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Assay Detail

CHEMBL950412

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

Binding
Displacement of [3H]flumazenil in rat GABAA alpha-2-beta-3-gamma-2 receptor expressed in HEK293 cells
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Cell Type HEK293
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

GABA A receptor alpha-2/beta-2/gamma-2 (CHEMBL2111327)
Type PROTEIN COMPLEX
Organism Rattus norvegicus

Publication

Azaflavones compared to flavones as ligands to the benzodiazepine binding site of brain GABA(A) receptors.
Nilsson J, Nielsen EØ, Liljefors T, Nielsen M, Sterner O.
Bioorg Med Chem Lett (2008) 18 : 5713 -5713
PubMed 18851913 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 3 7.46 7.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL502159 1 7.75
CHEMBL522061 1 7.72
CHEMBL452728 1 6.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL502159 Ki = 18.0 nM 7.75
CHEMBL522061 Ki = 19.0 nM 7.72
CHEMBL452728 Ki = 120.0 nM 6.92