AZD2858 [Ligand Id: 8478] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL2177161 |
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| 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 E in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094126] [GtoPdb: 1973] [UniProtKB: O96020, P24864, P24941] | ||||||||
| ChEMBL | Inhibition of CDK2/cyclin E expressed in baculovirus infected insect cells using [gamma33P]ATP after 60 mins by scintillation proximity assay | B | 6.27 | pKi | 540 | nM | Ki | J Med Chem (2012) 55: 9107-9119 [PMID:22489897] |
| 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 human recombinant GSK3beta using biotin- AAEELDSRAGS(PO3H2)PQL as substrate and [gamma32P]ATP after 20 mins by scintillation proximity assay | B | 8.31 | pKi | 4.9 | nM | Ki | J Med Chem (2012) 55: 9107-9119 [PMID:22489897] |
| GtoPdb | - | - | 8.31 | pKi | 4.9 | nM | Ki | J Med Chem (2012) 55: 9107-19 [PMID:22489897] |
| ChEMBL | Inhibition of GSK3beta (unknown origin) | B | 8.3 | pIC50 | 5 | nM | IC50 | Eur J Med Chem (2021) 210: 112949-112949 [PMID:33097303] |
| glycogen synthase kinase 3 beta/Glycogen synthase kinase-3 beta in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075321] [GtoPdb: 2030] [UniProtKB: Q9WV60] | ||||||||
| ChEMBL | Inhibition of GSK3beta-mediated Tau phosphorylation in mouse 3T3 cells after 4 hrs by Western blot analysis | B | 7.12 | pIC50 | 76 | nM | IC50 | J Med Chem (2012) 55: 9107-9119 [PMID:22489897] |
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]
