A-582941 [Ligand Id: 3995] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2151443 (A-582941)
  • nicotinic acetylcholine receptor β2 subunit/nicotinic acetylcholine receptor α4 subunit/Neuronal acetylcholine receptor; alpha4/beta2 in Human [ChEMBL: CHEMBL1907589] [GtoPdb: 472465] [UniProtKB: P17787P43681]
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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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  • 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 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 Binding affinity to alpha4beta2 nAChR B 4 pKi >100000 nM Ki J Med Chem (2011) 54: 7943-7961 [PMID:21919481]
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 Binding affinity to alpha7 nAchR in human frontal cortex membranes B 7.77 pKi 17 nM Ki J Med Chem (2011) 54: 7943-7961 [PMID:21919481]
ChEMBL Agonist activity at alpha7 nAChR F 5.37 pEC50 4260 nM EC50 J Med Chem (2011) 54: 7943-7961 [PMID:21919481]
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 Displacement of [3H]-MLA from alpha7 nAChR in rat brain membranes B 7.06 pKi 88 nM Ki J Med Chem (2011) 54: 7943-7961 [PMID:21919481]
ChEMBL Binding affinity to alpha7 nAChR in rat brain membranes B 7.97 pKi 10.8 nM Ki J Med Chem (2011) 54: 7943-7961 [PMID:21919481]
5-HT3A/Serotonin 3a (5-HT3a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1899] [GtoPdb: 373] [UniProtKB: P46098]
ChEMBL Displacement of [3H]-BRL-43694 from human 5HT3 receptor B 6.82 pKi 150 nM Ki J Med Chem (2011) 54: 7943-7961 [PMID:21919481]

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]