GSK-3beta inhibitor I [Ligand Id: 5977] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL284861
  • casein kinase 2, alpha prime polypeptide subunit/casein kinase 2, beta polypeptide subunit/casein kinase 2, alpha 1 polypeptide subunit/Casein kinase II in Human [ChEMBL: CHEMBL2095191] [GtoPdb: 1550, 1551, 1549] [UniProtKB: P19784, P67870, P68400]
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  • glycogen synthase kinase 3 beta/Glycogen synthase kinase-3 beta in Human [ChEMBL: CHEMBL262] [GtoPdb: 2030] [UniProtKB: P49841]
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  • CoV Replicase polyprotein 1ab/CoV RNA-dependent RNA polymerase/CoV Non-structural protein 15/CoV Non-structural protein 13/Replicase polyprotein 1ab in Severe acute respiratory syndrome coronavirus 2 [ChEMBL: CHEMBL4523582] [GtoPdb: 3125, 3139, 3206, 3261] [UniProtKB: P0DTD1]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
casein kinase 2, alpha prime polypeptide subunit/casein kinase 2, beta polypeptide subunit/casein kinase 2, alpha 1 polypeptide subunit/Casein kinase II in Human (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2095191] [GtoPdb: 1550, 1551, 1549] [UniProtKB: P19784, P67870, P68400]
ChEMBL Inhibition of Casein kinase II (CK II) from purified bovine brain B 4 pIC50 >100000 nM IC50 J Med Chem (2002) 45: 1292-1299 [PMID:11881998]
cyclin dependent kinase 1/Cyclin-dependent kinase 1/cyclin B in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094127] [GtoPdb: 1961] [UniProtKB: O95067, P06493, P14635, Q8WWL7]
ChEMBL Inhibition of Cyclin dependent kinase 1-cyclinB B 4 pIC50 >100000 nM IC50 J Med Chem (2002) 45: 1292-1299 [PMID:11881998]
ChEMBL Inhibition of CDK1/cyclinB B 5 pIC50 10000 nM IC50 Trends Pharmacol Sci (2004) 25: 471-480 [PMID:15559249]
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 Glycogen synthase kinase-3 beta B 4 pIC50 >100000 nM IC50 J Med Chem (2002) 45: 1292-1299 [PMID:11881998]
ChEMBL Inhibition of GSK3-beta B 5.7 pIC50 2000 nM IC50 Trends Pharmacol Sci (2004) 25: 471-480 [PMID:15559249]
ChEMBL Inhibitory activity against recombinant rabbit Glycogen synthase kinase-3 beta B 5.7 pIC50 2000 nM IC50 J Med Chem (2002) 45: 1292-1299 [PMID:11881998]
ChEMBL Non-competitive inhibition of human GSK-3beta in presence of ATP B 5.7 pIC50 2000 nM IC50 J Med Chem (2015) 58: 8920-8937 [PMID:26486317]
ChEMBL Inhibition of GSK3beta (unknown origin) B 5.7 pIC50 2000 nM IC50 Eur J Med Chem (2021) 210: 112949-112949 [PMID:33097303]
ChEMBL Inhibition of human recombinant GSK3beta expressed in Escherichia coli using GS-1 as substrate incubated for 20 mins by gamma[32P]ATP-based scintillation counting analysis B 5.82 pIC50 1500 nM IC50 Eur J Med Chem (2016) 116: 281-289 [PMID:27131621]
GtoPdb - - 5.85 pIC50 1400 nM IC50 Bioorg Med Chem Lett (2012) 22: 7232-6 [PMID:23099099]
ChEMBL Inhibition of recombinant human GSK-3beta using GS-2 peptide as substrate incubated for 30 mins in presence of ATP by kinase-glo luminescence assay B 5.85 pIC50 1400 nM IC50 J Med Chem (2021) 64: 7341-7358 [PMID:34027661]
ChEMBL Inhibition of recombinant N-terminal His6-tagged human GSK3beta H350L mutant expressed in baculovirus infected Sf21 insect cells using polypeptide GS-2 as substrate after 30 mins in presence of ATP by kinase-glo luminescence assay B 5.85 pIC50 1400 nM IC50 Eur J Med Chem (2017) 135: 370-381 [PMID:28460311]
ChEMBL Inhibition of GSK3beta by kinase-glo assay method B 5.85 pIC50 1400 nM IC50 Bioorg Med Chem Lett (2012) 22: 7232-7236 [PMID:23099099]
ChEMBL Inhibition of human recombinant GSK3beta using 650HSSPHQ(pS)EDEEE as substrate after 30 mins by luminescence assay B 5.85 pIC50 1400 nM IC50 Eur J Med Chem (2013) 61: 95-103 [PMID:23047001]
ChEMBL Inhibition of GSK3beta (unknown origin) using GS-2 peptide substrate incubated for 30 mins by kinase-Glo luminescent assay B 6.16 pIC50 690 nM IC50 J Med Chem (2018) 61: 7640-7656 [PMID:30078314]
CoV Replicase polyprotein 1ab/CoV RNA-dependent RNA polymerase/CoV Non-structural protein 15/CoV Non-structural protein 13/Replicase polyprotein 1ab in Severe acute respiratory syndrome coronavirus 2 (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523582] [GtoPdb: 3125, 3139, 3206, 3261] [UniProtKB: P0DTD1]
ChEMBL SARS-CoV-2 3CL-Pro protease inhibition IC50 determined by FRET kind of response from peptide substrate F 6.85 pIC50 140 nM IC50 Identification of inhibitors of SARS-Cov2 M-Pro enzymatic activity using a small molecule repurposing screen

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]