microcystin-LR [Ligand Id: 4735] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL444092
  • Protein phosphatase 2C alpha in Human [ChEMBL: CHEMBL2437] [UniProtKB: P35813]
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  • protein tyrosine phosphatase non-receptor type 1/Protein-tyrosine phosphatase 1B in Human [ChEMBL: CHEMBL335] [GtoPdb: 2976] [UniProtKB: P18031]
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  • Serine/threonine protein phosphatase 2A, 55 kDa regulatory subunit B, alpha isoform in Human [ChEMBL: CHEMBL4284] [UniProtKB: P63151]
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  • Serine/threonine protein phosphatase 2A, 56 kDa regulatory subunit, alpha isoform in Human [ChEMBL: CHEMBL4763] [UniProtKB: Q15172]
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  • Serine-threonine protein phosphatase 2A regulatory subunit in Chicken [ChEMBL: CHEMBL2669] [UniProtKB: Q8AWE3]
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  • Serine/threonine protein phosphatase PP1-gamma catalytic subunit in Human [ChEMBL: CHEMBL4438] [UniProtKB: P36873]
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  • protein phosphatase 2 catalytic subunit alpha in Human [GtoPdb: 3263] [UniProtKB: P67775]
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  • protein phosphatase 1 catalytic subunit alpha in Human [GtoPdb: 3264] [UniProtKB: P62136]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Protein phosphatase 2C alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2437] [UniProtKB: P35813]
ChEMBL Inhibitory concentration required against protein phosphatase 1 using pNPP assay B 8.52 pIC50 3 nM IC50 Bioorg Med Chem Lett (2003) 13: 2903-2906 [PMID:14611854]
protein tyrosine phosphatase non-receptor type 1/Protein-tyrosine phosphatase 1B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL335] [GtoPdb: 2976] [UniProtKB: P18031]
ChEMBL Observed inhibition activity of the compounds against protein phosphatases 1 (PP1) B 8.93 pIC50 1.17 nM IC50 J Med Chem (1997) 40: 3199-3206 [PMID:9379439]
ChEMBL Tested for inhibition against purified catalytic subunit of protein phosphatase-1 from rabbit skeletal muscle B 10 pIC50 0.1 nM IC50 Bioorg Med Chem Lett (1993) 3: 1029-1034
Serine/threonine protein phosphatase 2A, 55 kDa regulatory subunit B, alpha isoform in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4284] [UniProtKB: P63151]
ChEMBL Observed inhibition activity of the compounds against protein phosphatases 2A (PP2A) B 10.19 pIC50 0.07 nM IC50 J Med Chem (1997) 40: 3199-3206 [PMID:9379439]
Serine/threonine protein phosphatase 2A, 56 kDa regulatory subunit, alpha isoform in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4763] [UniProtKB: Q15172]
ChEMBL Tested for inhibition of purified catalytic subunit of protein phosphatase-2A from human erythrocytes B 10 pIC50 0.1 nM IC50 Bioorg Med Chem Lett (1993) 3: 1029-1034
Serine-threonine protein phosphatase 2A regulatory subunit in Chicken (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2669] [UniProtKB: Q8AWE3]
ChEMBL Inhibitory concentration required against protein phosphatase 2A using pNPP assay B 8.52 pIC50 3 nM IC50 Bioorg Med Chem Lett (2003) 13: 2903-2906 [PMID:14611854]
ChEMBL Exogenous inhibition concentration of Serine/threonine protein phosphatase 2A (PP2A) B 10 pIC50 0.1 nM IC50 J Med Chem (2002) 45: 1151-1175 [PMID:11881984]
Serine/threonine protein phosphatase PP1-gamma catalytic subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4438] [UniProtKB: P36873]
ChEMBL Inhibition of Serine/threonine protein phosphatase 1 (PP1) mutants by natural toxins in N124D B 6.7 pIC50 200 nM IC50 J Med Chem (2002) 45: 1151-1175 [PMID:11881984]
ChEMBL Inhibition of Serine/threonine protein phosphatase 1 (PP1) mutants by natural toxins in H248N B 7.46 pIC50 35 nM IC50 J Med Chem (2002) 45: 1151-1175 [PMID:11881984]
ChEMBL Inhibition of Serine/threonine protein phosphatase 1 (PP1) mutants by natural toxins in R96A B 7.46 pIC50 35 nM IC50 J Med Chem (2002) 45: 1151-1175 [PMID:11881984]
ChEMBL Inhibition of Serine/threonine protein phosphatase 1 9PP1) mutants by natural toxins in R221S B 7.54 pIC50 29 nM IC50 J Med Chem (2002) 45: 1151-1175 [PMID:11881984]
ChEMBL Inhibition of Serine/threonine protein phosphatase 1 (PP1) mutants by natural toxins in D208A B 8.72 pIC50 1.9 nM IC50 J Med Chem (2002) 45: 1151-1175 [PMID:11881984]
ChEMBL Inhibition of Serine/threonine protein phosphatase 1 (PP1) mutants by natural toxins in Y272F B 9.1 pIC50 0.8 nM IC50 J Med Chem (2002) 45: 1151-1175 [PMID:11881984]
ChEMBL Inhibition of Serine/threonine protein phosphatase 1 (PP1) mutants by natural toxins in C127S B 9.25 pIC50 0.56 nM IC50 J Med Chem (2002) 45: 1151-1175 [PMID:11881984]
ChEMBL Inhibition of Serine/threonine protein phosphatase 1 (PP1) mutants by natural toxins in wild type B 10.7 pIC50 0.02 nM IC50 J Med Chem (2002) 45: 1151-1175 [PMID:11881984]
ChEMBL Inhibition of Serine/threonine protein phosphatase 1 (PP1) mutants by natural toxins in D220V B 10.7 pIC50 0.02 nM IC50 J Med Chem (2002) 45: 1151-1175 [PMID:11881984]
ChEMBL Inhibition of Serine/threonine protein phosphatase 1 (PP1) mutants by natural toxins in E275R B 11 pIC50 0.01 nM IC50 J Med Chem (2002) 45: 1151-1175 [PMID:11881984]
protein phosphatase 2 catalytic subunit alpha in Human [GtoPdb: 3263] [UniProtKB: P67775]
GtoPdb - - 10 pIC50 0.1 nM IC50 Br J Pharmacol (2022) 179: 65-83 [PMID:34519023]
protein phosphatase 1 catalytic subunit alpha in Human [GtoPdb: 3264] [UniProtKB: P62136]
GtoPdb - - 10 pIC50 0.1 nM IC50 Bioorg Med Chem (1997) 5: 1739-50 [PMID:9354230]

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]