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Assay Detail

CHEMBL681137

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

Binding
In vitro inhibition of [3H]P4S binding to Gamma-aminobutyric acid receptor of rat brain synaptic membranes
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
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

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 7 7.10 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL273481 MUSCIMOL 1.0 1 8.22
CHEMBL42464 1 8.10
CHEMBL40363 1 7.75
CHEMBL96 GAMMA-AMINOBUTYRIC ACID 1.0 1 7.60
CHEMBL40804 1 6.27
CHEMBL296263 1 6.05
CHEMBL290216 1 5.72

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL273481 MUSCIMOL IC50 = 6.0 nM 8.22
CHEMBL42464 IC50 = 8.0 nM 8.10
CHEMBL40363 IC50 = 18.0 nM 7.75
CHEMBL96 GAMMA-AMINOBUTYRIC ACID IC50 = 25.0 nM 7.60
CHEMBL40804 IC50 = 540.0 nM 6.27
CHEMBL296263 IC50 = 900.0 nM 6.05
CHEMBL290216 IC50 = 1900.0 nM 5.72