compound 2 [PMID: 15546730] [Ligand Id: 8136] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL364623
  • cyclin dependent kinase 2/Cyclin-dependent kinase 2 in Human [ChEMBL: CHEMBL301] [GtoPdb: 1973] [UniProtKB: P24941]
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  • cyclin dependent kinase 4/Cyclin-dependent kinase 4 in Human [ChEMBL: CHEMBL331] [GtoPdb: 1976] [UniProtKB: P11802]
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  • epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
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  • fibroblast growth factor receptor 1/Fibroblast growth factor receptor 1 in Human [ChEMBL: CHEMBL3650] [GtoPdb: 1808] [UniProtKB: P11362]
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  • erb-b2 receptor tyrosine kinase 2/Receptor protein-tyrosine kinase erbB-2 in Human [ChEMBL: CHEMBL1824] [GtoPdb: 2019] [UniProtKB: P04626]
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  • FGR proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase FGR in Human [ChEMBL: CHEMBL4454] [GtoPdb: 2024] [UniProtKB: P09769]
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  • FYN proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase FYN in Human [ChEMBL: CHEMBL1841] [GtoPdb: 2026] [UniProtKB: P06241]
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  • HCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase HCK in Human [ChEMBL: CHEMBL3234] [GtoPdb: 2032] [UniProtKB: P08631]
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  • Janus kinase 3/Tyrosine-protein kinase JAK3 in Human [ChEMBL: CHEMBL2148] [GtoPdb: 2049] [UniProtKB: P52333]
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  • LCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase LCK in Human [ChEMBL: CHEMBL258] [GtoPdb: 2053] [UniProtKB: P06239]
  • LCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase LCK in Mouse [ChEMBL: CHEMBL2480] [GtoPdb: 2053] [UniProtKB: P06240]
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  • LYN proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase Lyn in Human [ChEMBL: CHEMBL3905] [GtoPdb: 2060] [UniProtKB: P07948]
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  • SRC proto-oncogene, non-receptor tyrosine kinase/Tyrosine-protein kinase SRC in Human [ChEMBL: CHEMBL267] [GtoPdb: 2206] [UniProtKB: P12931]
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  • YES proto-oncogene 1, Src family tyrosine kinase/Tyrosine-protein kinase YES in Human [ChEMBL: CHEMBL2073] [GtoPdb: 2284] [UniProtKB: P07947]
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  • kinase insert domain receptor/Vascular endothelial growth factor receptor 2 in Human [ChEMBL: CHEMBL279] [GtoPdb: 1813] [UniProtKB: P35968]
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  • BLK proto-oncogene, Src family tyrosine kinase in Human [GtoPdb: 1940] [UniProtKB: P51451]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
cyclin dependent kinase 2/Cyclin-dependent kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL301] [GtoPdb: 1973] [UniProtKB: P24941]
ChEMBL Inhibitory activity against Cyclin-dependent kinase 2 B 4.6 pIC50 >25000 nM IC50 Bioorg. Med. Chem. Lett. (2004) 14: 6061-6066 [PMID:15546730]
ChEMBL Inhibition of Cdk2 B 4.6 pIC50 >25000 nM IC50 J. Med. Chem. (2006) 49: 6819-6832 [PMID:17154512]
cyclin dependent kinase 4/Cyclin-dependent kinase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL331] [GtoPdb: 1976] [UniProtKB: P11802]
ChEMBL Inhibitory activity against Cyclin-dependent kinase 4 B 4.6 pIC50 >25000 nM IC50 Bioorg. Med. Chem. Lett. (2004) 14: 6061-6066 [PMID:15546730]
epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
ChEMBL Inhibition of Her1 B 5.28 pIC50 5200 nM IC50 J. Med. Chem. (2006) 49: 6819-6832 [PMID:17154512]
fibroblast growth factor receptor 1/Fibroblast growth factor receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3650] [GtoPdb: 1808] [UniProtKB: P11362]
ChEMBL Inhibition of FGFR1 B 5 pIC50 >10000 nM IC50 J. Med. Chem. (2006) 49: 6819-6832 [PMID:17154512]
