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ChEMBL ligand: CHEMBL1784637 |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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cyclin dependent kinase 2/Cyclin-dependent kinase 2/cyclin E1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907605] [GtoPdb: 1973] [UniProtKB: P24864, P24941] | ||||||||
ChEMBL | Inhibition of human CDK2/Cyclin E using Histone H1 substrate by Hotspot assay | B | 8.19 | pIC50 | 6.4 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 3743-3748 [PMID:21561767] |
EPH receptor A2/Ephrin type-A receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2068] [GtoPdb: 1822] [UniProtKB: P29317] | ||||||||
GtoPdb | - | - | 9.22 | pIC50 | 0.6 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 3743-8 [PMID:21561767] |
ChEMBL | Inhibition of human EPHA2 using poly[Glu:Tyr] peptide substrate by Hotspot assay | B | 9.22 | pIC50 | 0.6 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 3743-3748 [PMID:21561767] |
EPH receptor A3/Ephrin type-A receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4954] [GtoPdb: 1823] [UniProtKB: P29320] | ||||||||
GtoPdb | - | - | 8.92 | pIC50 | 1.2 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 3743-8 [PMID:21561767] |
ChEMBL | Inhibition of human EPHA3 using poly[Glu:Tyr] peptide substrate by Hotspot assay | B | 8.92 | pIC50 | 1.2 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 3743-3748 [PMID:21561767] |
EPH receptor A7/Ephrin type-A receptor 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4602] [GtoPdb: 1827] [UniProtKB: Q15375] | ||||||||
ChEMBL | Inhibition of human EPHA7 using poly[Glu:Tyr] peptide substrate by Hotspot assay | B | 8.38 | pIC50 | 4.2 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 3743-3748 [PMID:21561767] |
GtoPdb | - | - | 8.38 | pIC50 | 4.2 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 3743-8 [PMID:21561767] |
epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533] | ||||||||
ChEMBL | Inhibition of human EGFR L858R, T790M mutant using poly[Glu:Tyr] by Hotspot assay | B | 5.52 | pIC50 | >3000 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 3743-3748 [PMID:21561767] |
ChEMBL | Inhibition of human EGFR T790M mutant using poly[Glu:Tyr] by Hotspot assay | B | 5.52 | pIC50 | >3000 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 3743-3748 [PMID:21561767] |
ChEMBL | Inhibition of human EGFR using poly[Glu:Tyr] by Hotspot assay | B | 6.13 | pIC50 | 736 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 3743-3748 [PMID:21561767] |
ChEMBL | Inhibition of human EGFR L858R mutant using poly[Glu:Tyr] by Hotspot assay | B | 6.64 | pIC50 | 231 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 3743-3748 [PMID:21561767] |
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 human FGFR1 using KKKSPGEYVNIEFG peptide substrate by Hotspot assay | B | 8.74 | pIC50 | 1.8 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 3743-3748 [PMID:21561767] |
fibroblast growth factor receptor 2/Fibroblast growth factor receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4142] [GtoPdb: 1809] [UniProtKB: P21802] | ||||||||
ChEMBL | Inhibition of human FGFR2 using poly[Glu:Tyr] peptide substrate by Hotspot assay | B | 8.82 | pIC50 | 1.5 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 3743-3748 [PMID:21561767] |
fibroblast growth factor receptor 3/Fibroblast growth factor receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2742] [GtoPdb: 1810] [UniProtKB: P22607] | ||||||||
ChEMBL | Inhibition of human FGFR3 using poly[Glu:Tyr] peptide substrate by Hotspot assay | B | 7.98 | pIC50 | 10.5 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 3743-3748 [PMID:21561767] |
fibroblast growth factor receptor 4/Fibroblast growth factor receptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3973] [GtoPdb: 1811] [UniProtKB: P22455] | ||||||||
ChEMBL | Inhibition of human FGFR4 using poly[Glu:Tyr] peptide substrate by Hotspot assay | B | 7.47 | pIC50 | 34 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 3743-3748 [PMID:21561767] |
MET proto-oncogene, receptor tyrosine kinase/Hepatocyte growth factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3717] [GtoPdb: 1815] [UniProtKB: P08581] | ||||||||
ChEMBL | Inhibition of human c-Met using KKKSPGEYVNIEFG peptide substrate by Hotspot assay | B | 5.52 | pIC50 | >3000 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 3743-3748 [PMID:21561767] |
Insulin receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1981] [GtoPdb: 1800] [UniProtKB: P06213] | ||||||||
ChEMBL | Inhibition of human IR using poly[Glu:Tyr] by Hotspot assay | B | 5.52 | pIC50 | >3000 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 3743-3748 [PMID:21561767] |
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 human PDGFRalpha using poly[Glu:Tyr] by Hotspot assay | B | 8.89 | pIC50 | 1.3 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 3743-3748 [PMID:21561767] |
GtoPdb | - | - | 8.89 | pIC50 | 1.3 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 3743-8 [PMID:21561767] |
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 human PDGFRbeta using poly[Glu:Tyr] by Hotspot assay | B | 8.59 | pIC50 | 2.6 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 3743-3748 [PMID:21561767] |
aurora kinase A/Serine/threonine-protein kinase Aurora-A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4722] [GtoPdb: 1936] [UniProtKB: O14965] | ||||||||
ChEMBL | Inhibition of human Aurora A using H-LRRASLG peptide substrate by Hotspot assay | B | 5.52 | pIC50 | >3000 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 3743-3748 [PMID:21561767] |
B-Raf proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase B-raf in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5145] [GtoPdb: 1943] [UniProtKB: P15056] | ||||||||
