compound 8i [PMID: 22765894] [Ligand Id: 9905] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL2087167 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| fibroblast growth factor receptor 1/Fibroblast growth factor receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3650] [GtoPdb: 1808] [UniProtKB: P11362] | ||||||||
| ChEMBL | Inhibition of FGFR1 in human SK-N-MC cells assessed as inhibition of FGF-induced ERK phosphorylation incubated for 1 hr prior to VEGF-stimulation measured after 30 mins by ELISA | B | 7.7 | pIC50 | 20 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 4979-4985 [PMID:22765894] |
| GtoPdb | - | - | 8.21 | pIC50 | 6.2 | nM | IC50 | Cancer Res (2011) 71: 4758-68 [PMID:21613405] |
| ChEMBL | Inhibition of N-terminal GST-tagged FGFR1 using poly(Glu,Tyr) as substrate after 30 mins by alphascreen assay | B | 8.4 | pIC50 | 4 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 4979-4985 [PMID:22765894] |
| GtoPdb | - | - | 8.4 | pIC50 | 4 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 4979-85 [PMID:22765894] |
| 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 N-terminal GST-tagged PDGFRalpha after 2 hrs by luciferase-luciferin coupled chemiluminescence assay | B | 8.7 | pIC50 | 2 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 4979-4985 [PMID:22765894] |
| GtoPdb | - | - | 8.7 | pIC50 | 2 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 4979-85 [PMID:22765894] |
| fms related receptor tyrosine kinase 1/Vascular endothelial growth factor receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1868] [GtoPdb: 1812] [UniProtKB: P17948] | ||||||||
| GtoPdb | - | - | 7.54 | pIC50 | 29 | nM | IC50 | Cancer Res (2011) 71: 4758-68 [PMID:21613405] |
| ChEMBL | Inhibition of N-terminal GST-tagged Flt1 using poly(Glu,Tyr) as substrate after 60 mins by alphascreen assay | B | 7.7 | pIC50 | 20 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 4979-4985 [PMID:22765894] |
| GtoPdb | - | - | 7.7 | pIC50 | 20 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 4979-85 [PMID:22765894] |
| 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 KDR in human HUVEC cells assessed as inhibition of VEGF-induced ERK phosphorylation incubated for 1 hr prior to VEGF-stimulation measured after 5 mins by ELISA | B | 8.22 | pIC50 | 6 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 4979-4985 [PMID:22765894] |
| ChEMBL | Inhibition of N-terminal GST-tagged KDR after 4 hrs by luciferase-luciferin coupled chemiluminescence assay | B | 8.4 | pIC50 | 4 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 4979-4985 [PMID:22765894] |
| GtoPdb | - | - | 8.4 | pIC50 | 4 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 4979-85 [PMID:22765894] |
| GtoPdb | - | - | 8.59 | pIC50 | 2.6 | nM | IC50 | Cancer Res (2011) 71: 4758-68 [PMID:21613405] |
| platelet derived growth factor receptor beta in Human [GtoPdb: 1804] [UniProtKB: P09619] | ||||||||
| GtoPdb | - | - | 8.82 | pIC50 | 1.5 | nM | IC50 | Cancer Res (2011) 71: 4758-68 [PMID:21613405] |
| KIT proto-oncogene, receptor tyrosine kinase in Human [GtoPdb: 1805] [UniProtKB: P10721] | ||||||||
| GtoPdb | - | - | 7.86 | pIC50 | 13.8 | nM | IC50 | Cancer Res (2011) 71: 4758-68 [PMID:21613405] |
| fms related receptor tyrosine kinase 3 in Human [GtoPdb: 1807] [UniProtKB: P36888] | ||||||||
| GtoPdb | - | - | 9.1 | pIC50 | 0.8 | nM | IC50 | Cancer Res (2011) 71: 4758-68 [PMID:21613405] |
| fms related receptor tyrosine kinase 4 in Human [GtoPdb: 1814] [UniProtKB: P35916] | ||||||||
| GtoPdb | - | - | 8.52 | pIC50 | 3 | nM | IC50 | Cancer Res (2011) 71: 4758-68 [PMID:21613405] |
| MET proto-oncogene, receptor tyrosine kinase in Human [GtoPdb: 1815] [UniProtKB: P08581] | ||||||||
| GtoPdb | - | - | 6.33 | pIC50 | 463 | nM | IC50 | Cancer Res (2011) 71: 4758-68 [PMID:21613405] |
| macrophage stimulating 1 receptor in Human [GtoPdb: 1816] [UniProtKB: Q04912] | ||||||||
| GtoPdb | - | - | 6.91 | pIC50 | 124 | nM | IC50 | Cancer Res (2011) 71: 4758-68 [PMID:21613405] |
| AXL receptor tyrosine kinase in Human [GtoPdb: 1835] [UniProtKB: P30530] | ||||||||
| GtoPdb | - | - | 8.34 | pIC50 | 4.6 | nM | IC50 | Cancer Res (2011) 71: 4758-68 [PMID:21613405] |
| TEK receptor tyrosine kinase in Human [GtoPdb: 1842] [UniProtKB: Q02763] | ||||||||
| GtoPdb | - | - | 6.57 | pIC50 | 270 | nM | IC50 | Cancer Res (2011) 71: 4758-68 [PMID:21613405] |
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]
