AG 1295 [Ligand Id: 5914] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL7724 (AG-1295)
  • platelet derived growth factor receptor beta/platelet derived growth factor receptor alpha/Platelet-derived growth factor receptor in Mouse [ChEMBL: CHEMBL2096980] [GtoPdb: 18041803] [UniProtKB: P05622P26618]
  • This target only has 0 pki data point
  • 0
1 CHEMBL7724_lig_chart_1 Platelet-derived growth factor receptor Mouse
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  • platelet derived growth factor receptor beta/Platelet-derived growth factor receptor beta in Human [ChEMBL: CHEMBL1913] [GtoPdb: 1804] [UniProtKB: P09619]
  • platelet derived growth factor receptor beta/Platelet-derived growth factor receptor beta in Mouse [ChEMBL: CHEMBL2749] [GtoPdb: 1804] [UniProtKB: P05622]
  • This target only has 0 pki data point
  • 0
2 CHEMBL7724_lig_chart_2 Platelet-derived growth factor receptor beta HumanMouse
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  • fms related receptor tyrosine kinase 3/Tyrosine-protein kinase receptor FLT3 in Human [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888]
  • This target only has 0 pki data point
  • 0
3 CHEMBL7724_lig_chart_3 Tyrosine-protein kinase receptor FLT3 Human
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  • kinase insert domain receptor/Vascular endothelial growth factor receptor 2 in Human [ChEMBL: CHEMBL279] [GtoPdb: 1813] [UniProtKB: P35968]
  • This target only has 0 pki data point
  • 0
4 CHEMBL7724_lig_chart_4 Vascular endothelial growth factor receptor 2 Human
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
platelet derived growth factor receptor beta/platelet derived growth factor receptor alpha/Platelet-derived growth factor receptor in Mouse (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2096980] [GtoPdb: 18041803] [UniProtKB: P05622P26618]
ChEMBL Inhibition of endogenous PDGFR in Swiss3T3 fibroblasts B 5.27 pIC50 5400 nM IC50 J. Med. Chem. (2006) 49: 3101-3115 [PMID:16722630]
ChEMBL Inhibitory activity against platelet-derived growth factor receptor tyrosine kinase in Swiss 3T3 cells B 6.4 pIC50 400 nM IC50 J. Med. Chem. (1996) 39: 2170-2177 [PMID:8667360]
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 PDGFRbeta B 5.19 pIC50 6500 nM IC50 Bioorg. Med. Chem. Lett. (2010) 20: 3177-3181 [PMID:20403693]
ChEMBL Inhibition of PDGFRbeta expressed in human tumor cells B 5.21 pIC50 6200 nM IC50 Bioorg. Med. Chem. (2008) 16: 5514-5528 [PMID:18467105]
ChEMBL Inhibition of PDGFBB-induced PDGFRbeta autophosphorylation in human SF539 cells incubated for 60 mins prior to PDGFBB-induction measured after 10 mins by phosphotyrosine ELISA B 5.21 pIC50 6200 nM IC50 Bioorg. Med. Chem. (2012) 20: 2444-2454 [PMID:22370340]
ChEMBL Inhibition of PDGF-BB-induced PDGFR beta phosphorylation in human SF539 cells overexpressing PDGFR beta pretreated for 60 mins prior to PDGF-BB addition measured after 10 mins by phosphotyrosine ELISA cytoblot analysis B 5.21 pIC50 6200 nM IC50 Bioorg. Med. Chem. (2013) 21: 1312-1323 [PMID:23375090]
platelet derived growth factor receptor beta/Platelet-derived growth factor receptor beta in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2749] [GtoPdb: 1804] [UniProtKB: P05622]
ChEMBL Inhibition of endogenous PDGFRbeta autophosphorylation in Swiss 3T3 fibroblasts B 5.27 pIC50 5400 nM IC50 Bioorg. Med. Chem. (2007) 15: 2187-2197 [PMID:17210255]
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 endogenous FLT3 in EOL1 cells B 5.96 pIC50 1100 nM IC50 J. Med. Chem. (2006) 49: 3101-3115 [PMID:16722630]
ChEMBL Inhibition of endogenous FLT3 autophosphorylation in EOL1 cells B 5.96 pIC50 1100 nM IC50 Bioorg. Med. Chem. (2007) 15: 2187-2197 [PMID:17210255]
kinase insert domain receptor/Vascular endothelial growth factor receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL279] [GtoPdb: 1813] [UniProtKB: P35968]
ChEMBL Inhibition of VEGFR2 in human U251 cells by phosphotyrosine ELISA B 5.21 pIC50 6200 nM IC50 Bioorg. Med. Chem. (2009) 17: 7324-7336 [PMID:19748785]

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]