A-867744 [Ligand Id: 3986] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL490153 (A-867744)
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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
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL Displacement of [3H]dofetilide from human ERG channel B 5 pKi >10000 nM Ki J. Med. Chem. (2009) 52: 3377-3384 [PMID:19419141]
ChEMBL Inhibition of human ERG channel B 4.7 pIC50 >20000 nM IC50 J. Med. Chem. (2009) 52: 3377-3384 [PMID:19419141]
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 Positive allosteric modulation at human alpha7 nACHR expressed in Xenopus oocyte assessed as potentiation of 200 uM ACh-induced current at holding potential of -80 mV by electrophysiology B 5.96 pEC50 1100 nM EC50 Eur. J. Med. Chem. (2014) 86: 724-739 [PMID:25232969]
ChEMBL Allosteric modulator activity at alpha7 nAChR in human IMR32 cells assessed as stimulation of agonist-induced intracellular calcium level by FLIPR assay F 6 pEC50 1000 nM EC50 J. Med. Chem. (2009) 52: 3377-3384 [PMID:19419141]
ChEMBL Agonist activity at recombinant human nAChRalpha7 expressed in HEK293 Flip-In cells co-expressing RIC3 assessed as increase in intra cellular calcium level after 10 mins by fluorescence relative to control B 6.22 pEC50 600 nM EC50 Eur J Med Chem (2021) 214: 113189-113189 [PMID:33540354]
ChEMBL Positive allosteric modulatory activity against alpha7 nAChR in human IMR-32 cells assessed as potentiation of PNU-282987-induced Ca2+ efflux at by FLIPR assay B 6.67 pEC50 212 nM EC50 J Med Chem (2020) 63: 944-960 [PMID:31755711]

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]