PDGF receptor tyrosine kinase inhibitor IV [Ligand Id: 6020] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL120077 (JNJ-10198409)
  • casein kinase 2, alpha prime polypeptide subunit/casein kinase 2, beta polypeptide subunit/casein kinase 2, alpha 1 polypeptide subunit/Casein kinase II in Human [ChEMBL: CHEMBL2095191] [GtoPdb: 155015511549] [UniProtKB: P19784P67870P68400]
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  • cyclin dependent kinase 1/Cyclin-dependent kinase 1 in Human [ChEMBL: CHEMBL308] [GtoPdb: 1961] [UniProtKB: P06493]
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  • 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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  • cyclin dependent kinase 7/Cyclin-dependent kinase 7 in Human [ChEMBL: CHEMBL3055] [GtoPdb: 1979] [UniProtKB: P50613]
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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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  • protein tyrosine kinase 2/Focal adhesion kinase 1 in Human [ChEMBL: CHEMBL2695] [GtoPdb: 2180] [UniProtKB: Q05397]
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  • mitogen-activated protein kinase 1/MAP kinase ERK2 in Human [ChEMBL: CHEMBL4040] [GtoPdb: 1495] [UniProtKB: P28482]
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  • platelet derived growth factor receptor alpha/Platelet-derived growth factor receptor alpha in Human [ChEMBL: CHEMBL2007] [GtoPdb: 1803] [UniProtKB: P16234]
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  • platelet derived growth factor receptor beta/Platelet-derived growth factor receptor beta in Human [ChEMBL: CHEMBL1913] [GtoPdb: 1804] [UniProtKB: P09619]
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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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  • ABL proto-oncogene 1, non-receptor tyrosine kinase/Tyrosine-protein kinase ABL in Human [ChEMBL: CHEMBL1862] [GtoPdb: 1923] [UniProtKB: P00519]
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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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  • LCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase LCK in Human [ChEMBL: CHEMBL258] [GtoPdb: 2053] [UniProtKB: P06239]
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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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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
casein kinase 2, alpha prime polypeptide subunit/casein kinase 2, beta polypeptide subunit/casein kinase 2, alpha 1 polypeptide subunit/Casein kinase II in Human (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2095191] [GtoPdb: 155015511549] [UniProtKB: P19784P67870P68400]
ChEMBL Inhibitory activity against Casein Kinase 2 B 4 pIC50 >100000 nM IC50 J. Med. Chem. (2005) 48: 8163-8173 [PMID:16366598]
cyclin dependent kinase 1/Cyclin-dependent kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL308] [GtoPdb: 1961] [UniProtKB: P06493]
ChEMBL Inhibitory activity against CDK1 B 4 pIC50 >100000 nM IC50 J. Med. Chem. (2005) 48: 8163-8173 [PMID:16366598]
ChEMBL Inhibition of Cdk1 B 5 pIC50 >10000 nM IC50 Proc. Natl. Acad. Sci. U.S.A. (2007) 104: 20523-20528 [PMID:18077363]
cyclin dependent kinase 2/Cyclin-dependent kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL301] [GtoPdb: 1973] [UniProtKB: P24941]
ChEMBL Inhibitory activity against CDK2 B 5 pIC50 >10000 nM IC50 J. Med. Chem. (2005) 48: 8163-8173 [PMID:16366598]
ChEMBL Inhibition of Cdk2 B 5 pIC50 >10000 nM IC50 Proc. Natl. Acad. Sci. U.S.A. (2007) 104: 20523-20528 [PMID:18077363]
cyclin dependent kinase 4/Cyclin-dependent kinase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL331] [GtoPdb: 1976] [UniProtKB: P11802]
ChEMBL Inhibitory activity against CDK4 B 4 pIC50 >100000 nM IC50 J. Med. Chem. (2005) 48: 8163-8173 [PMID:16366598]
ChEMBL Inhibition of Cdk4 B 4 pIC50 >100000 nM IC50 Proc. Natl. Acad. Sci. U.S.A. (2007) 104: 20523-20528 [PMID:18077363]
cyclin dependent kinase 7/Cyclin-dependent kinase 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3055] [GtoPdb: 1979] [UniProtKB: P50613]
ChEMBL Inhibitory activity against CDK7 B 4.25 pIC50 56700 nM IC50 J. Med. Chem. (2005) 48: 8163-8173 [PMID:16366598]
