calyculin A [Ligand Id: 13083] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL430266
  • 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, 56 kDa regulatory subunit, alpha isoform in Human [ChEMBL: CHEMBL4763] [UniProtKB: Q15172]
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  • protein phosphatase 2 catalytic subunit alpha/Serine/threonine protein phosphatase 2A, catalytic subunit, alpha isoform in Human [ChEMBL: CHEMBL4703] [GtoPdb: 3263] [UniProtKB: P67775]
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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 6 catalytic subunit in Human [ChEMBL: CHEMBL4105731] [UniProtKB: O00743]
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  • Serine/threonine protein phosphatase PP1-gamma catalytic subunit in Human [ChEMBL: CHEMBL4438] [UniProtKB: P36873]
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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 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 8.92 pIC50 1.2 nM IC50 J Med Chem (1997) 40: 3199-3206 [PMID:9379439]
ChEMBL Inhibitory concentration against Protein phosphatase 1 was determined; 0.5-1.0 B 9.3 pIC50 0.5 nM IC50 Bioorg Med Chem Lett (2002) 12: 391-393 [PMID:11814804]
ChEMBL Tested for inhibition against purified catalytic subunit of protein phosphatase-1 from rabbit skeletal muscle B 9.52 pIC50 0.3 nM IC50 Bioorg Med Chem Lett (1993) 3: 1029-1034
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 9.89 pIC50 0.13 nM IC50 Bioorg Med Chem Lett (1993) 3: 1029-1034
protein phosphatase 2 catalytic subunit alpha/Serine/threonine protein phosphatase 2A, catalytic subunit, alpha isoform in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4703] [GtoPdb: 3263] [UniProtKB: P67775]
GtoPdb - - 8.7 pIC50 2 nM IC50 Bioorg Med Chem Lett (2002) 12: 391-3 [PMID:11814804]
ChEMBL Inhibition of human PP2AC using [3H]-phosphohistone as substrate B 9.6 pIC50 0.25 nM IC50 J Med Chem (2021) 64: 8916-8938 [PMID:34156850]
Serine-threonine protein phosphatase 2A regulatory subunit in Chicken (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2669] [UniProtKB: Q8AWE3]
ChEMBL Observed inhibition activity of the compounds against protein phosphatases 2A (PP2A) B 8.14 pIC50 7.3 nM IC50 J Med Chem (1997) 40: 3199-3206 [PMID:9379439]
ChEMBL Concentration required to inhibit the action of protein phosphatase 2A B 8.7 pIC50 2 nM IC50 Bioorg Med Chem Lett (2002) 12: 391-393 [PMID:11814804]
ChEMBL Exogenous inhibition concentration of Serine/threonine protein phosphatase 2A (PP2A) B 9.7 pIC50 0.2 nM IC50 J Med Chem (2002) 45: 1151-1175 [PMID:11881984]
Serine/threonine-protein phosphatase 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3425389] [UniProtKB: P53041]
ChEMBL Inhibition of human PP5 using [3H]-phosphohistone as substrate B 8.52 pIC50 3 nM IC50 J Med Chem (2021) 64: 8916-8938 [PMID:34156850]
Serine/threonine-protein phosphatase 6 catalytic subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105731] [UniProtKB: O00743]
ChEMBL Inhibition of PP6 (unknown origin) using [3H]-phosphohistone as substrate by liquid scintillation counting analysis B 8 pIC50 10 nM IC50 J Med Chem (2021) 64: 8916-8938 [PMID:34156850]
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 R221S B 6.3 pIC50 >500 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 N124D B 6.3 pIC50 >500 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 6.3 pIC50 >500 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 6.3 pIC50 >500 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 7.24 pIC50 58 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 7.32 pIC50 48 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 8.66 pIC50 2.2 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 9.35 pIC50 0.45 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 9.4 pIC50 0.4 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 9.85 pIC50 0.14 nM IC50 J Med Chem (2002) 45: 1151-1175 [PMID:11881984]
protein phosphatase 1 catalytic subunit alpha in Human [GtoPdb: 3264] [UniProtKB: P62136]
GtoPdb - - 9 pIC50 1 nM IC50 Bioorg Med Chem Lett (2002) 12: 391-3 [PMID:11814804]

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]