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

CHEMBL681136

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

Binding
In vitro inhibition of [3H]GABA binding to Gamma-aminobutyric acid receptor of rat brain synaptic membranes
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
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

GABA agonists. Resolution, absolute stereochemistry, and enantioselectivity of (S)-(+)- and (R)-(-)-dihydromuscimol.
Krogsgaard-Larsen P, Nielsen L, Falch E, Curtis DR.
J Med Chem (1985) 28 : 1612 -1617
PubMed 2999396 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 7.42 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL42464 1 8.40
CHEMBL273481 MUSCIMOL 1.0 1 8.22
CHEMBL96 GAMMA-AMINOBUTYRIC ACID 1.0 1 7.48
CHEMBL40804 1 6.60
CHEMBL296263 1 6.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL42464 IC50 = 4.0 nM 8.40
CHEMBL273481 MUSCIMOL IC50 = 6.0 nM 8.22
CHEMBL96 GAMMA-AMINOBUTYRIC ACID IC50 = 33.0 nM 7.48
CHEMBL40804 IC50 = 250.0 nM 6.60
CHEMBL296263 IC50 = 400.0 nM 6.40