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 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]