compound 8h [PMID: 22765894] | Ligand Activity Charts

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compound 8h [PMID: 22765894]
Ligand Activity Charts

compound 8h [PMID: 22765894] [Ligand Id: 8175] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2086760
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 B4/Ephrin type-B receptor 4 in Human [ChEMBL: CHEMBL5147] [GtoPdb: 1833] [UniProtKB: P54760] 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!
K_v11.1/HERG in Human [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] There should be some charts here, you may need to enable JavaScript!
Insulin-like growth factor I receptor in Human [ChEMBL: CHEMBL1957] [GtoPdb: 1801] [UniProtKB: P08069] 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!
mitogen-activated protein kinase kinase kinase kinase 3/Mitogen-activated protein kinase kinase kinase kinase 3 in Human [ChEMBL: CHEMBL5432] [GtoPdb: 2087] [UniProtKB: Q8IVH8] 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!
ribosomal protein S6 kinase A3/Ribosomal protein S6 kinase alpha 3 in Human [ChEMBL: CHEMBL2345] [GtoPdb: 1528] [UniProtKB: P51812] 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!
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!
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!
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
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]
K_v11.1/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]