GSK2830371 [Ligand Id: 11103] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3613749
  • protein phosphatase, Mg2+/Mn2+ dependent 1D/Protein phosphatase 1D in Human [ChEMBL: CHEMBL1938224] [GtoPdb: 3134] [UniProtKB: O15297]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
protein phosphatase, Mg2+/Mn2+ dependent 1D/Protein phosphatase 1D in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1938224] [GtoPdb: 3134] [UniProtKB: O15297]
ChEMBL Inhibition of His-tagged PPM1D (1 to 420 residues) (unknown origin) expressed in Escherichia coli BL21 (DE3) pLysS cells using Ac-VEPPLS(P)QETFSDLW-NH2 substrate B 7.06 pIC50 86.3 nM IC50 Bioorg Med Chem (2015) 23: 6246-6249 [PMID:26358280]
GtoPdb Inhibition of PPM1D phosphatase activity determined using recombinant His-PPM1D(1-420) and a phosphorylated peptide derived from p53 as the substrate. - 7.07 pIC50 86 nM IC50 Bioorg Med Chem (2015) 23: 6246-9 [PMID:26358280]
GtoPdb Inhibition of dephosphorylation of Thr180 of the endogenous substrate phospho-p38 MAPK in vitro. - 7.89 pIC50 13 nM IC50 Nat Chem Biol (2014) 10: 181-7 [PMID:24390428]
ChEMBL Inhibition of human Wip1 (2 to 420 residues) expressed in baculovirus-infected insect SF9 cells assessed as fluorescein diphosphate hydrolysis after 5 mins by fluorescence assay B 8.22 pIC50 6 nM IC50 J Med Chem (2016) 59: 6629-6644 [PMID:26914744]
ChEMBL Allosteric inhibition of human Wip1 (2 to 420 residues) expressed in baculovirus infected sf9 cells using FDP as substrate by fluorescence method B 8.22 pIC50 6 nM IC50 J Med Chem (2020) 63: 11368-11396 [PMID:32460492]

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]