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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 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]