loreclezole [Ligand Id: 5466] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1397886 (Loreclezol, Loreclezole, R 72063, R-72063) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| GABAA receptor α1 subunit/GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABA-A receptor; alpha-1/beta-3/gamma-2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094121] [GtoPdb: 404, 414, 412] [UniProtKB: P14867, P18507, P28472] | ||||||||
| ChEMBL | Positive allosteric modulation of GABA-A alpha1beta3gamma2S receptor (unknown origin) expressed in Xenopus laevis oocytes assessed as increase in GABA-induced chloride current after 15 mins at -70 mV holding potential by two-microelectrode voltage clamp method | B | 4.96 | pEC50 | 11000 | nM | EC50 | J Med Chem (2018) 62: 317-341 [PMID:30289721] |
| GABAA receptor γ2 subunit/GABAA receptor α6 subunit/GABAA receptor β3 subunit/Gamma-aminobutyric acid receptor subunit alpha-6/beta-3/gamma-2 in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL4296054] [GtoPdb: 414, 409, 412] [UniProtKB: P18508, P30191, P63079] | ||||||||
| ChEMBL | Modulation of rat alpha6beta3gamma2 GABA A receptor expressed in Xenopus oocytes assessed as reduction in desensitization at -80 mV holding potential by two-electrode voltage-clamp assay | B | 4.42 | pEC50 | 38000 | nM | EC50 | Eur J Med Chem (2022) 244: 114780-114780 [PMID:36279694] |
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]
