Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL952531

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Activity at rat wild type GABAA alpha-1H101Cbeta-2-gamma-2 mutant receptor expressed in xenopus oocytes assessed as GABA-elicited response by two electrode voltage clamp method relative to control
8
Total Activities
4
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Cell Type Oocyte
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Proximity-accelerated chemical coupling reaction in the benzodiazepine-binding site of gamma-aminobutyric acid type A receptors: superposition of different allosteric modulators.
Tan KR, Gonthier A, Baur R, Ernst M, Goeldner M, Sigel E.
J Biol Chem (2007) 282 : 26316 -26325
PubMed 17626010 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 4 7.25 7.77
max activation 4 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL485829 2 7.77
CHEMBL6597 Ro-154513 2 7.77
CHEMBL407 FLUMAZENIL 4.0 2 7.52
CHEMBL911 ZOLPIDEM 4.0 2 5.93

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL485829 EC50 = 17.0 nM 7.77
CHEMBL6597 Ro-154513 EC50 = 17.0 nM 7.77
CHEMBL407 FLUMAZENIL EC50 = 30.0 nM 7.52
CHEMBL911 ZOLPIDEM EC50 = 1180.0 nM 5.93
CHEMBL911 ZOLPIDEM max activation = 162.0 % -
CHEMBL485829 max activation = 90.0 % -
CHEMBL6597 Ro-154513 max activation = 40.0 % -
CHEMBL407 FLUMAZENIL max activation = 22.0 % -