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Assay Detail

CHEMBL829786

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

Binding
Displacement of [3H]flumazenil from rat GABA-A Gamma-aminobutyric acid A receptor alpha-2-beta-2-gamma-2 expressed in HEK293 cells
5
Total Activities
5
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 Expert

Target

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

Publication

High affinity central benzodiazepine receptor ligands: synthesis and biological evaluation of a series of phenyltriazolobenzotriazindione derivatives.
Primofiore G, Da Settimo F, Taliani S, Salerno S, Novellino E, Greco G, Cosimelli B, Besnard F, Costa B, Montali M, Martini C.
J Med Chem (2005) 48 : 2936 -2943
PubMed 15828832 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 7.43 7.86

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL372281 1 7.86
CHEMBL192554 1 7.84
CHEMBL191088 1 7.75
CHEMBL192555 1 7.56
CHEMBL911 ZOLPIDEM 4.0 1 6.12

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL372281 Ki = 13.9 nM 7.86
CHEMBL192554 Ki = 14.3 nM 7.84
CHEMBL191088 Ki = 18.0 nM 7.75
CHEMBL192555 Ki = 27.6 nM 7.56
CHEMBL911 ZOLPIDEM Ki = 765.0 nM 6.12