ChEMBL | Inhibition of human BRAF V599E mutant using MEK1 (K97R), ATP substrate by Hotspot assay | B | 7.59 | pIC50 | 26 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 3743-3748 [PMID:21561767] |
ChEMBL | Inhibition of human BRAF using MEK1 (K97R), ATP substrate by Hotspot assay | B | 7.7 | pIC50 | 20 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 3743-3748 [PMID:21561767] |
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 human c-Kit using poly[Glu:Tyr] by Hotspot assay | B | 5.52 | pIC50 | >3000 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 3743-3748 [PMID:21561767] |
ABL proto-oncogene 1, non-receptor tyrosine kinase/Tyrosine-protein kinase ABL in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1862] [GtoPdb: 1923] [UniProtKB: P00519] | ||||||||
ChEMBL | Inhibition of human ABL T315I mutant using [EAIYAAPFAKKK] peptide substrate after 2 hrs by TR-FRET assay | B | 7.22 | pIC50 | 60.2 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 3743-3748 [PMID:21561767] |
ChEMBL | Inhibition of wild type human ABL using [EAIYAAPFAKKK] peptide substrate after 1 hr by TR-FRET assay | B | 7.76 | pIC50 | 17.2 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 3743-3748 [PMID:21561767] |
ChEMBL | Inhibition of human ABL T315I mutant using [EAIYAAPFAKKK] peptide substrate by Hotspot assay | B | 9.4 | pIC50 | 0.4 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 3743-3748 [PMID:21561767] |
ChEMBL | Inhibition of wild type human ABL using [EAIYAAPFAKKK] peptide substrate by Hotspot assay | B | 9.7 | pIC50 | 0.2 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 3743-3748 [PMID:21561767] |
GtoPdb | - | - | 9.7 | pIC50 | 0.2 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 3743-8 [PMID:21561767] |
Janus kinase 1/Tyrosine-protein kinase JAK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2835] [GtoPdb: 2047] [UniProtKB: P23458] | ||||||||
ChEMBL | Inhibition of human JAK1 using poly[Glu:Tyr] by Hotspot assay | B | 7.26 | pIC50 | 55.3 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 3743-3748 [PMID:21561767] |
Janus kinase 2/Tyrosine-protein kinase JAK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2971] [GtoPdb: 2048] [UniProtKB: O60674] | ||||||||
ChEMBL | Inhibition of human JAK2 using poly[Glu:Tyr] by Hotspot assay | B | 6.27 | pIC50 | 536 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 3743-3748 [PMID:21561767] |
Janus kinase 3/Tyrosine-protein kinase JAK3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2148] [GtoPdb: 2049] [UniProtKB: P52333] | ||||||||
ChEMBL | Inhibition of human JAK3 using GEEEEYFELVKKKK peptide substrate by Hotspot assay | B | 7.24 | pIC50 | 57.5 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 3743-3748 [PMID:21561767] |
LYN proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase Lyn in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3905] [GtoPdb: 2060] [UniProtKB: P07948] | ||||||||
ChEMBL | Inhibition of human LYN using poly[Glu:Tyr] by Hotspot assay | B | 9.82 | pIC50 | <0.15 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 3743-3748 [PMID:21561767] |
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 human FMS using poly[Glu:Tyr] by Hotspot assay | B | 8.14 | pIC50 | 7.2 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 3743-3748 [PMID:21561767] |
ChEMBL | Inhibition of human FLT3 using EAIYAAPFAKKK peptide substrate by Hotspot assay | B | 8.7 | pIC50 | 2 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 3743-3748 [PMID:21561767] |
ret proto-oncogene/Tyrosine-protein kinase receptor RET in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2041] [GtoPdb: 2185] [UniProtKB: P07949] | ||||||||
ChEMBL | Inhibition of human RET using KKKSPGEYVNIEFG by Hotspot assay | B | 9.7 | pIC50 | 0.2 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 3743-3748 [PMID:21561767] |
GtoPdb | - | - | 9.7 | pIC50 | 0.2 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 3743-8 [PMID:21561767] |
SRC proto-oncogene, non-receptor tyrosine kinase/Tyrosine-protein kinase SRC in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL267] [GtoPdb: 2206] [UniProtKB: P12931] | ||||||||
ChEMBL | Inhibition of human Src using poly[Glu:Tyr] by Hotspot assay | B | 8.4 | pIC50 | 4 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 3743-3748 [PMID:21561767] |
TEK receptor tyrosine kinase/Tyrosine-protein kinase TIE-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4128] [GtoPdb: 1842] [UniProtKB: Q02763] | ||||||||
ChEMBL | Inhibition of human Tie2/TEK using poly[Glu:Tyr] by Hotspot assay | B | 8.66 | pIC50 | 2.2 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 3743-3748 [PMID:21561767] |
GtoPdb | - | - | 8.66 | pIC50 | 2.2 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 3743-8 [PMID:21561767] |
fms related receptor tyrosine kinase 1/Vascular endothelial growth factor receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1868] [GtoPdb: 1812] [UniProtKB: P17948] | ||||||||
ChEMBL | Inhibition of human VEGFR1 using poly[Glu:Tyr] by Hotspot assay | B | 8.28 | pIC50 | 5.2 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 3743-3748 [PMID:21561767] |
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 human VEGFR2 using poly[Glu:Tyr] by Hotspot assay | B | 8.64 | pIC50 | 2.3 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 3743-3748 [PMID:21561767] |
fms related receptor tyrosine kinase 4/Vascular endothelial growth factor receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1955] [GtoPdb: 1814] [UniProtKB: P35916] | ||||||||
ChEMBL | Inhibition of human VEGFR3 using poly[Glu:Tyr] by Hotspot assay | B | 8.59 | pIC50 | 2.6 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 3743-3748 [PMID:21561767] |
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]