PF-06372865 [Ligand Id: 9798] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3647536
  • GABAA receptor α2 subunit/GABA receptor alpha-2 subunit in Human [ChEMBL: CHEMBL4956] [GtoPdb: 405] [UniProtKB: P47869]
1 CHEMBL3647536_lig_chart_1 GABA receptor alpha-2 subunit Human
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
GABAA receptor α2 subunit/GABA receptor alpha-2 subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4956] [GtoPdb: 405] [UniProtKB: P47869]
ChEMBL Radioligand Competition Binding Assay: The affinity of the test compounds was determined by radioligand competition binding assay, using the known compound [3H]Ro-15-1788 (Flumazenil) (Perkin Elmer, 85.4 Ci/mmol) and the human recombinant GABA A receptor containing the alpha2, beta2, and gamma3 subunits.Membranes were prepared from HEK cells expressing hGABA A alpha2beta2- gamma3 receptor, and validated to ascertain protein concentration, receptor expression and to determine the Kd of the flumazenil as well as the Ki of a standard set of compounds before being used to test new compounds.The assay was carried out in 96 well plates; testing compounds using a 10 point semi-log dilution range from 19 uM top concentration. 100 ul of radioligand and 100 ul of membrane in 50 mM Tris-HCI and 0.05% F127 with 1 ul of test compound was incubated for 2 hours to allow the reaction to achieve equilibrium, and then harvested onto filter plates, dried and counted on a TopCount NXT. The data was analysed, and the Ki values were presented. B 8.61 pKi <2.47 nM Ki US-8952008-B2. Chemical compounds (2015)
GtoPdb Determined in a radioligand competition binding assay using [3H]flumazenil and recombinant human GABAA receptor with the α2/β2/γ3 configuration. - 8.61 pKi <2.47 nM Ki WO2014091368. Imidazopyridazine derivatives as GABAA receptor modulators. (2014)

ChEMBL data shown on this page come from version 27:

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]