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ChEMBL ligand: CHEMBL1206 (Ethopropazine, Parsidol, Profenamina, 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 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]