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 GSK-3beta (unknown origin) using GS-1 as substrate incubated for 20 mins B 5.7 pIC50 2000 nM IC50 Eur J Med Chem (2022) 236: 114301-114301 [PMID:35390715]
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 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 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 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 Inhibition of SARS-COV2 main protease using Mca-AVLQ-SGFR-K as substrate by Fluorescence microplate reader assay B 5.6 pIC50 2500 nM IC50 Eur J Med Chem (2021) 213: 113157-113157 [PMID:33486200]
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 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]