rivanicline [Ligand Id: 3994] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL132966 ((e)-metanicotine, Rivaniclina, Rivanicline, TC-2403, Trans-metanicotine) |
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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: 474, 464] [UniProtKB: P30926, P32297] | ||||||||
| 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: 472, 465] [UniProtKB: P17787, P43681] | ||||||||
| 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: 465, 472] [UniProtKB: P09483, P12390] | ||||||||
| 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 35:
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]
