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: 472, 465] [UniProtKB: P17787, P43681]
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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: 472, 465] [UniProtKB: P17787, P43681]
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 31:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños 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]