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Assay Detail

CHEMBL839938

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

Binding
Binding affinity towards gamma-aminobutyric-acid GABA-A receptor alpha-4-beta-3-gamma-2
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 6 — Multiple protein complex / RNA
Curated By Expert

Target

GABA A receptor alpha-4/beta-3/gamma-2 (CHEMBL2111366)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

An orally bioavailable, functionally selective inverse agonist at the benzodiazepine site of GABAA alpha5 receptors with cognition enhancing properties.
Chambers MS, Atack JR, Carling RW, Collinson N, Cook SM, Dawson GR, Ferris P, Hobbs SC, O'connor D, Marshall G, Rycroft W, Macleod AM.
J Med Chem (2004) 47 : 5829 -5832
PubMed 15537339 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 1 6.40 6.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL363211 1 6.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL363211 Ki = 395.0 nM 6.40