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

CHEMBL680680

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

Binding
Non-competitive displacement of [35S]TBPS from picrotoxin binding site found in heterogeneous Gamma-aminobutyric acid A receptor in rat brain membranes
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

GABA-A receptor; anion channel (CHEMBL1907607)
Type PROTEIN COMPLEX GROUP
Organism Rattus norvegicus

Publication

Neurosteroid analogues. 9. Conformationally constrained pregnanes: structure-activity studies of 13,24-cyclo-18,21-dinorcholane analogues of the GABA modulatory and anesthetic steroids (3alpha,5alpha)- and (3alpha,5beta)-3-hydroxypregnan-20-one.
Jiang X, Manion BD, Benz A, Rath NP, Evers AS, Zorumski CF, Mennerick S, Covey DF.
J Med Chem (2003) 46 : 5334 -5348
PubMed 14640542 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 7.13 7.13

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL207538 BREXANOLONE 4.0 1 7.13

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL207538 BREXANOLONE IC50 = 74.0 nM 7.13