GSK2334470 [Ligand Id: 8008] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1765740 (GSK2334470) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| 3-phosphoinositide dependent protein kinase 1/3-phosphoinositide dependent protein kinase-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2534] [GtoPdb: 1519] [UniProtKB: O15530] | ||||||||
| ChEMBL | Inhibition of PDK1-mediated RSK phosphorylation at Ser221 residue in human PC3 cells by ELISA | B | 6.53 | pIC50 | 293 | nM | IC50 | J Med Chem (2011) 54: 1871-1895 [PMID:21341675] |
| ChEMBL | Inhibition of PDK1-mediated AKT phosphorylation at Thr308 residue in human PC3 cells by ELISA | B | 6.95 | pIC50 | 113 | nM | IC50 | J Med Chem (2011) 54: 1871-1895 [PMID:21341675] |
| ChEMBL | Inhibition of recombinant full length PDK1 (unknown origin) expressed in insect cells assessed as inhibition of Akt activation measured for 30 mins in presence of [gamma32P-ATP] | B | 8 | pIC50 | 10 | nM | IC50 | J Med Chem (2013) 56: 2726-2737 [PMID:23448267] |
| ChEMBL | Inhibition of recombinant human His-tagged PDK1 catalytic domain using Ac-Sox-PKTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIAD-NH2 as substrate by fluorescence-based spectrophotometry | B | 8 | pIC50 | 10 | nM | IC50 | J Med Chem (2011) 54: 8490-8500 [PMID:22040023] |
| ChEMBL | Inhibition of PDK1 | B | 8.6 | pIC50 | 2.51 | nM | IC50 | J Med Chem (2011) 54: 1871-1895 [PMID:21341675] |
| GtoPdb | - | - | 8.6 | pIC50 | 2.51 | nM | IC50 | J Med Chem (2011) 54: 1871-95 [PMID:21341675] |
| ChEMBL | Inhibition of PDK1 | B | 8.6 | pIC50 | 2.5 | nM | IC50 | J Med Chem (2011) 54: 1871-1895 [PMID:21341675] |
| ChEMBL | Inhibition of PDK1 (unknown origin) | B | 8.6 | pIC50 | 2.5 | nM | IC50 | Eur J Med Chem (2016) 118: 47-63 [PMID:27123901] |
| 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 | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2011) 54: 1871-1895 [PMID:21341675] |
| glycogen synthase kinase 3 beta/Glycogen synthase kinase-3 beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL262] [GtoPdb: 2030] [UniProtKB: P49841] | ||||||||
| ChEMBL | Inhibition of GSK3B | B | 4.6 | pIC50 | >25118 | nM | IC50 | J Med Chem (2011) 54: 1871-1895 [PMID:21341675] |
| component of inhibitor of nuclear factor kappa B kinase complex/Inhibitor of nuclear factor kappa B kinase alpha subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3476] [GtoPdb: 1989] [UniProtKB: O15111] | ||||||||
| ChEMBL | Inhibition of IKK1 | B | 4.6 | pIC50 | >25118 | nM | IC50 | J Med Chem (2011) 54: 1871-1895 [PMID:21341675] |
| mitogen-activated protein kinase kinase kinase 5/Mitogen-activated protein kinase kinase kinase 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5285] [GtoPdb: 2080] [UniProtKB: Q99683] | ||||||||
| ChEMBL | Inhibition of ASK1 | B | 4.56 | pIC50 | >27542 | nM | IC50 | J Med Chem (2011) 54: 1871-1895 [PMID:21341675] |
| phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma/PI3-kinase p110-gamma subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3267] [GtoPdb: 2156] [UniProtKB: P48736] | ||||||||
| ChEMBL | Inhibition of PI3Kgamma | B | 4.6 | pIC50 | 25118 | nM | IC50 | J Med Chem (2011) 54: 1871-1895 [PMID:21341675] |
| Rho associated coiled-coil containing protein kinase 1/Rho-associated protein kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3231] [GtoPdb: 1503] [UniProtKB: Q13464] | ||||||||
| ChEMBL | Inhibition of ROCK1 | B | 5.1 | pIC50 | 7943.28 | nM | IC50 | J Med Chem (2011) 54: 1871-1895 [PMID:21341675] |
| ChEMBL | Inhibition of ROCK1 | B | 5.1 | pIC50 | 7943 | nM | IC50 | J Med Chem (2011) 54: 1871-1895 [PMID:21341675] |
| AKT serine/threonine kinase 1/Serine/threonine-protein kinase AKT in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4282] [GtoPdb: 1479] [UniProtKB: P31749] | ||||||||
| ChEMBL | Inhibition of AKT1 | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2011) 54: 1871-1895 [PMID:21341675] |
| aurora kinase A/Serine/threonine-protein kinase Aurora-A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4722] [GtoPdb: 1936] [UniProtKB: O14965] | ||||||||
| ChEMBL | Inhibition of aurora A | B | 4.4 | pIC50 | 39810 | nM | IC50 | J Med Chem (2011) 54: 1871-1895 [PMID:21341675] |
| GtoPdb | - | - | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2011) 54: 1871-95 [PMID:21341675] |
| ChEMBL | Inhibition of aurora A | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2011) 54: 1871-1895 [PMID:21341675] |
| aurora kinase B/Serine/threonine-protein kinase Aurora-B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2185] [GtoPdb: 1937] [UniProtKB: Q96GD4] | ||||||||
| ChEMBL | Inhibition of aurora B | B | 5.5 | pIC50 | 3162.28 | nM | IC50 | J Med Chem (2011) 54: 1871-1895 [PMID:21341675] |
| GtoPdb | - | - | 5.5 | pIC50 | 3160 | nM | IC50 | J Med Chem (2011) 54: 1871-95 [PMID:21341675] |
| ChEMBL | Inhibition of aurora B | B | 5.5 | pIC50 | 3162 | nM | IC50 | J Med Chem (2011) 54: 1871-1895 [PMID:21341675] |
| transforming growth factor beta receptor 1/TGF-beta receptor type I in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4439] [GtoPdb: 1788] [UniProtKB: P36897] | ||||||||
| ChEMBL | Inhibition of ALK5 | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2011) 54: 1871-1895 [PMID:21341675] |
| ChEMBL | Inhibition of ALK5 | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2011) 54: 1871-1895 [PMID:21341675] |
| spleen associated tyrosine kinase/Tyrosine-protein kinase SYK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2599] [GtoPdb: 2230] [UniProtKB: P43405] | ||||||||
| ChEMBL | Inhibition of SYK | B | 4.6 | pIC50 | >25118 | nM | IC50 | J Med Chem (2011) 54: 1871-1895 [PMID:21341675] |
| 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 VEGFR2 | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2011) 54: 1871-1895 [PMID:21341675] |
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]
