PDGF receptor tyrosine kinase inhibitor III [Ligand Id: 6019] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL102346
  • epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
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  • platelet derived growth factor receptor beta/platelet derived growth factor receptor alpha/Platelet-derived growth factor receptor in Human [ChEMBL: CHEMBL2095189] [GtoPdb: 18041803] [UniProtKB: P09619P16234]
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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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  • KIT proto-oncogene, receptor tyrosine kinase/Stem cell growth factor receptor in Human [ChEMBL: CHEMBL1936] [GtoPdb: 1805] [UniProtKB: P10721]
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  • fms related receptor tyrosine kinase 3/Tyrosine-protein kinase receptor FLT3 in Human [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888]
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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
epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
ChEMBL Inhibition of Epidermal growth factor receptor B 4.52 pIC50 >30000 nM IC50 J Med Chem (2002) 45: 3057-3066 [PMID:12086491]
platelet derived growth factor receptor beta/platelet derived growth factor receptor alpha/Platelet-derived growth factor receptor in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2095189] [GtoPdb: 18041803] [UniProtKB: P09619P16234]
ChEMBL Concentration required for 50% inhibition against autophosphorylation of Platelet-derived growth factor receptor beta in intact cells using a two site ELISA B 7.1 pIC50 80 nM IC50 J Med Chem (2002) 45: 4513-4523 [PMID:12238930]
GtoPdb - - 7.1 pIC50 80 nM IC50 J Med Chem (2003) 46: 4910-25 [PMID:14584942]
platelet derived growth factor receptor alpha/Platelet-derived growth factor receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2007] [GtoPdb: 1803] [UniProtKB: P16234]
ChEMBL Inhibition of Platelet-derived growth factor receptor alpha B 7.3 pIC50 50 nM IC50 J Med Chem (2002) 45: 3057-3066 [PMID:12086491]
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 Inhibition of Platelet-derived growth factor receptor beta B 6.89 pIC50 130 nM IC50 J Med Chem (2002) 45: 3057-3066 [PMID:12086491]
ChEMBL Inhibition of platelet-derived growth factor receptor beta phosphorylation was measured in intact cells using a two-site enzyme linked immunosorbent assay (ELISA) B 7.1 pIC50 80 nM IC50 J Med Chem (2003) 46: 4910-4925 [PMID:14584942]
ChEMBL Inhibitory concentration against platelet-derived growth factor receptor beta phosphorylation in CHO cells F 7.1 pIC50 >80 nM IC50 Bioorg Med Chem Lett (2003) 13: 3001-3004 [PMID:12941321]
ChEMBL Inhibition of Platelet-derived growth factor receptor beta phosphorylation B 7.1 pIC50 80 nM IC50 J Med Chem (2002) 45: 3057-3066 [PMID:12086491]
GtoPdb - - 7.1 pIC50 80 nM IC50 J Med Chem (2003) 46: 4910-25 [PMID:14584942]
KIT proto-oncogene, receptor tyrosine kinase/Stem cell growth factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1936] [GtoPdb: 1805] [UniProtKB: P10721]
ChEMBL Inhibition of Mast/stem cell growth factor receptor (c-Kit kinase) B 7.3 pIC50 50 nM IC50 J Med Chem (2002) 45: 3057-3066 [PMID:12086491]
fms related receptor tyrosine kinase 3/Tyrosine-protein kinase receptor FLT3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888]
ChEMBL Inhibition of Flt3 kinase B 6.64 pIC50 230 nM IC50 J Med Chem (2002) 45: 3057-3066 [PMID:12086491]
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 protein tyrosine kinase B 4.52 pIC50 >30000 nM IC50 J Med Chem (2002) 45: 3057-3066 [PMID:12086491]

ChEMBL data shown on this page come from version 33:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]