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Assay Detail

CHEMBL681844

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

Binding
In vitro binding affinity for human GABA-A receptor alpha-2-beta-3-gamma-2 subunits expressed in L(tk-) cell membranes
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

GABA-A receptor; alpha-2/beta-3/gamma-2 (CHEMBL2094130)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Synthesis, in vitro affinity, and efficacy of a bis 8-ethynyl-4H-imidazo[1,5a]- [1,4]benzodiazepine analogue, the first bivalent alpha5 subtype selective BzR/GABA(A) antagonist.
Li X, Cao H, Zhang C, Furtmueller R, Fuchs K, Huck S, Sieghart W, Deschamps J, Cook JM.
J Med Chem (2003) 46 : 5567 -5570
PubMed 14667209 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 1 8.59 8.59

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL6597 Ro-154513 1 8.59

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL6597 Ro-154513 Ki = 2.6 nM 8.59