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 | Affinity Phenotypic Cellular interaction (ELISA (phosphorylation of Thr308-AKT (PI3K-dependent) in PC-3 cells)) EUB0000153b PDPK1 | B | 6.95 | pIC50 | 113 | nM | IC50 | Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomics Library wave 3 |
| 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 (unknown origin) | B | 8.6 | pIC50 | 2.5 | nM | IC50 | Eur J Med Chem (2016) 118: 47-63 [PMID:27123901] |
| ChEMBL | Inhibition of PDK1 | B | 8.6 | pIC50 | 2.5 | nM | IC50 | J Med Chem (2011) 54: 1871-1895 [PMID:21341675] |
| ChEMBL | Affinity Biochemical interaction (Enzymatic inhibition assay) EUB0000153b PDPK1 | B | 8.6 | pIC50 | 2.5 | nM | IC50 | Affinity Biochemical Literature for EUbOPEN Chemogenomics Library wave 3 |
| 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] |
| ChEMBL | Selectivity interaction (Kinase panel (enzymatic assay)) EUB0000153b EGFR | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomics Library wave 3 |
| 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] |
| ChEMBL | Selectivity interaction (Kinase panel (enzymatic assay)) EUB0000153b GSK3B | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomics Library wave 3 |
| 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] |
| ChEMBL | Selectivity interaction (Kinase panel (enzymatic assay)) EUB0000153b CHUK | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomics Library wave 3 |
| 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] |
| ChEMBL | Selectivity interaction (Kinase panel (enzymatic assay)) EUB0000153b MAP3K5 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomics Library wave 3 |
| 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] |
| ChEMBL | Selectivity interaction (Kinase panel (enzymatic assay)) EUB0000153b PIK3CG | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomics Library wave 3 |
| pyruvate dehydrogenase kinase 1/Pyruvate dehydrogenase kinase isoform 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4766] [GtoPdb: 2915] [UniProtKB: Q15118] | ||||||||
| ChEMBL | Inhibition of PDK1 (unknown origin) | B | 8 | pIC50 | 10 | nM | IC50 | Eur J Med Chem (2023) 246: 114971-114971 [PMID:36462440] |
| ChEMBL | Selectivity interaction (Kinase panel (enzymatic assay)) EUB0000153b PDK1 | B | 8.6 | pIC50 | 2.5 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomics Library wave 3 |
| 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] |
| ChEMBL | Selectivity interaction (Kinase panel (enzymatic assay)) EUB0000153b ROCK1 | B | 5.1 | pIC50 | 7943 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomics Library wave 3 |
| 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] |
| ChEMBL | Selectivity interaction (Kinase panel (enzymatic assay)) EUB0000153b AKT1 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomics Library wave 3 |
| 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] |
| ChEMBL | Selectivity interaction (Kinase panel (enzymatic assay)) EUB0000153b STK6 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomics Library wave 3 |
| 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] |
| ChEMBL | Selectivity interaction (Kinase panel (enzymatic assay)) EUB0000153b AURKB | B | 5.5 | pIC50 | 3162 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomics Library wave 3 |
| 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] |
| ChEMBL | Selectivity interaction (Kinase panel (enzymatic assay)) EUB0000153b TGFBR1 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomics Library wave 3 |
| 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] |
| ChEMBL | Selectivity interaction (Kinase panel (enzymatic assay)) EUB0000153b SYK | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomics Library wave 3 |
| 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 | Selectivity interaction (Kinase panel (enzymatic assay)) EUB0000153b KDR | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomics Library wave 3 |
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]
