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Assay Detail

CHEMBL5263770

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

Binding
Displacement of [35S]-TBPS GABAA receptor in Wistar rat brain membrane incubated for 60 mins by competitive binding assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Brain
Subcellular Membrane
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

GABA-A receptor; anion channel (CHEMBL1907607)
Type PROTEIN COMPLEX GROUP
Organism Rattus norvegicus

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
IC50 4 6.30 7.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL207538 BREXANOLONE 4.0 1 7.10
CHEMBL5266289 1 6.59
CHEMBL5268883 1 6.20
CHEMBL5284331 1 5.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL207538 BREXANOLONE IC50 = 80.0 nM 7.10
CHEMBL5266289 IC50 = 255.3 nM 6.59
CHEMBL5268883 IC50 = 625.0 nM 6.20
CHEMBL5284331 IC50 = 5000.0 nM 5.30