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Assay Detail

CHEMBL685366

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

Binding
Displacement of [3H]GABA from gamma-aminobutyric-acid A (GABA-A) receptor
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

GABA-A receptor; anion channel (CHEMBL2093872)
Type PROTEIN COMPLEX GROUP
Organism Homo sapiens

Publication

Structure and molecular modeling of GABAA receptor antagonists.
Rognan D, Boulanger T, Hoffmann R, Vercauteren DP, Andre JM, Durant F, Wermuth CG.
J Med Chem (1992) 35 : 1969 -1977
PubMed 1317920 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 5.39 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL61683 1 7.70
CHEMBL417990 BICUCULLINE 1 4.82
CHEMBL292757 1 4.80
CHEMBL1687 1 4.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL61683 IC50 = 20.0 nM 7.70
CHEMBL417990 BICUCULLINE IC50 = 15000.0 nM 4.82
CHEMBL292757 IC50 = 16000.0 nM 4.80
CHEMBL1687 IC50 = 58000.0 nM 4.24