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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 |
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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 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]