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 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 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]