AZD2858 [Ligand Id: 8478] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2177161
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  • glycogen synthase kinase 3 beta/Glycogen synthase kinase-3 beta in Human [ChEMBL: CHEMBL262] [GtoPdb: 2030] [UniProtKB: P49841]
  • glycogen synthase kinase 3 beta/Glycogen synthase kinase-3 beta in Mouse [ChEMBL: CHEMBL1075321] [GtoPdb: 2030] [UniProtKB: Q9WV60]
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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: O96020P24864P24941]
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]
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 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]