AG 1295 [Ligand Id: 5914] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL7724 (AG-1295) |
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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: 1804, 1803] [UniProtKB: P05622, P26618] | ||||||||
| 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 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]
