase)) EUB0000678a MST1R | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Selectivity interaction (Kinase panel (cellular selectivity, Bright-Glo proliferation assay in BaF3 Cell line, Promega)) EUB0000678a MST1R | B | 5.54 | pIC50 | 2891 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| MAPK activated protein kinase 5/MAP kinase-activated protein kinase 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3094] [GtoPdb: 2096] [UniProtKB: Q8IW41] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (Enzymatic assay, microfluidic mobility shift readout, Caliper lifesciences, conc. ATP = Km for each kinase)) EUB0000678a MAPKAPK5 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| mitogen-activated protein kinase 1/MAP kinase ERK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4040] [GtoPdb: 1495] [UniProtKB: P28482] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (Enzymatic assay, microfluidic mobility shift readout, Caliper lifesciences, conc. ATP = Km for each kinase)) EUB0000678a MAPK1 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| MAPK interacting serine/threonine kinase 1/MAP kinase-interacting serine/threonine-protein kinase MNK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4718] [GtoPdb: 2104] [UniProtKB: Q9BUB5] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (Enzymatic assay, microfluidic mobility shift readout, Caliper lifesciences, conc. ATP = Km for each kinase)) EUB0000678a MKNK1 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| mitogen-activated protein kinase 14/MAP kinase p38 alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL260] [GtoPdb: 1499] [UniProtKB: Q16539] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (Enzymatic assay, microfluidic mobility shift readout, Caliper lifesciences, conc. ATP = Km for each kinase)) EUB0000678a MAPK14 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| mitogen-activated protein kinase 12/MAP kinase p38 gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4674] [GtoPdb: 1501] [UniProtKB: P53778] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (Enzymatic assay, microfluidic mobility shift readout, Caliper lifesciences, conc. ATP = Km for each kinase)) EUB0000678a MAPK12 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| MAPK interacting serine/threonine kinase 2/MAP kinase signal-integrating kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4204] [GtoPdb: 2105] [UniProtKB: Q9HBH9] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (Enzymatic assay, microfluidic mobility shift readout, Caliper lifesciences, conc. ATP = Km for each kinase)) EUB0000678a MKNK2 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| 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 | Selectivity interaction (Kinase panel (Enzymatic assay, microfluidic mobility shift readout, Caliper lifesciences, conc. ATP = Km for each kinase)) EUB0000678a MAP3K8 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| neurotrophic receptor tyrosine kinase 2/Neurotrophic tyrosine kinase receptor type 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4898] [GtoPdb: 1818] [UniProtKB: Q16620] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (cellular selectivity, Bright-Glo proliferation assay in BaF3 Cell line, Promega)) EUB0000678a NTRK2 | B | 5.5 | pIC50 | 3139 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| 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 | Selectivity interaction (Kinase panel (KinaseGlo Luminescent Kinase Assay, Promega)) EUB0000678a PIK3C3 | B | 5.05 | pIC50 | >9000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha/PI3-kinase p110-alpha subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4005] [GtoPdb: 2153] [UniProtKB: P42336] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (KinaseGlo Luminescent Kinase Assay, Promega)) EUB0000678a PIK3CA | B | 5.05 | pIC50 | >9000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit beta/PI3-kinase p110-beta subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3145] [GtoPdb: 2154] [UniProtKB: P42338] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (KinaseGlo Luminescent Kinase Assay, Promega)) EUB0000678a PIK3CB | B | 5.05 | pIC50 | >9000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit delta/PI3-kinase p110-delta subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3130] [GtoPdb: 2155] [UniProtKB: O00329] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (KinaseGlo Luminescent Kinase Assay, Promega)) EUB0000678a PIK3CD | B | 5.05 | pIC50 | >9000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| phosphatidylinositol 4-kinase beta/PI4-kinase beta subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3268] [GtoPdb: 2149] [UniProtKB: Q9UBF8] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (KinaseGlo Luminescent Kinase Assay, Promega)) EUB0000678a PI4KB | B | 5.05 | pIC50 | >9000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| 