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Assay Detail

CHEMBL679565

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

Binding
Affinity for GGABA-A receptor alpha by inhibiting binding of [3H]muscimol to rat brain synaptosomes
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Brain
Subcellular Synaptosomes
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

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

Publication

Novel class of potent 4-arylalkyl substituted 3-isoxazolol GABA(A) antagonists: synthesis, pharmacology, and molecular modeling.
Frølund B, Jørgensen AT, Tagmose L, Stensbøl TB, Vestergaard HT, Engblom C, Kristiansen U, Sanchez C, Krogsgaard-Larsen P, Liljefors T.
J Med Chem (2002) 45 : 2454 -2468
PubMed 12036354 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 8.22 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL273481 MUSCIMOL 1.0 1 8.22
CHEMBL81327 1 -

Activity Data

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