A-582941 [Ligand Id: 3995] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL2151443 (A-582941) |
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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 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]