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 | Selectivity interaction (Kinase panel (Enzymatic assay, microfluidic mobility shift readout, Caliper lifesciences, conc. ATP = Km for each kinase)) EUB0000678a PDGFRA | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Selectivity interaction (Kinase panel (cellular selectivity, Bright-Glo proliferation assay in BaF3 Cell line, Promega)) EUB0000678a PDGFRA | B | 5.57 | pIC50 | 2718 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| protein kinase C alpha/Protein kinase C alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL299] [GtoPdb: 1482] [UniProtKB: P17252] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (Enzymatic assay, microfluidic mobility shift readout, Caliper lifesciences, conc. ATP = Km for each kinase)) EUB0000678a PRKCA | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| protein kinase C theta/Protein kinase C theta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3920] [GtoPdb: 1488] [UniProtKB: Q04759] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (Enzymatic assay, microfluidic mobility shift readout, Caliper lifesciences, conc. ATP = Km for each kinase)) EUB0000678a PRKCQ | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| protein kinase N1/Protein kinase N1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3384] [GtoPdb: 1520] [UniProtKB: Q16512] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (Enzymatic assay, microfluidic mobility shift readout, Caliper lifesciences, conc. ATP = Km for each kinase)) EUB0000678a PKN1 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| protein kinase N2/Protein kinase N2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3032] [GtoPdb: 1521] [UniProtKB: Q16513] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (Enzymatic assay, microfluidic mobility shift readout, Caliper lifesciences, conc. ATP = Km for each kinase)) EUB0000678a PKN2 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| MER proto-oncogene, tyrosine kinase/Proto-oncogene tyrosine-protein kinase MER in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5331] [GtoPdb: 1837] [UniProtKB: Q12866] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (Enzymatic assay, microfluidic mobility shift readout, Caliper lifesciences, conc. ATP = Km for each kinase)) EUB0000678a MERTK | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| 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 | Selectivity interaction (Kinase panel (cellular selectivity, Bright-Glo proliferation assay in BaF3 Cell line, Promega)) EUB0000678a ROS1 | B | 5.49 | pIC50 | 3263 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| pyruvate dehydrogenase kinase 1/Pyruvate dehydrogenase kinase isoform 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4766] [GtoPdb: 2915] [UniProtKB: Q15118] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (Enzymatic assay, microfluidic mobility shift readout, Caliper lifesciences, conc. ATP = Km for each kinase)) EUB0000678a PDK1 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| erb-b2 receptor tyrosine kinase 2/Receptor protein-tyrosine kinase erbB-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1824] [GtoPdb: 2019] [UniProtKB: P04626] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (Enzymatic assay, microfluidic mobility shift readout, Caliper lifesciences, conc. ATP = Km for each kinase)) EUB0000678a ERBB2 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| erb-b2 receptor tyrosine kinase 4/Receptor protein-tyrosine kinase erbB-4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3009] [GtoPdb: 1799] [UniProtKB: Q15303] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (Enzymatic assay, microfluidic mobility shift readout, Caliper lifesciences, conc. ATP = Km for each kinase)) EUB0000678a ERBB4 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| 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 | Selectivity interaction (Kinase panel (Enzymatic assay, microfluidic mobility shift readout, Caliper lifesciences, conc. ATP = Km for each kinase)) EUB0000678a ROCK2 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| ribosomal protein S6 kinase A1/Ribosomal protein S6 kinase alpha 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2553] [GtoPdb: 1527] [UniProtKB: Q15418] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (Enzymatic assay, microfluidic mobility shift readout, Caliper lifesciences, conc. ATP = Km for each kinase)) EUB0000678a RPS6KA1 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| AKT serine/threonine kinase 1/Serine/threonine-protein kinase AKT in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4282] [GtoPdb: 1479] [UniProtKB: P31749] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (Enzymatic assay, microfluidic mobility shift readout, Caliper lifesciences, conc. ATP = Km for each kinase)) EUB0000678a AKT1 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| aurora