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Assay Detail

CHEMBL857377

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

Binding
Allosteric modulation of [35S]TBPS binding to Gamma-aminobutyric acid A receptor in rat brain cortical P2 membranes (inhibits binding with two components)
1
Total Activities
1
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

Synthesis and in vitro activity of 3 beta-substituted-3 alpha-hydroxypregnan-20-ones: allosteric modulators of the GABAA receptor.
Hogenkamp DJ, Tahir SH, Hawkinson JE, Upasani RB, Alauddin M, Kimbrough CL, Acosta-Burruel M, Whittemore ER, Woodward RM, Lan NC, Gee KW, Bolger MB.
J Med Chem (1997) 40 : 61 -72
PubMed 9016329 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 7.36 7.36

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL210952 ELTANOLONE 2.0 1 7.36

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL210952 ELTANOLONE IC50 = 44.0 nM 7.36