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Assay Detail

CHEMBL872982

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

Functional
In vitro inhibition of [35S]-TBPS binding to Gamma-aminobutyric acid A receptor in rat brain cortical membranes in the presence of 5 uM GABA (low affinity)
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Tissue Brain
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Expert

Target

Gamma-aminobutyric acid receptor subunit gamma-1 (CHEMBL296)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

3 alpha-Hydroxy-3 beta-(phenylethynyl)-5 beta-pregnan-20-ones: synthesis and pharmacological activity of neuroactive steroids with high affinity for GABAA receptors.
Upasani RB, Yang KC, Acosta-Burruel M, Konkoy CS, McLellan JA, Woodward RM, Lan NC, Carter RB, Hawkinson JE.
J Med Chem (1997) 40 : 73 -84
PubMed 9016330 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 5.29 5.29

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3138017 1 5.29

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3138017 IC50 = 5100.0 nM 5.29