kinase A/Serine/threonine-protein kinase Aurora-A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4722] [GtoPdb: 1936] [UniProtKB: O14965] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (Enzymatic assay, microfluidic mobility shift readout, Caliper lifesciences, conc. ATP = Km for each kinase)) EUB0000678a STK6 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| 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 | Selectivity interaction (Kinase panel (cellular selectivity, Bright-Glo proliferation assay in BaF3 Cell line, Promega)) EUB0000678a BRAF | B | 5.38 | pIC50 | 4142 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| mechanistic target of rapamycin kinase/Serine/threonine-protein kinase mTOR in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2842] [GtoPdb: 2109] [UniProtKB: P42345] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (KinaseGlo Luminescent Kinase Assay, Promega)) EUB0000678a MTOR | B | 5.05 | pIC50 | >9000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| p21 (RAC1) activated kinase 2/Serine/threonine-protein kinase PAK 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4487] [GtoPdb: 2134] [UniProtKB: Q13177] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (Enzymatic assay, microfluidic mobility shift readout, Caliper lifesciences, conc. ATP = Km for each kinase)) EUB0000678a PAK2 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| Pim-2 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase PIM2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523] [GtoPdb: 2159] [UniProtKB: Q9P1W9] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (Enzymatic assay, microfluidic mobility shift readout, Caliper lifesciences, conc. ATP = Km for each kinase)) EUB0000678a PIM2 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| polo like kinase 1/Serine/threonine-protein kinase PLK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3024] [GtoPdb: 2168] [UniProtKB: P53350] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (Enzymatic assay, microfluidic mobility shift readout, Caliper lifesciences, conc. ATP = Km for each kinase)) EUB0000678a PLK1 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| WNK lysine deficient protein kinase 1/Serine/threonine-protein kinase WNK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075173] [GtoPdb: 2280] [UniProtKB: Q9H4A3] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (Enzymatic assay, microfluidic mobility shift readout, Caliper lifesciences, conc. ATP = Km for each kinase)) EUB0000678a WNK1 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| SMO/Smoothened homolog in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5971] [GtoPdb: 239] [UniProtKB: Q99835] | ||||||||
| ChEMBL | Displacement of [3H]-cyclopamine from SMO V404M mutant in gefitinib resistant human HCC827 cells by scintillation counting | B | 7.33 | pKi | 46.5 | nM | Ki | J Med Chem (2017) 60: 7447-7458 [PMID:28787156] |
| KIT proto-oncogene, receptor tyrosine kinase/Stem cell growth factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1936] [GtoPdb: 1805] [UniProtKB: P10721] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (cellular selectivity, Bright-Glo proliferation assay in BaF3 Cell line, Promega)) EUB0000678a KIT | B | 5.6 | pIC50 | 2501 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Selectivity interaction (Kinase panel (Enzymatic assay, microfluidic mobility shift readout, Caliper lifesciences, conc. ATP = Km for each kinase)) EUB0000678a KIT | B | 6.12 | pIC50 | 750 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| ABL proto-oncogene 1, non-receptor tyrosine kinase/Tyrosine-protein kinase ABL in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1862] [GtoPdb: 1923] [UniProtKB: P00519] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (Enzymatic assay, microfluidic mobility shift readout, Caliper lifesciences, conc. ATP = Km for each kinase)) EUB0000678a ABL1 | B | 5.64 | pIC50 | 2300 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| BMX non-receptor tyrosine kinase/Tyrosine-protein kinase BMX in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3834] [GtoPdb: 1942] [UniProtKB: P51813] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (cellular selectivity, Bright-Glo proliferation assay in BaF3 Cell line, Promega)) EUB0000678a BMX | B | 5.47 | pIC50 | 3405 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| Bruton tyrosine kinase/Tyrosine-protein kinase BTK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5251] [GtoPdb: 1948] [UniProtKB: Q06187] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (Enzymatic assay, microfluidic mobility shift readout, Caliper lifesciences, conc. ATP = Km for each kinase)) EUB0000678a BTK | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| C-terminal Src kinase/Tyrosine-protein kinase CSK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2634] [GtoPdb: 1994] [UniProtKB: