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 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]