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Assay Detail

CHEMBL829787

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-5-beta-3-gamma-2 expressed in HEK293 cells
4
Total Activities
4
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-5/beta-3/gamma-2 (CHEMBL2111374)
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 4 7.87 8.12

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL191088 1 8.12
CHEMBL372281 1 7.99
CHEMBL192554 1 7.76
CHEMBL192555 1 7.62

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL191088 Ki = 7.57 nM 8.12
CHEMBL372281 Ki = 10.3 nM 7.99
CHEMBL192554 Ki = 17.2 nM 7.76
CHEMBL192555 Ki = 24.1 nM 7.62