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Assay Detail

CHEMBL4348569

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

Binding
Positive allosteric modulation of human GABA-A alpha1beta2gamma2S receptor expressed in Xenopus laevis oocytes assessed as increase in GABA-induced chloride channel current by two-electrode voltage clamp method relative to control
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-2/gamma-2 (CHEMBL2095172)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

GABA allosteric modulators: An overview of recent developments in non-benzodiazepine modulators.
Solomon VR, Tallapragada VJ, Chebib M, Johnston GAR, Hanrahan JR.
Eur J Med Chem (2019) 171 : 434 -461
PubMed 30928713 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 2 4.73 4.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL52229 OSTHOLE 1 4.85
CHEMBL510120 OXYPEUCEDANIN 1 4.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL52229 OSTHOLE EC50 = 14000.0 nM 4.85
CHEMBL510120 OXYPEUCEDANIN EC50 = 25000.0 nM 4.60