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ChEMBL ligand: CHEMBL1206 (Ethopropazine, Parsidol, Profenamine) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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]