RGS4 inhibitor 11b [Ligand Id: 8033] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL24773
  • glycogen synthase kinase 3 beta/Glycogen synthase kinase-3 beta in Human [ChEMBL: CHEMBL262] [GtoPdb: 2030] [UniProtKB: P49841]
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  • regulator of G-protein signaling 4/Regulator of G-protein signaling 4 in Human [ChEMBL: CHEMBL1795091] [GtoPdb: 2811] [UniProtKB: P49798]
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  • regulator of G-protein signaling 8/Regulator of G-protein signaling 8 in Human [ChEMBL: CHEMBL2034803] [GtoPdb: 2813] [UniProtKB: P57771]
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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]
ChEMBL Inhibitory activity against recombinant rabbit Glycogen synthase kinase-3 beta B 4.15 pIC50 70000 nM IC50 J Med Chem (2002) 45: 1292-1299 [PMID:11881998]
ChEMBL Inhibition of GSK3beta B 4.15 pIC50 70000 nM IC50 ACS Med Chem Lett (2012) 3: 146-150 [PMID:22368763]
regulator of G-protein signaling 4/Regulator of G-protein signaling 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795091] [GtoPdb: 2811] [UniProtKB: P49798]
GtoPdb Inhibition of Gαo binding - 7.84 pIC50 14.4 nM IC50 ACS Med Chem Lett (2012) 3: 146-150 [PMID:22368763]
ChEMBL Inhibition of RGS4 interaction with Galpha0 protein by flow cytometry protein interaction assay B 7.84 pIC50 14.4 nM IC50 ACS Med Chem Lett (2012) 3: 146-150 [PMID:22368763]
regulator of G-protein signaling 8/Regulator of G-protein signaling 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2034803] [GtoPdb: 2813] [UniProtKB: P57771]
ChEMBL Inhibition of RGS8 interaction with Galpha0 protein by flow cytometry protein interaction assay B 4.08 pIC50 83500 nM IC50 ACS Med Chem Lett (2012) 3: 146-150 [PMID:22368763]
GtoPdb Inhibition of Gαo binding - 4.08 pIC50 83500 nM IC50 ACS Med Chem Lett (2012) 3: 146-150 [PMID:22368763]

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]