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Assay Detail

CHEMBL4403727

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

Binding
Displacement of [3H]-flumazenil from human GABAA alpha1beta3gamma2 expressed in Ltk cells
2
Total Activities
2
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-1/beta-3/gamma-2 (CHEMBL2094121)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Subtype Selective γ-Aminobutyric Acid Type A Receptor (GABA<sub>A</sub>R) Modulators Acting at the Benzodiazepine Binding Site: An Update.
Maramai S, Benchekroun M, Ward SE, Atack JR.
J Med Chem (2020) 63 : 3425 -3446
PubMed 31738537 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 2 9.38 9.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4303594 1 9.66
CHEMBL373250 1 9.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4303594 Ki = 0.22 nM 9.66
CHEMBL373250 Ki = 0.79 nM 9.10