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Assay Detail

CHEMBL5263771

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

Binding
Positive allosteric modulation of human GABAA alpha1beta2gamma2 receptor expressed in Xenopus laevis oocytes by two-microelectrode voltage-clamp assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Oocyte
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

Breakthroughs in neuroactive steroid drug discovery.
Blanco MJ, La D, Coughlin Q, Newman CA, Griffin AM, Harrison BL, Salituro FG.
Bioorg Med Chem Lett (2018) 28 : 61 -70
PubMed 29223589 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 2 6.31 6.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1568698 GANAXOLONE 4.0 1 6.70
CHEMBL5281882 1 5.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1568698 GANAXOLONE EC50 = 200.0 nM 6.70
CHEMBL5281882 EC50 = 1200.0 nM 5.92