A-867744 [Ligand Id: 3986] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL490153 (A-867744) |
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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 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]
