chelerythrine [Ligand Id: 5953] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL13045 (Chelerythrine)
  • acetylcholinesterase (Cartwright blood group)/Acetylcholinesterase in Human [ChEMBL: CHEMBL220] [GtoPdb: 2465] [UniProtKB: P22303]
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  • butyrylcholinesterase/Butyrylcholinesterase in Human [ChEMBL: CHEMBL1914] [GtoPdb: 2471] [UniProtKB: P06276]
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  • Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Human [ChEMBL: CHEMBL235] [GtoPdb: 595] [UniProtKB: P37231]
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  • Sarcoplasmic/endoplasmic reticulum calcium ATP-ase in Rabbit [ChEMBL: CHEMBL4693] [UniProtKB: P04191]
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  • SERCA1/Sarcoplasmic/endoplasmic reticulum calcium ATPase 1 in Human [ChEMBL: CHEMBL3136] [GtoPdb: 840] [UniProtKB: O14983]
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  • P2X7 in Human [GtoPdb: 484] [UniProtKB: Q99572]
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  • protein kinase C epsilon in Human [GtoPdb: 1486] [UniProtKB: Q02156]
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  • protein kinase A in Human [GtoPdb: 1694]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
acetylcholinesterase (Cartwright blood group)/Acetylcholinesterase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL220] [GtoPdb: 2465] [UniProtKB: P22303]
ChEMBL Inhibition of AChE (unknown origin) preincubated for 30 mins followed by substrate addition acetylthiocholineiodide measured after 40 mins by Ellman's method B 5.84 pIC50 1450 nM IC50 Eur J Med Chem (2020) 200: 112415-112415 [PMID:32454229]
butyrylcholinesterase/Butyrylcholinesterase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1914] [GtoPdb: 2471] [UniProtKB: P06276]
ChEMBL Inhibition of BuChE (unknown origin) preincubated for 30 mins followed by substrate addition acetylthiocholineiodide measured after 40 mins by Ellman's method B 5.07 pIC50 8580 nM IC50 Eur J Med Chem (2020) 200: 112415-112415 [PMID:32454229]
Monoamine oxidase A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1951] [GtoPdb: 2489] [UniProtKB: P21397]
ChEMBL Competitive inhibition of recombinant human MAO-A using kynuramine as substrate by Lineweaver-Burk plot analysis B 6.66 pKi 220 nM Ki Bioorg Med Chem Lett (2018) 28: 2403-2407 [PMID:29925480]
ChEMBL Inhibition of recombinant human MAO-A using kynuramine as substrate incubated for 20 mins by spectrophotometric method B 6.26 pIC50 550 nM IC50 Bioorg Med Chem Lett (2018) 28: 2403-2407 [PMID:29925480]
Monoamine oxidase B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2039] [GtoPdb: 2490] [UniProtKB: P27338]
ChEMBL Inhibition of recombinant human MAO-B using benzylamine as substrate incubated for 30 mins by spectrophotometric method B 4.7 pIC50 >20000 nM IC50 Bioorg Med Chem Lett (2018) 28: 2403-2407 [PMID:29925480]
Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL235] [GtoPdb: 595] [UniProtKB: P37231]
ChEMBL Binding affinity to human 6xHis-tagged PPARgamma ligand binding domain (206 to 477 residues) by TR-FRET assay B 6.25 pIC50 566 nM IC50 Bioorg Med Chem Lett (2016) 26: 4157-4164 [PMID:27503683]
Sarcoplasmic/endoplasmic reticulum calcium ATP-ase in Rabbit (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4693] [UniProtKB: P04191]
ChEMBL Inhibition of rabbit skeletal muscle microsomes SERCA1a incubated for 10 mins by enzyme-coupled method B 5.92 pIC50 1200 nM IC50 J Med Chem (2020) 63: 1937-1963 [PMID:32030976]
SERCA1/Sarcoplasmic/endoplasmic reticulum calcium ATPase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3136] [GtoPdb: 840] [UniProtKB: O14983]
ChEMBL Inhibition of SERCA1a (unknown origin) incubated for 10 mins by enzyme-coupled method B 4.57 pIC50 27000 nM IC50 J Med Chem (2020) 63: 1937-1963 [PMID:32030976]
P2X7 in Human [GtoPdb: 484] [UniProtKB: Q99572]
GtoPdb Inhibition of ATP-induced 86Rb+ (K+) efflux in human B-lymphocytes - 5.25 pIC50 5600 nM IC50 Br J Pharmacol (2004) 142: 1015-9 [PMID:15210579]
protein kinase C epsilon in Human [GtoPdb: 1486] [UniProtKB: Q02156]
GtoPdb - - 7.62 pIC50 24 nM IC50 Proc Natl Acad Sci USA (2007) 104: 20523-8 [PMID:18077363]
protein kinase A in Human [GtoPdb: 1694]
GtoPdb - - 6.05 pIC50 900 nM IC50 Proc Natl Acad Sci USA (2007) 104: 20523-8 [PMID:18077363]

ChEMBL data shown on this page come from version 31:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]