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Assay Detail

CHEMBL922472

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

Binding
Displacement of [3H]TBOB from GABAA receptor in Sprague-Dawley rat cerebral cortex
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Cerebral cortex
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Synthesis and GABA(A) receptor activity of oxygen-bridged neurosteroid analogs.
Alvarez LD, Veleiro AS, Baggio RF, Garland MT, Edelsztein VC, Coirini H, Burton G.
Bioorg Med Chem (2008) 16 : 3831 -3838
PubMed 18262792 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 6.27 6.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL207538 BREXANOLONE 4.0 1 6.48
CHEMBL259201 1 6.38
CHEMBL259828 1 6.29
CHEMBL260226 1 6.13
CHEMBL210952 ELTANOLONE 2.0 1 6.08

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL207538 BREXANOLONE IC50 = 329.0 nM 6.48
CHEMBL259201 IC50 = 420.0 nM 6.38
CHEMBL259828 IC50 = 518.0 nM 6.29
CHEMBL260226 IC50 = 741.0 nM 6.13
CHEMBL210952 ELTANOLONE IC50 = 830.0 nM 6.08