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ChEMBL ligand: CHEMBL2086760 |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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EPH receptor A2/Ephrin type-A receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2068] [GtoPdb: 1822] [UniProtKB: P29317] | ||||||||
ChEMBL | Inhibition of EphA2 | B | 5.77 | pIC50 | 1700 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 4979-4985 [PMID:22765894] |
EPH receptor B4/Ephrin type-B receptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5147] [GtoPdb: 1833] [UniProtKB: P54760] | ||||||||
ChEMBL | Inhibition of EphB4 | B | 5.9 | pIC50 | 1250 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 4979-4985 [PMID:22765894] |
epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533] | ||||||||
ChEMBL | Inhibition of EGFR | B | 6.86 | pIC50 | 137 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 4979-4985 [PMID:22765894] |
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 | 7.62 | pIC50 | 24 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 4979-4985 [PMID:22765894] |
ChEMBL | Inhibition of N-terminal GST-tagged FGFR1 using poly(Glu,Tyr) as substrate after 30 mins by alphascreen assay | B | 8.22 | pIC50 | 6 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 4979-4985 [PMID:22765894] |
GtoPdb | - | - | 8.24 | pIC50 | 5.7 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 4979-85 [PMID:22765894] |
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
ChEMBL | Binding affinity to human ERG | B | 5.47 | pIC50 | 3367 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 4979-4985 [PMID:22765894] |
Insulin-like growth factor I receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1957] [GtoPdb: 1801] [UniProtKB: P08069] | ||||||||
ChEMBL | Inhibition of IGF1R | B | 5.57 | pIC50 | 2700 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 4979-4985 [PMID:22765894] |
Insulin receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1981] [GtoPdb: 1800] [UniProtKB: P06213] | ||||||||
ChEMBL | Inhibition of IRK | B | 5.39 | pIC50 | 4100 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 4979-4985 [PMID:22765894] |
mitogen-activated protein kinase kinase kinase kinase 3/Mitogen-activated protein kinase kinase kinase kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5432] [GtoPdb: 2087] [UniProtKB: Q8IVH8] | ||||||||
GtoPdb | - | - | 7.6 | pIC50 | 25 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 4979-85 [PMID:22765894] |
ChEMBL | Inhibition of MAP4K3 | B | 7.6 | pIC50 | 25 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 4979-4985 [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] | ||||||||
GtoPdb | - | - | 8.52 | pIC50 | 3 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 4979-85 [PMID:22765894] |
ChEMBL | Inhibition of N-terminal GST-tagged PDGFRalpha after 2 hrs by luciferase-luciferin coupled chemiluminescence assay | B | 8.52 | pIC50 | 3 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 4979-4985 [PMID:22765894] |
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 | 8.89 | pIC50 | 1.3 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 4979-4985 [PMID:22765894] |
GtoPdb | - | - | 8.89 | pIC50 | 1.3 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 4979-85 [PMID:22765894] |
ribosomal protein S6 kinase A3/Ribosomal protein S6 kinase alpha 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2345] [GtoPdb: 1528] [UniProtKB: P51812] | ||||||||
GtoPdb | - | - | 8.52 | pIC50 | 3 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 4979-85 [PMID:22765894] |
ChEMBL | Inhibition of RSK2 | B | 8.52 | pIC50 | 3 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 4979-4985 [PMID:22765894] |
KIT proto-oncogene, receptor tyrosine kinase/Stem cell growth factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1936] [GtoPdb: 1805] [UniProtKB: P10721] | ||||||||
ChEMBL | Inhibition of c-KIT | B | 7.96 | pIC50 | 11 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 4979-4985 [PMID:22765894] |
GtoPdb | - | - | 7.96 | pIC50 | 11 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 4979-85 [PMID:22765894] |
fms related receptor tyrosine kinase 3/Tyrosine-protein kinase receptor FLT3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888] | ||||||||
GtoPdb | - | - | 9.07 | pIC50 | 0.85 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 4979-85 [PMID:22765894] |
ChEMBL | Inhibition of Flt3 | B | 9.07 | pIC50 | 0.85 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 4979-4985 [PMID:22765894] |
SRC proto-oncogene, non-receptor tyrosine kinase/Tyrosine-protein kinase SRC in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL267] [GtoPdb: 2206] [UniProtKB: P12931] | ||||||||
GtoPdb | - | - | 7.48 | pIC50 | 33 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 4979-85 [PMID:22765894] |
ChEMBL | Inhibition of SRC | B | 7.48 | pIC50 | 33 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 4979-4985 [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 | - | - | 8.14 | pIC50 | 7.2 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 4979-85 [PMID:22765894] |
ChEMBL | Inhibition of N-terminal GST-tagged Flt1 using poly(Glu,Tyr) as substrate after 60 mins by alphascreen assay | B | 8.15 | pIC50 | 7 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 4979-4985 [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 | 7.96 | pIC50 | 11 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 4979-4985 [PMID:22765894] |
GtoPdb | - | - | 8.38 | pIC50 | 4.2 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 4979-85 [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] |
fms related receptor tyrosine kinase 4/Vascular endothelial growth factor receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1955] [GtoPdb: 1814] [UniProtKB: P35916] | ||||||||
GtoPdb | - | - | 8.49 | pIC50 | 3.2 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 4979-85 [PMID:22765894] |
ChEMBL | Inhibition of Flt4 | B | 8.49 | pIC50 | 3.2 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 4979-4985 [PMID:22765894] |
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]