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 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]
