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Assay Detail

CHEMBL4403739

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

Binding
Displacement of [3H]-flunitrazepam from human GABAA alpha1beta3gamma2 expressed in HEK293T cells by liquid scintillation counting method
3
Total Activities
3
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 3 6.32 6.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL475022 1 6.52
CHEMBL4547830 1 6.33
CHEMBL4571892 1 6.12

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL475022 Ki = 300.0 nM 6.52
CHEMBL4547830 Ki = 468.0 nM 6.33
CHEMBL4571892 Ki = 759.0 nM 6.12