P41240] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (Enzymatic assay, microfluidic mobility shift readout, Caliper lifesciences, conc. ATP = Km for each kinase)) EUB0000678a CSK | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| FYN proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase FYN in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1841] [GtoPdb: 2026] [UniProtKB: P06241] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (Enzymatic assay, microfluidic mobility shift readout, Caliper lifesciences, conc. ATP = Km for each kinase)) EUB0000678a FYN | B | 5.72 | pIC50 | 1900 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| HCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase HCK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3234] [GtoPdb: 2032] [UniProtKB: P08631] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (Enzymatic assay, microfluidic mobility shift readout, Caliper lifesciences, conc. ATP = Km for each kinase)) EUB0000678a HCK | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| Janus kinase 1/Tyrosine-protein kinase JAK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2835] [GtoPdb: 2047] [UniProtKB: P23458] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (Enzymatic assay, microfluidic mobility shift readout, Caliper lifesciences, conc. ATP = Km for each kinase)) EUB0000678a JAK1 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| Janus kinase 2/Tyrosine-protein kinase JAK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2971] [GtoPdb: 2048] [UniProtKB: O60674] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (Enzymatic assay, microfluidic mobility shift readout, Caliper lifesciences, conc. ATP = Km for each kinase)) EUB0000678a JAK2 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Selectivity interaction (Kinase panel (cellular selectivity, Bright-Glo proliferation assay in BaF3 Cell line, Promega)) EUB0000678a JAK2 | B | 5.54 | pIC50 | 2882 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| Janus kinase 3/Tyrosine-protein kinase JAK3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2148] [GtoPdb: 2049] [UniProtKB: P52333] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (Enzymatic assay, microfluidic mobility shift readout, Caliper lifesciences, conc. ATP = Km for each kinase)) EUB0000678a JAK3 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| LCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase LCK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL258] [GtoPdb: 2053] [UniProtKB: P06239] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (Enzymatic assay, microfluidic mobility shift readout, Caliper lifesciences, conc. ATP = Km for each kinase)) EUB0000678a LCK | B | 5.6 | pIC50 | 2500 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Selectivity interaction (Kinase panel (cellular selectivity, Bright-Glo proliferation assay in BaF3 Cell line, Promega)) EUB0000678a LCK | B | 5.61 | pIC50 | 2482 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| LYN proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase Lyn in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3905] [GtoPdb: 2060] [UniProtKB: P07948] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (cellular selectivity, Bright-Glo proliferation assay in BaF3 Cell line, Promega)) EUB0000678a LYN | B | 5.52 | pIC50 | 3019 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Selectivity interaction (Kinase panel (Enzymatic assay, microfluidic mobility shift readout, Caliper lifesciences, conc. ATP = Km for each kinase)) EUB0000678a LYN | B | 6.52 | pIC50 | 300 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| fms related receptor tyrosine kinase 3/Tyrosine-protein kinase receptor FLT3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (Enzymatic assay, microfluidic mobility shift readout, Caliper lifesciences, conc. ATP = Km for each kinase)) EUB0000678a FLT3 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Selectivity interaction (Kinase panel (cellular selectivity, Bright-Glo proliferation assay in BaF3 Cell line, Promega)) EUB0000678a FLT3 | B | 5.49 | pIC50 | 3252 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| ret proto-oncogene/Tyrosine-protein kinase receptor RET in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2041] [GtoPdb: 2185] [UniProtKB: P07949] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (Enzymatic assay, microfluidic mobility shift readout, Caliper lifesciences, conc. ATP = Km for each kinase)) EUB0000678a RET | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Selectivity interaction (Kinase panel (cellular selectivity, Bright-Glo proliferation assay in BaF3 Cell line, Promega)) EUB0000678a RET | B | 5.47 | pIC50 | 3352 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| AXL receptor tyrosine kinase/Tyrosine-protein kinase receptor UFO in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4895] [GtoPdb: 