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Electrophysiology Assay from US Patent US20240002393: "SUBSTITUTED BENZO[f][l ,2,4JTRIAZOL0[4,3-a][l ,4JDIAZEPINES AS GABA A GAMMA! POSITIVE ALLOSTERIC MODULATORS"
Assay data:44 Active, 44 Activity ≤ 1 µM, 44 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by DepositorRelated BioAssays by Target
Binding affinity to GABAA receptor (unknown origin) at 10000 nM by radioligand displacement assay relative to control
Assay data:1 Tested
SummaryPubMed CitationRelated BioAssays by Target
Inhibition of alpha2beta2gamma2 GABAA receptor (unknown origin) relative to control
Displacement of [3H]flunitrazepam from human recombinant alpha2beta2gamma2 GABAA receptor expressed in HEK cell membrane by competitive radioligand binding assay
Assay data:20 Active, 7 Activity ≤ 1 nM, 20 Activity ≤ 1 µM, 21 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Binding affinity to GABA A receptor (unknown origin)
Assay data:2 Active, 2 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Inhibition of GABA-A receptor (unknown origin)
Assay data:4 Tested
Inhibition of GABAA receptor (unknown origin) at 50 uM by radioligand receptor binding assay relative to control
Assay data:20 Tested
Antagonist activity at human alpha2beta2gamma2 GABAA receptor expressed in HEK cells by FMP assay
Assay data:2 Active, 1 Activity ≤ 1 µM, 2 Tested
Antagonist activity at human alpha2beta2gamma2 GABAA receptor expressed in HEK293 cells by FMP assay
Assay data:1 Active, 2 Tested
Negative allosteric modulation activity at human GABAA alpha2beta3gamma2 stably expressed in HEK cells by whole cell patch clamp method
Binding Assay from US Patent US10538523: "4-(biphen-3-yl)-1H-pyrazolo[3,4-c]pyridazine derivatives of formula (I) as GABA receptor modulators for use in the treatment of epilepsy and pain"
Assay data:3 Active, 1 Activity ≤ 1 nM, 3 Activity ≤ 1 µM, 3 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
Radioligand Competition Binding Assay from US Patent US8952008: "Chemical compounds"
Assay data:50 Active, 49 Activity ≤ 1 µM, 50 Tested
Radioligand Binding Assay from Article 10.1021/jm800889m: "Structural Requirements for Eszopiclone and Zolpidem Binding to the gamma-Aminobutyric Acid Type-A (GABAA) Receptor Are Different."
Assay data:4 Active, 2 Activity ≤ 1 nM, 4 Activity ≤ 1 µM, 4 Tested
Radioligand Binding Assay from Article 10.1016/j.bmc.2008.08.072: "A study of the structure-activity relationship of GABA(A)-benzodiazepine receptor bivalent ligands by conformational analysis with low temperature NMR and X-ray analysis."
Assay data:8 Active, 1 Activity ≤ 1 nM, 8 Activity ≤ 1 µM, 8 Tested
Binding Assay from US Patent US9802945: "Imidazopyridazine derivatives as modulators of the GABAA receptor activity"
Assay data:23 Active, 23 Activity ≤ 1 µM, 23 Tested
GABAA CEREP ligand profiling
SummaryRelated BioAssays by Target
GABAA BZD (central) CEREP ligand profiling
Cl- channel CEREP ligand profiling
BZD (central) CEREP ligand profiling
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