chelerythrine [Ligand Id: 5953] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL13045 (Chelerythrine) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| acetylcholinesterase (Yt 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] |
| ChEMBL | Agonist activity at PPARgamma (unknown origin) | B | 6.25 | pIC50 | 566 | nM | IC50 | Eur J Med Chem (2021) 221: 113535-113535 [PMID:33992930] |
| 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 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]
