compound 8h [PMID: 21561767] | Ligand Activity Charts

Home
Ligands
compound 8h [PMID: 21561767]
Ligand Activity Charts

compound 8h [PMID: 21561767] [Ligand Id: 8170] activity data from GtoPdb and ChEMBL

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL1784637
cyclin dependent kinase 2/Cyclin-dependent kinase 2/cyclin E1 in Human [ChEMBL: CHEMBL1907605] [GtoPdb: 1973] [UniProtKB: P24864, P24941] There should be some charts here, you may need to enable JavaScript!
EPH receptor A2/Ephrin type-A receptor 2 in Human [ChEMBL: CHEMBL2068] [GtoPdb: 1822] [UniProtKB: P29317] There should be some charts here, you may need to enable JavaScript!
EPH receptor A3/Ephrin type-A receptor 3 in Human [ChEMBL: CHEMBL4954] [GtoPdb: 1823] [UniProtKB: P29320] There should be some charts here, you may need to enable JavaScript!
EPH receptor A7/Ephrin type-A receptor 7 in Human [ChEMBL: CHEMBL4602] [GtoPdb: 1827] [UniProtKB: Q15375] There should be some charts here, you may need to enable JavaScript!
epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533] There should be some charts here, you may need to enable JavaScript!
fibroblast growth factor receptor 1/Fibroblast growth factor receptor 1 in Human [ChEMBL: CHEMBL3650] [GtoPdb: 1808] [UniProtKB: P11362] There should be some charts here, you may need to enable JavaScript!
fibroblast growth factor receptor 2/Fibroblast growth factor receptor 2 in Human [ChEMBL: CHEMBL4142] [GtoPdb: 1809] [UniProtKB: P21802] There should be some charts here, you may need to enable JavaScript!
fibroblast growth factor receptor 3/Fibroblast growth factor receptor 3 in Human [ChEMBL: CHEMBL2742] [GtoPdb: 1810] [UniProtKB: P22607] There should be some charts here, you may need to enable JavaScript!
fibroblast growth factor receptor 4/Fibroblast growth factor receptor 4 in Human [ChEMBL: CHEMBL3973] [GtoPdb: 1811] [UniProtKB: P22455] There should be some charts here, you may need to enable JavaScript!
MET proto-oncogene, receptor tyrosine kinase/Hepatocyte growth factor receptor in Human [ChEMBL: CHEMBL3717] [GtoPdb: 1815] [UniProtKB: P08581] There should be some charts here, you may need to enable JavaScript!
Insulin receptor in Human [ChEMBL: CHEMBL1981] [GtoPdb: 1800] [UniProtKB: P06213] There should be some charts here, you may need to enable JavaScript!
platelet derived growth factor receptor alpha/Platelet-derived growth factor receptor alpha in Human [ChEMBL: CHEMBL2007] [GtoPdb: 1803] [UniProtKB: P16234] There should be some charts here, you may need to enable JavaScript!
platelet derived growth factor receptor beta/Platelet-derived growth factor receptor beta in Human [ChEMBL: CHEMBL1913] [GtoPdb: 1804] [UniProtKB: P09619] There should be some charts here, you may need to enable JavaScript!
aurora kinase A/Serine/threonine-protein kinase Aurora-A in Human [ChEMBL: CHEMBL4722] [GtoPdb: 1936] [UniProtKB: O14965] There should be some charts here, you may need to enable JavaScript!
B-Raf proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase B-raf in Human [ChEMBL: CHEMBL5145] [GtoPdb: 1943] [UniProtKB: P15056] There should be some charts here, you may need to enable JavaScript!
KIT proto-oncogene, receptor tyrosine kinase/Stem cell growth factor receptor in Human [ChEMBL: CHEMBL1936] [GtoPdb: 1805] [UniProtKB: P10721] There should be some charts here, you may need to enable JavaScript!
ABL proto-oncogene 1, non-receptor tyrosine kinase/Tyrosine-protein kinase ABL in Human [ChEMBL: CHEMBL1862] [GtoPdb: 1923] [UniProtKB: P00519] There should be some charts here, you may need to enable JavaScript!
Janus kinase 1/Tyrosine-protein kinase JAK1 in Human [ChEMBL: CHEMBL2835] [GtoPdb: 2047] [UniProtKB: P23458] There should be some charts here, you may need to enable JavaScript!
Janus kinase 2/Tyrosine-protein kinase JAK2 in Human [ChEMBL: CHEMBL2971] [GtoPdb: 2048] [UniProtKB: O60674] There should be some charts here, you may need to enable JavaScript!
Janus kinase 3/Tyrosine-protein kinase JAK3 in Human [ChEMBL: CHEMBL2148] [GtoPdb: 2049] [UniProtKB: P52333] There should be some charts here, you may need to enable JavaScript!
LYN proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase Lyn in Human [ChEMBL: CHEMBL3905] [GtoPdb: 2060] [UniProtKB: P07948] There should be some charts here, you may need to enable JavaScript!
fms related receptor tyrosine kinase 3/Tyrosine-protein kinase receptor FLT3 in Human [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888] There should be some charts here, you may need to enable JavaScript!
ret proto-oncogene/Tyrosine-protein kinase receptor RET in Human [ChEMBL: CHEMBL2041] [GtoPdb: 2185] [UniProtKB: P07949] There should be some charts here, you may need to enable JavaScript!
SRC proto-oncogene, non-receptor tyrosine kinase/Tyrosine-protein kinase SRC in Human [ChEMBL: CHEMBL267] [GtoPdb: 2206] [UniProtKB: P12931] There should be some charts here, you may need to enable JavaScript!
TEK receptor tyrosine kinase/Tyrosine-protein kinase TIE-2 in Human [ChEMBL: CHEMBL4128] [GtoPdb: 1842] [UniProtKB: Q02763] There should be some charts here, you may need to enable JavaScript!
fms related receptor tyrosine kinase 1/Vascular endothelial growth factor receptor 1 in Human [ChEMBL: CHEMBL1868] [GtoPdb: 1812] [UniProtKB: P17948] There should be some charts here, you may need to enable JavaScript!
kinase insert domain receptor/Vascular endothelial growth factor receptor 2 in Human [ChEMBL: CHEMBL279] [GtoPdb: 1813] [UniProtKB: P35968] There should be some charts here, you may need to enable JavaScript!
fms related receptor tyrosine kinase 4/Vascular endothelial growth factor receptor 3 in Human [ChEMBL: CHEMBL1955] [GtoPdb: 1814] [UniProtKB: P35916] There should be some charts here, you may need to enable JavaScript!

DB	Assay description	Assay Type	Standard value	Standard parameter	Original value	Original units	Original parameter	Reference
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]