TWS119 [Ligand Id: 5980] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL405759 (TWS-119)
  • 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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  • eukaryotic translation initiation factor 2 alpha kinase 2/Interferon-induced, double-stranded RNA-activated protein kinase in Human [ChEMBL: CHEMBL5785] [GtoPdb: 2016] [UniProtKB: P19525]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
glycogen synthase kinase 3 beta/Glycogen synthase kinase-3 beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL262] [GtoPdb: 2030] [UniProtKB: P49841]
GtoPdb - - 7.52 pIC50 30 nM IC50 Proc Natl Acad Sci USA (2003) 100: 7632-7 [PMID:12794184]
ChEMBL Inhibition of GSK3-beta B 7.52 pIC50 30 nM IC50 Trends Pharmacol Sci (2004) 25: 471-480 [PMID:15559249]
ChEMBL Inhibition of Glycogen synthase kinase-3 beta (unknown origin) B 7.52 pIC50 30 nM IC50 Eur J Med Chem (2019) 164: 448-470 [PMID:30616053]
ChEMBL Inhibition of GSK3beta (unknown origin) B 7.52 pIC50 30 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 GSK-3 beta in mouse D3 cells B 6.9 pKd 126 nM Kd Nat Chem Biol (2005) 1: 74-84 [PMID:16408003]
ChEMBL Binding affinity to GSK-3 beta in mouse D3 cells B 7.52 pIC50 30 nM IC50 Nat Chem Biol (2005) 1: 74-84 [PMID:16408003]
ChEMBL Inhibition of GSK-3 beta in mouse D3 cells assessed as induction of neuron specific marker microtubule-associated protein 2 by immunofluorescence method B 6 pEC50 1000 nM EC50 Nat Chem Biol (2005) 1: 74-84 [PMID:16408003]
ChEMBL Inhibition of GSK-3 beta in mouse D3 cells assessed as induction of neuron specific marker neurofilament-M by immunofluorescence method B 6 pEC50 1000 nM EC50 Nat Chem Biol (2005) 1: 74-84 [PMID:16408003]
ChEMBL Inhibition of GSK-3 beta in mouse D3 cells assessed as induction of neuron specific marker beta3-tubulin by immunofluorescence method B 6 pEC50 1000 nM EC50 Nat Chem Biol (2005) 1: 74-84 [PMID:16408003]
eukaryotic translation initiation factor 2 alpha kinase 2/Interferon-induced, double-stranded RNA-activated protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5785] [GtoPdb: 2016] [UniProtKB: P19525]
ChEMBL Inhibition of human recombinant PKR autophosphorylation using poly[I:C] after 10 mins by luminescent assay B 5.4 pIC50 4000 nM IC50 Bioorg Med Chem Lett (2011) 21: 4108-4114 [PMID:21632247]

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]