AZD0328 [Ligand Id: 7697] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2151437 (Azd0328, Azd 0328, Azd-0328, AZD0328, AZD-0328)
  • 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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  • 5-HT3A in Human [GtoPdb: 379]
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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 human alpha4beta2 nAChR B 6.85 pKi 140 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]
GtoPdb - - 8.52 pKi 3 nM Ki J Med Chem (2011) 54: 7943-61 [PMID:21919481]
ChEMBL Binding affinity to human alpha7 nAchR B 8.52 pKi 3 nM Ki J. Med. Chem. (2011) 54: 7943-7961 [PMID:21919481]
ChEMBL Displacement of [125I]alpha-bungarotoxin from human alpha7 nAChR expressed in HEK293 cell membranes after 2 hrs by topcount scintillation counting analysis B 8.52 pKi 3 nM Ki Bioorg Med Chem Lett (2017) 27: 5002-5005 [PMID:29050783]
ChEMBL Agonist activity at human alpha7 nAChR F 6.47 pEC50 340 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 [125I]alpha-bungarotoxin from rat alpha7 nAChR expressed in HEK293 cell membranes after 2 hrs by topcount scintillation counting analysis B 8.3 pKi 5 nM Ki Bioorg Med Chem Lett (2017) 27: 5002-5005 [PMID:29050783]
5-HT3A/Serotonin 3a (5-HT3a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1899] [GtoPdb: 373] [UniProtKB: P46098]
ChEMBL Binding affinity to human 5HT3A receptor B 7.92 pKi 12 nM Ki J. Med. Chem. (2011) 54: 7943-7961 [PMID:21919481]
5-HT3A in Human [GtoPdb: 379]
GtoPdb - - 7.92 pKi 12 nM Ki J Med Chem (2011) 54: 7943-61 [PMID:21919481]

ChEMBL data shown on this page come from version 28:

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]