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Assay Detail

CHEMBL1052639

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

Binding
Inhibition of [35S]tert-butylbicyclo[ 2.2.2]phosphorothionate binding to GABAA receptor in Wistar rat brain membrane
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 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Synthesis of fluorinated brassinosteroids based on alkene cross-metathesis and preliminary biological assessment.
Eignerová B, Slavíková B, Budĕsínský M, Dracínský M, Klepetárová B, St'astná E, Kotora M.
J Med Chem (2009) 52 : 5753 -5757
PubMed 19719120 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 6.72 7.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL207538 BREXANOLONE 4.0 1 7.10
CHEMBL558049 1 7.00
CHEMBL538884 1 6.05
CHEMBL555224 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL207538 BREXANOLONE IC50 = 80.0 nM 7.10
CHEMBL558049 IC50 = 100.0 nM 7.00
CHEMBL538884 IC50 = 900.0 nM 6.05
CHEMBL555224 IC50 - -