1835] [UniProtKB: P30530] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (Enzymatic assay, microfluidic mobility shift readout, Caliper lifesciences, conc. ATP = Km for each kinase)) EUB0000678a AXL | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| SRC proto-oncogene, non-receptor tyrosine kinase/Tyrosine-protein kinase SRC in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL267] [GtoPdb: 2206] [UniProtKB: P12931] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (Enzymatic assay, microfluidic mobility shift readout, Caliper lifesciences, conc. ATP = Km for each kinase)) EUB0000678a SRC | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Selectivity interaction (Kinase panel (cellular selectivity, Bright-Glo proliferation assay in BaF3 Cell line, Promega)) EUB0000678a SRC | B | 5.53 | pIC50 | 2969 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| spleen associated tyrosine kinase/Tyrosine-protein kinase SYK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2599] [GtoPdb: 2230] [UniProtKB: P43405] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (Enzymatic assay, microfluidic mobility shift readout, Caliper lifesciences, conc. ATP = Km for each kinase)) EUB0000678a SYK | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Selectivity interaction (Kinase panel (cellular selectivity, Bright-Glo proliferation assay in BaF3 Cell line, Promega)) EUB0000678a SYK | B | 5.27 | pIC50 | 5358 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| TEK receptor tyrosine kinase/Tyrosine-protein kinase TIE-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4128] [GtoPdb: 1842] [UniProtKB: Q02763] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (cellular selectivity, Bright-Glo proliferation assay in BaF3 Cell line, Promega)) EUB0000678a TEK | B | 5.69 | pIC50 | 2051 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| tyrosine kinase 2/Tyrosine-protein kinase TYK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3553] [GtoPdb: 2269] [UniProtKB: P29597] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (Enzymatic assay, microfluidic mobility shift readout, Caliper lifesciences, conc. ATP = Km for each kinase)) EUB0000678a TYK2 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Selectivity interaction (Kinase panel (cellular selectivity, Bright-Glo proliferation assay in BaF3 Cell line, Promega)) EUB0000678a TYK2 | B | 5.48 | pIC50 | 3303 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| 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 | Selectivity interaction (Kinase panel (Enzymatic assay, microfluidic mobility shift readout, Caliper lifesciences, conc. ATP = Km for each kinase)) EUB0000678a YES1 | B | 5.96 | pIC50 | 1100 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| 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 | Selectivity interaction (Kinase panel (Enzymatic assay, microfluidic mobility shift readout, Caliper lifesciences, conc. ATP = Km for each kinase)) EUB0000678a ZAP70 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| fms related receptor tyrosine kinase 1/Vascular endothelial growth factor receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1868] [GtoPdb: 1812] [UniProtKB: P17948] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (cellular selectivity, Bright-Glo proliferation assay in BaF3 Cell line, Promega)) EUB0000678a FLT1 | B | 5.82 | pIC50 | 1510 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| kinase insert domain receptor/Vascular endothelial growth factor receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL279] [GtoPdb: 1813] [UniProtKB: P35968] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (cellular selectivity, Bright-Glo proliferation assay in BaF3 Cell line, Promega)) EUB0000678a KDR | B | 5.84 | pIC50 | 1449 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Selectivity interaction (Kinase panel (cellular selectivity, Bright-Glo proliferation assay in BaF3 Cell line, Promega)) EUB0000678a KDR | B | 6.03 | pIC50 | 938 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| GtoPdb | - | - | 6.74 | pIC50 | 180 | nM | IC50 | J Med Chem (2011) 54: 7066-83 [PMID:21936542] |
| ChEMBL | Selectivity interaction (Kinase panel (Enzymatic assay, microfluidic mobility shift readout, Caliper lifesciences, conc. ATP = Km for each kinase)) EUB0000678a KDR | B | 6.74 | pIC50 | 180 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| fms related receptor tyrosine kinase 4/Vascular endothelial growth factor receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1955] [GtoPdb: 1814] [UniProtKB: P35916] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (cellular selectivity, Bright-Glo proliferation assay in BaF3 Cell line, Promega)) EUB0000678a FLT4 | B | 5.68 | pIC50 | 2072 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
ChEMBL data shown on this page come from version 34:
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]