ChEMBL Inhibition of Cdk7 B 5 pIC50 >10000 nM IC50 Proc. Natl. Acad. Sci. U.S.A. (2007) 104: 20523-20528 [PMID:18077363]
epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
ChEMBL Inhibitory activity against EGFR B 4 pIC50 >100000 nM IC50 J. Med. Chem. (2005) 48: 8163-8173 [PMID:16366598]
ChEMBL Inhibition of human EGFR at 10000 nM B 4 pIC50 >100000 nM IC50 Proc. Natl. Acad. Sci. U.S.A. (2007) 104: 20523-20528 [PMID:18077363]
fibroblast growth factor receptor 1/Fibroblast growth factor receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3650] [GtoPdb: 1808] [UniProtKB: P11362]
ChEMBL Inhibitory activity against bFGFR1 B 4.34 pIC50 45800 nM IC50 J. Med. Chem. (2005) 48: 8163-8173 [PMID:16366598]
ChEMBL Inhibition of bFGFR1 B 4.34 pIC50 45800 nM IC50 Proc. Natl. Acad. Sci. U.S.A. (2007) 104: 20523-20528 [PMID:18077363]
protein tyrosine kinase 2/Focal adhesion kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2695] [GtoPdb: 2180] [UniProtKB: Q05397]
ChEMBL Inhibitory activity against FAK B 4 pIC50 >100000 nM IC50 J. Med. Chem. (2005) 48: 8163-8173 [PMID:16366598]
Insulin receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1981] [GtoPdb: 1800] [UniProtKB: P06213]
ChEMBL Inhibitory activity against IRK B 4 pIC50 >100000 nM IC50 J. Med. Chem. (2005) 48: 8163-8173 [PMID:16366598]
mitogen-activated protein kinase 1/MAP kinase ERK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4040] [GtoPdb: 1495] [UniProtKB: P28482]
ChEMBL Inhibitory activity against MAPK B 4 pIC50 >100000 nM IC50 J. Med. Chem. (2005) 48: 8163-8173 [PMID:16366598]
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 Inhibitory activity against PDGFRalpha B 7.35 pIC50 45 nM IC50 J. Med. Chem. (2005) 48: 8163-8173 [PMID:16366598]
ChEMBL Inhibition of PDGFRalpha B 7.35 pIC50 45 nM IC50 Proc. Natl. Acad. Sci. U.S.A. (2007) 104: 20523-20528 [PMID:18077363]
platelet derived growth factor receptor beta/Platelet-derived growth factor receptor beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1913] [GtoPdb: 1804] [UniProtKB: P09619]
ChEMBL Inhibitory activity against PDGFRbeta kinase B 8.38 pIC50 4.2 nM IC50 J. Med. Chem. (2005) 48: 8163-8173 [PMID:16366598]
ChEMBL Inhibition of PDGFRbeta B 8.38 pIC50 4.2 nM IC50 Proc. Natl. Acad. Sci. U.S.A. (2007) 104: 20523-20528 [PMID:18077363]
GtoPdb - - 8.38 pIC50 4.2 nM IC50 J Med Chem (2005) 48: 8163-73 [PMID:16366598]
ChEMBL Antiproliferative activity against PDGF-BB stimulated HCASMC F 8.52 pIC50 3 nM IC50 J. Med. Chem. (2005) 48: 8163-8173 [PMID:16366598]
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 B 5 pIC50 >10000 nM IC50 J. Med. Chem. (2005) 48: 8163-8173 [PMID:16366598]
ChEMBL Inhibition of HER2 B 5 pIC50 >10000 nM IC50 Proc. Natl. Acad. Sci. U.S.A. (2007) 104: 20523-20528 [PMID:18077363]
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 Inhibitory activity against c-ABL B 7.66 pIC50 22 nM IC50 J. Med. Chem. (2005) 48: 8163-8173 [PMID:16366598]
ChEMBL Inhibition of cAbl B 7.66 pIC50 22 nM IC50 Proc. Natl. Acad. Sci. U.S.A. (2007) 104: 20523-20528 [PMID:18077363]
FYN proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase FYN in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1841] [GtoPdb: 2026] [UniProtKB: P06241]
ChEMBL Inhibitory activity against FYN B 6.42 pIC50 378 nM IC50 J. Med. Chem. (2005) 48: 8163-8173 [PMID:16366598]
ChEMBL Inhibition of Fyn B 6.42 pIC50 378 nM IC50 Proc. Natl. Acad. Sci. U.S.A. (2007) 104: 20523-20528 [PMID:18077363]
LCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase LCK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL258] [GtoPdb: 2053] [UniProtKB: P06239]
ChEMBL Inhibitory activity against LCK B 7 pIC50 100 nM IC50 J. Med. Chem. (2005) 48: 8163-8173 [PMID:16366598]
ChEMBL Inhibition of Lck B 7 pIC50 100 nM IC50 Proc. Natl. Acad. Sci. U.S.A. (2007) 104: 20523-20528 [PMID:18077363]
SRC proto-oncogene, non-receptor tyrosine kinase/Tyrosine-protein kinase SRC in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL267] [GtoPdb: 2206] [UniProtKB: P12931]
ChEMBL Inhibitory activity against c-SRC B 6.73 pIC50 185 nM IC50 J. Med. Chem. (2005) 48: 8163-8173 [PMID:16366598]
ChEMBL Inhibition of c-Src B 6.73 pIC50 185 nM IC50 Proc. Natl. Acad. Sci. U.S.A. (2007) 104: 20523-20528 [PMID:18077363]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos 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]