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 Inhibitory activity against HER2 kinase B 5.28 pIC50 5200 nM IC50 Bioorg. Med. Chem. Lett. (2004) 14: 6061-6066 [PMID:15546730]
ChEMBL Inhibition of Her2 B 6.3 pIC50 500 nM IC50 J. Med. Chem. (2006) 49: 6819-6832 [PMID:17154512]
FGR proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase FGR in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4454] [GtoPdb: 2024] [UniProtKB: P09769]
GtoPdb - - 9 pIC50 <1 nM IC50 Bioorg Med Chem Lett (2004) 14: 6061-6 [PMID:15546730]
ChEMBL Inhibitory activity against Fgr kinase B 9 pIC50 <1 nM IC50 Bioorg. Med. Chem. Lett. (2004) 14: 6061-6066 [PMID:15546730]
ChEMBL Inhibition of Fgr B 9.1 pIC50 0.8 nM IC50 J. Med. Chem. (2006) 49: 6819-6832 [PMID:17154512]
FYN proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase FYN in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1841] [GtoPdb: 2026] [UniProtKB: P06241]
GtoPdb - - 9 pIC50 1 nM IC50 Bioorg Med Chem Lett (2004) 14: 6061-6 [PMID:15546730]
ChEMBL inhibitory activity against Fyn protein kinase B 9 pIC50 1 nM IC50 Bioorg. Med. Chem. Lett. (2004) 14: 6061-6066 [PMID:15546730]
ChEMBL Inhibition of Fyn B 9 pIC50 1 nM IC50 J. Med. Chem. (2006) 49: 6819-6832 [PMID:17154512]
HCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase HCK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3234] [GtoPdb: 2032] [UniProtKB: P08631]
ChEMBL inhibitory activity against Hck kinase B 8.7 pIC50 2 nM IC50 Bioorg. Med. Chem. Lett. (2004) 14: 6061-6066 [PMID:15546730]
ChEMBL Inhibition of Hck B 8.7 pIC50 2 nM IC50 J. Med. Chem. (2006) 49: 6819-6832 [PMID:17154512]
GtoPdb - - 8.7 pIC50 2 nM IC50 Bioorg Med Chem Lett (2004) 14: 6061-6 [PMID:15546730]
Janus kinase 3/Tyrosine-protein kinase JAK3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2148] [GtoPdb: 2049] [UniProtKB: P52333]
GtoPdb - - 8.22 pIC50 6 nM IC50 Bioorg Med Chem Lett (2004) 14: 6061-6 [PMID:15546730]
ChEMBL inhibitory activity against Janus kinase 3 B 8.22 pIC50 6 nM IC50 Bioorg. Med. Chem. Lett. (2004) 14: 6061-6066 [PMID:15546730]
LCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase LCK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL258] [GtoPdb: 2053] [UniProtKB: P06239]
GtoPdb - - 9 pIC50 1 nM IC50 Bioorg Med Chem Lett (2004) 14: 6061-6 [PMID:15546730]
ChEMBL Inhibition of human Lck in presence of ATP B 9 pIC50 1 nM IC50 J. Med. Chem. (2006) 49: 6819-6832 [PMID:17154512]
LCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase LCK in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2480] [GtoPdb: 2053] [UniProtKB: P06240]
ChEMBL Inhibition of murine Lck in presence of ATP B 9.89 pKi 0.13 nM Ki J. Med. Chem. (2006) 49: 6819-6832 [PMID:17154512]
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 B 8.4 pIC50 4 nM IC50 J. Med. Chem. (2006) 49: 6819-6832 [PMID:17154512]
SRC proto-oncogene, non-receptor tyrosine kinase/Tyrosine-protein kinase SRC in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL267] [GtoPdb: 2206] [UniProtKB: P12931]
ChEMBL Inhibition of Src in presence of ATP B 8.7 pIC50 <2 nM IC50 J. Med. Chem. (2006) 49: 6819-6832 [PMID:17154512]
GtoPdb - - 9 pIC50 <1 nM IC50 Bioorg Med Chem Lett (2004) 14: 6061-6 [PMID:15546730]
ChEMBL Inhibitory activity against Src tyrosine kinase B 9 pIC50 <1 nM IC50 Bioorg. Med. Chem. Lett. (2004) 14: 6061-6066 [PMID:15546730]
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 Inhibition of Yes B 8.7 pIC50 2 nM IC50 J. Med. Chem. (2006) 49: 6819-6832 [PMID:17154512]
kinase insert domain receptor/Vascular endothelial growth factor receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL279] [GtoPdb: 1813] [UniProtKB: P35968]
ChEMBL inhibitory activity against Vascular endothelial growth factor receptor 2 B 5 pIC50 >10000 nM IC50 Bioorg. Med. Chem. Lett. (2004) 14: 6061-6066 [PMID:15546730]
BLK proto-oncogene, Src family tyrosine kinase in Human [GtoPdb: 1940] [UniProtKB: P51451]
GtoPdb - - 9 pIC50 1 nM IC50 Bioorg Med Chem Lett (2004) 14: 6061-6 [PMID:15546730]

ChEMBL data shown on this page come from version 31:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]