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Assay Detail

CHEMBL1014536

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

Binding
Displacement of [35S]TBPS from Wistar rat brain GABAA receptor
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Allopregnanolone (3alpha-hydroxy-5alpha-pregnan-20-one) derivatives with a polar chain in position 16alpha: synthesis and activity.
Slavíková B, Kristofíková Z, Chodounská H, Budesínský M, Durán FJ, Veleiro AS, Burton G, Kasal A.
J Med Chem (2009) 52 : 2119 -2125
PubMed 19290593 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 6.87 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL515590 1 7.40
CHEMBL207538 BREXANOLONE 4.0 1 7.10
CHEMBL474985 1 7.07
CHEMBL1094 FELBAMATE 4.0 1 7.02
CHEMBL522179 1 6.52
CHEMBL493339 1 6.12

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL515590 IC50 = 40.0 nM 7.40
CHEMBL207538 BREXANOLONE IC50 = 80.0 nM 7.10
CHEMBL474985 IC50 = 86.0 nM 7.07
CHEMBL1094 FELBAMATE IC50 = 95.0 nM 7.02
CHEMBL522179 IC50 = 300.0 nM 6.52
CHEMBL493339 IC50 = 750.0 nM 6.12