ethopropazine [Ligand Id: 7181] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1206 (Ethopropazine, Parsidol, Profenamine)
  • acetylcholinesterase (Yt 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]
  • Butyrylcholinesterase in Equus caballus [ChEMBL: CHEMBL5077] [UniProtKB: Q9N1N9]
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  • Organic cation transporter 1/Solute carrier family 22 member 1 in Human [ChEMBL: CHEMBL5685] [GtoPdb: 1019] [UniProtKB: O15245]
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  • M1 receptor in Rat [GtoPdb: 13] [UniProtKB: P08482]
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  • M2 receptor in Rat [GtoPdb: 14] [UniProtKB: P10980]
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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 human erythrocytes BChE B 6.52 pIC50 300 nM IC50 Eur J Med Chem (2011) 46: 2170-2184 [PMID:21459491]
ChEMBL Inhibition of human plasma BChE B 6.52 pIC50 300 nM IC50 Eur J Med Chem (2011) 46: 2170-2184 [PMID:21459491]
ChEMBL Inhibition of human erythrocytes AChE B 6.59 pIC50 260 nM IC50 Eur J Med Chem (2011) 46: 2170-2184 [PMID:21459491]
ChEMBL Inhibition of AChE (unknown origin) B 6.59 pIC50 260 nM IC50 J Med Chem (2014) 57: 8167-8179 [PMID:25226236]
butyrylcholinesterase/Butyrylcholinesterase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1914] [GtoPdb: 2471] [UniProtKB: P06276]
ChEMBL Inhibitory activity against Equine Butyrylcholinesterase B 7.7 pKi 20 nM Ki J Med Chem (2003) 46: 1-4 [PMID:12502352]
ChEMBL Inhibition of human BChE assessed as inhibition constant B 7.7 pKi 20 nM Ki J Med Chem (2022) 65: 11365-11387 [PMID:35969197]
ChEMBL Inhibition of recombinant human BChE by Ellman method B 6.52 pIC50 300 nM IC50 J Med Chem (2014) 57: 8167-8179 [PMID:25226236]
ChEMBL Inhibition of BChE (unknown origin) incubated for 10 mins by Ellman's method B 6.68 pIC50 210 nM IC50 Bioorg Med Chem Lett (2019) 29: 126754-126754 [PMID:31708262]
Butyrylcholinesterase in Equus caballus (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5077] [UniProtKB: Q9N1N9]
ChEMBL Dissociation constant for inhibition of equine Butyrylcholinesterase (BuChE) B 7.7 pKi 20 nM Ki J Med Chem (2005) 48: 1919-1929 [PMID:15771436]
Cholinesterase in Equus caballus (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5763] [UniProtKB: P81908]
ChEMBL Inhibition of Equine serum BChE using butyrylthiocholine iodide as a substrate after 20 mins by Ellman's assay B 6.14 pIC50 720 nM IC50 Eur J Med Chem (2011) 46: 2170-2184 [PMID:21459491]
Organic cation transporter 1/Solute carrier family 22 member 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5685] [GtoPdb: 1019] [UniProtKB: O15245]
ChEMBL Inhibition of human OCT1 expressed in HEK293 cells assessed as decrease in uptake of ASP+ after 2 mins by fluorescence assay B 4.69 pIC50 20460 nM IC50 J Med Chem (2017) 60: 2685-2696 [PMID:28230985]
M1 receptor in Rat [GtoPdb: 13] [UniProtKB: P08482]
GtoPdb Displacement of [H]QNB binding in rat forebrain brain homogenate. - 8.51 pKi 3.1 nM Ki Mov Disord (1986) 1: 135-44 [PMID:2904117]
M2 receptor in Rat [GtoPdb: 14] [UniProtKB: P10980]
GtoPdb Displacement of [H]QNB binding in rat hindbrain brain homogenate. - 8.14 pKi 7.2 nM Ki Mov Disord (1986) 1: 135-44 [PMID:2904117]

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]