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Assay Detail

CHEMBL682045

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

Binding
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 (high affinity)
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Brain
Subcellular Membrane
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

GABA-A receptor; anion channel (CHEMBL1907607)
Type PROTEIN COMPLEX GROUP
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 2 7.19 7.35

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3138018 1 7.35
CHEMBL3138315 1 7.02

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3138018 IC50 = 45.0 nM 7.35
CHEMBL3138315 IC50 = 96.0 nM 7.02