TC-2559 [Ligand Id: 3987] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1876219
  • nicotinic acetylcholine receptor β4 subunit/nicotinic acetylcholine receptor α3 subunit/Neuronal acetylcholine receptor; alpha3/beta4 in Human [ChEMBL: CHEMBL1907594] [GtoPdb: 474464] [UniProtKB: P30926P32297]
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  • nicotinic acetylcholine receptor β2 subunit/nicotinic acetylcholine receptor α4 subunit/Neuronal acetylcholine receptor; alpha4/beta2 in Human [ChEMBL: CHEMBL1907589] [GtoPdb: 472465] [UniProtKB: P17787P43681]
  • nicotinic acetylcholine receptor α4 subunit/nicotinic acetylcholine receptor β2 subunit/Neuronal acetylcholine receptor; alpha4/beta2 in Rat [ChEMBL: CHEMBL1907596] [GtoPdb: 465472] [UniProtKB: P09483P12390]
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  • nicotinic acetylcholine receptor α7 subunit/Neuronal acetylcholine receptor protein alpha-7 subunit in Human [ChEMBL: CHEMBL2492] [GtoPdb: 468] [UniProtKB: P36544]
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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: 474464] [UniProtKB: P30926P32297]
ChEMBL Displacement of [3H]epibatidine from alpha3beta4 nAChR in human SH-SY5Y cells after 2 hrs by liquid scintillation counting B 5.15 pKi 7000 nM Ki J. Med. Chem. (2012) 55: 9181-9194 [PMID:22793665]
ChEMBL Agonist activity at human alpha3beta4 nAChR expressed in CHO cells assessed as calcium flux by calcium4-based FLIPR assay F 4.7 pEC50 20000 nM EC50 J. Med. Chem. (2012) 55: 9181-9194 [PMID:22793665]
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 Displacement of [3H]nicotine from alpha4beta2 nAChR in human SH-EP1 cells after 2 hrs by liquid scintillation assay B 7.92 pKi 12 nM Ki J. Med. Chem. (2012) 55: 9181-9194 [PMID:22793665]
ChEMBL Agonist activity at alpha4beta2 nAChR in human SH-EP1 cells assessed as calcium flux by calcium4-based FLIPR assay F 6.77 pEC50 170 nM EC50 J. Med. Chem. (2012) 55: 9181-9194 [PMID:22793665]
nicotinic acetylcholine receptor α4 subunit/nicotinic acetylcholine receptor β2 subunit/Neuronal acetylcholine receptor; alpha4/beta2 in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907596] [GtoPdb: 465472] [UniProtKB: P09483P12390]
ChEMBL Displacement of [3H]epibatidine from alpha4beta2 nAChR in Sprague-Dawley rat cortex after 2 hrs by liquid scintillation counting B 8.22 pKi 6 nM Ki J. Med. Chem. (2012) 55: 9181-9194 [PMID:22793665]
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 CHO cells after 2 hrs by liquid scintillation counting B 4.15 pKi 71000 nM Ki J. Med. Chem. (2012) 55: 9181-9194 [PMID:22793665]

ChEMBL data shown on this page come from version 27:

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]