encenicline [Ligand Id: 6926] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2151572 (MT-4666, EVP-6124, MT4666, Encenicline)
  • nicotinic acetylcholine receptor α7 subunit/Neuronal acetylcholine receptor protein alpha-7 subunit in Human [ChEMBL: CHEMBL2492] [GtoPdb: 468] [UniProtKB: P36544]
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  • 5-HT3A/Serotonin 3a (5-HT3a) receptor in Human [ChEMBL: CHEMBL1899] [GtoPdb: 373] [UniProtKB: P46098]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
nicotinic acetylcholine receptor α7 subunit/Neuronal acetylcholine receptor protein alpha-7 subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2492] [GtoPdb: 468] [UniProtKB: P36544]
ChEMBL Displacement of [3H]epibatidine form human alpha7 nAchR expressed in HEK293 cells B 8 pKi 9.98 nM Ki J. Med. Chem. (2012) 55: 9793-9809 [PMID:23126648]
ChEMBL Binding affinity to human alpha7 nAchR B 8.37 pKi 4.3 nM Ki J. Med. Chem. (2011) 54: 7943-7961 [PMID:21919481]
GtoPdb - - 8.37 pKi 4.3 nM Ki Drugs R D (2004) 5: 102-7 [PMID:15293871];
J. Med. Chem. (2011) 54: 7943-61 [PMID:21919481]
ChEMBL Agonist activity at human alpha7 nAChR expressed in xenopus oocytes preincubated for 10 mins followed by acetylcholine addition by patch clamp electrophysiological assay B 6.47 pEC50 340 nM EC50 Eur. J. Med. Chem. (2016) 115: 94-108 [PMID:26994846]
5-HT3A/Serotonin 3a (5-HT3a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1899] [GtoPdb: 373] [UniProtKB: P46098]
ChEMBL Binding affinity to 5HT3 receptor B 6.52 pIC50 299 nM IC50 J. Med. Chem. (2011) 54: 7943-7961 [PMID:21919481]

ChEMBL data shown on this page come from version 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]