rivanicline [Ligand Id: 3994] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL132966 (Rivanicline, TC-2403)
  • nicotinic acetylcholine receptor β4 subunit/nicotinic acetylcholine receptor α3 subunit/Neuronal acetylcholine receptor; alpha3/beta4 in Human [ChEMBL: CHEMBL1907594] [GtoPdb: 474464] [UniProtKB: P30926P32297]
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  • nicotinic acetylcholine receptor β2 subunit/nicotinic acetylcholine receptor α4 subunit/Neuronal acetylcholine receptor; alpha4/beta2 in Human [ChEMBL: CHEMBL1907589] [GtoPdb: 472465] [UniProtKB: P17787P43681]
  • nicotinic acetylcholine receptor α4 subunit/nicotinic acetylcholine receptor β2 subunit/Neuronal acetylcholine receptor; alpha4/beta2 in Rat [ChEMBL: CHEMBL1907596] [GtoPdb: 465472] [UniProtKB: P09483P12390]
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  • nicotinic acetylcholine receptor α7 subunit/Neuronal acetylcholine receptor protein alpha-7 subunit in Human [ChEMBL: CHEMBL2492] [GtoPdb: 468] [UniProtKB: P36544]
  • nicotinic acetylcholine receptor α7 subunit/Neuronal acetylcholine receptor protein alpha-7 subunit in Rat [ChEMBL: CHEMBL4980] [GtoPdb: 468] [UniProtKB: Q05941]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
nicotinic acetylcholine receptor β4 subunit/nicotinic acetylcholine receptor α3 subunit/Neuronal acetylcholine receptor; alpha3/beta4 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907594] [GtoPdb: 474464] [UniProtKB: P30926P32297]
ChEMBL Displacement of [3H]epibatidine from human alpha3beta4 nAChR expressed in human SH-SY5Y cells B 5.27 pKi 5400 nM Ki J. Med. Chem. (2012) 55: 9929-9945 [PMID:23025891]
ChEMBL Compound was evaluated for functional potencies and efficacies at human Nicotinic acetylcholine receptor subtype IMR-32 (ganglionic) B 4.34 pEC50 46000 nM EC50 J. Med. Chem. (1997) 40: 4169-4194 [PMID:9435889]
nicotinic acetylcholine receptor β2 subunit/nicotinic acetylcholine receptor α4 subunit/Neuronal acetylcholine receptor; alpha4/beta2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907589] [GtoPdb: 472465] [UniProtKB: P17787P43681]
ChEMBL Displacement of [3H]nicotine from human alpha4beta2 nAChR expressed in human SH-EP1 cells B 7.59 pKi 26 nM Ki J. Med. Chem. (2012) 55: 9929-9945 [PMID:23025891]
GtoPdb Binding affinity for the α4β2 nicotinic acetylcholine receptor. - 7.6 pKi ~25 nM Ki Bioorg. Med. Chem. Lett. (2004) 14: 523-6 [PMID:14698195]
ChEMBL Binding affinity towards nicotinic acetylcholine receptor alpha4-beta2 B 7.6 pKi 25 nM Ki Bioorg. Med. Chem. Lett. (2004) 14: 523-526 [PMID:14698195]
ChEMBL Compound was evaluated for functional potencies and efficacies at human Nicotinic acetylcholine receptor alpha4-beta2 B 5.37 pEC50 4300 nM EC50 J. Med. Chem. (1997) 40: 4169-4194 [PMID:9435889]
nicotinic acetylcholine receptor α4 subunit/nicotinic acetylcholine receptor β2 subunit/Neuronal acetylcholine receptor; alpha4/beta2 in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907596] [GtoPdb: 465472] [UniProtKB: P09483P12390]
ChEMBL Affinity for Nicotinic acetylcholine receptor alpha4-beta2 in rat brain B 7.59 pKi 26 nM Ki J. Med. Chem. (1997) 40: 4169-4194 [PMID:9435889]
ChEMBL Displacement of [3H]L-nicotine from alpha-4-beta-2 nAChR in rat cerebral cortex B 7.59 pKi 26 nM Ki Bioorg. Med. Chem. Lett. (2008) 18: 188-193 [PMID:18006307]
GtoPdb - - 7.59 pKi 26 nM Ki J. Pharmacol. Exp. Ther. (1996) 279: 1413-21 [PMID:8968366]
ChEMBL Compound was evaluated for functional potencies and efficacies at rat Nicotinic acetylcholine receptor alpha4-beta2 B 6.14 pEC50 730 nM EC50 J. Med. Chem. (1997) 40: 4169-4194 [PMID:9435889]
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 from human alpha7 nAChR expressed in human HEK/RIC3 cells B 5.1 pKi 8000 nM Ki J. Med. Chem. (2012) 55: 9929-9945 [PMID:23025891]
nicotinic acetylcholine receptor α7 subunit/Neuronal acetylcholine receptor protein alpha-7 subunit in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4980] [GtoPdb: 468] [UniProtKB: Q05941]
ChEMBL Affinity for Nicotinic acetylcholine receptor alpha7 B 4.44 pKi 36000 nM Ki J. Med. Chem. (1997) 40: 4169-4194 [PMID:9435889]

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]