LAU463 [Ligand Id: 12405] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL4092332 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| GABAA receptor γ2 subunit/GABAA receptor α6 subunit/GABAA receptor α1 subunit/GABAA receptor β3 subunit/Gamma-aminobutyric acid receptor subunit alpha-1/alpha-6/beta-3/gamma-2 in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL5291947] [GtoPdb: 414, 409, 404, 412] [UniProtKB: P18508, P30191, P62813, P63079] | ||||||||
| ChEMBL | Positive allosteric modulation of rat recombinant GABAA gamma2beta3alpha1-beta3alpha6 receptor expressed in Xenopus laevis oocytes assessed as increase in GABA-induced current amplitude at -80 mV holding potential under less potent phase in presence of GABA EC1 to 1.5 by two-electrode voltage-clamp assay | B | 4.44 | pEC50 | 36000 | nM | EC50 | Bioorg Med Chem (2019) 27: 3167-3178 [PMID:31186146] |
| ChEMBL | Positive allosteric modulation of rat recombinant GABAA alpha6beta3alpha1-gamma2beta3 receptor expressed in Xenopus laevis oocytes assessed as increase in GABA-induced current amplitude at -80 mV holding potential under less potent phase in presence of GABA EC1 to 1.5 by two-electrode voltage-clamp assay | B | 5.15 | pEC50 | 7000 | nM | EC50 | Bioorg Med Chem (2019) 27: 3167-3178 [PMID:31186146] |
| ChEMBL | Positive allosteric modulation of rat recombinant GABAA gamma2beta3alpha1-beta3alpha6 receptor expressed in Xenopus laevis oocytes assessed as increase in GABA-induced current amplitude at -80 mV holding potential under more potent phase in presence of GABA EC1 to 1.5 by two-electrode voltage-clamp assay | B | 8.4 | pEC50 | 4 | nM | EC50 | Bioorg Med Chem (2019) 27: 3167-3178 [PMID:31186146] |
| GABAA receptor γ2 subunit/GABAA receptor α1 subunit/GABAA receptor β3 subunit/Gamma-aminobutyric acid receptor subunit alpha-1/beta-3/gamma-2 in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL4296062] [GtoPdb: 414, 404, 412] [UniProtKB: P18508, P62813, P63079] | ||||||||
| ChEMBL | Positive allosteric modulation of rat recombinant GABAA alpha1beta3alpha1-gamma2beta3 receptor expressed in Xenopus laevis oocytes assessed as increase in GABA-induced current amplitude at -80 mV holding potential under less potent phase in presence of GABA EC1 to 1.5 by two-electrode voltage-clamp assay | B | 5 | pEC50 | 10000 | nM | EC50 | Bioorg Med Chem (2019) 27: 3167-3178 [PMID:31186146] |
| ChEMBL | Positive allosteric modulation of rat recombinant GABAA alpha1beta3gamma2 receptor expressed in Xenopus laevis oocytes assessed as increase in GABA-induced current amplitude at -80 mV holding potential under less potent phase in presence of GABA EC1 to 1.5 by two-electrode voltage-clamp assay | B | 5.22 | pEC50 | 6000 | nM | EC50 | Bioorg Med Chem (2019) 27: 3167-3178 [PMID:31186146] |
| 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 | Positive allosteric modulation of rat recombinant GABAA alpha6beta3alpha6-gamma2beta3 receptor expressed in Xenopus laevis oocytes assessed as increase in GABA-induced current amplitude at -80 mV holding potential under less potent phase in presence of GABA EC1 to 1.5 by two-electrode voltage-clamp assay | B | 4.62 | pEC50 | 24000 | nM | EC50 | Bioorg Med Chem (2019) 27: 3167-3178 [PMID:31186146] |
| ChEMBL | Positive allosteric modulation of rat recombinant GABAA alpha6beta3gamma2 receptor expressed in Xenopus laevis oocytes assessed as increase in GABA-induced current amplitude at -80 mV holding potential under less potent phase in presence of GABA EC1 to 1.5 by two-electrode voltage-clamp assay | B | 4.96 | pEC50 | 11000 | nM | EC50 | Bioorg Med Chem (2019) 27: 3167-3178 [PMID:31186146] |
| ChEMBL | Positive allosteric modulation of rat recombinant GABAA alpha6beta3alpha6-gamma2beta3 receptor expressed in Xenopus laevis oocytes assessed as increase in GABA-induced current amplitude at -80 mV holding potential under more potent phase in presence of GABA EC1 to 1.5 by two-electrode voltage-clamp assay | B | 8.05 | pEC50 | 9 | nM | EC50 | Bioorg Med Chem (2019) 27: 3167-3178 [PMID:31186146] |
| ChEMBL | Positive allosteric modulation of rat recombinant GABAA alpha6beta3gamma2 receptor expressed in Xenopus laevis oocytes assessed as increase in GABA-induced current amplitude at -80 mV holding potential under more potent phase in presence of GABA EC1 to 1.5 by two-electrode voltage-clamp assay | B | 9 | pEC50 | 1 | nM | EC50 | Bioorg Med Chem (2019) 27: 3167-3178 [PMID:31186146] |
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]
