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Assay Detail

CHEMBL681140

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

Functional
Inhibition of GABA-stimulated 36Cl- uptake by membrane vesicles of rat cerebral cortex
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Tissue Cerebral cortex
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

(+/-)-4-tert-butyl-3-cyano-1-(4-ethynylphenyl)-2,6,7-trioxabi cyclo[2.2.2]octane: synthesis of a remarkably potent GABAA receptor antagonist.
Palmer CJ, Cole LM, Carida JE.
J Med Chem (1988) 31 : 1064 -1066
PubMed 2836586 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 7.40 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL10438 1 7.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL10438 IC50 = 40.0 nM 7.40