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Assay Detail

CHEMBL681241

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

Binding
Inhibition against Gamma-aminobutyric acid A (GABA-A) receptor
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

A novel class of potent 3-isoxazolol GABA(A) antagonists: design, synthesis, and pharmacology.
Frølund B, Tagmose L, Liljefors T, Stensbøl TB, Engblom C, Kristiansen U, Krogsgaard-Larsen P.
J Med Chem (2000) 43 : 4930 -4933
PubMed 11150163 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 7.56 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL273481 MUSCIMOL 1.0 1 8.22
CHEMBL312443 GABOXADOL 3.0 1 6.89
CHEMBL81327 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL273481 MUSCIMOL IC50 = 6.0 nM 8.22
CHEMBL312443 GABOXADOL IC50 = 130.0 nM 6.89
CHEMBL81327 IC50 > 100000.0 nM -