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Assay Detail

CHEMBL932857

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

Binding
Displacement of [35S]TBPS from GABAA receptor in rat brain membrane
10
Total Activities
10
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

Neurosteroid analogues. 14. Alternative ring system scaffolds: GABA modulatory and anesthetic actions of cyclopenta[b]phenanthrenes and cyclopenta[b]anthracenes.
Scaglione JB, Jastrzebska I, Krishnan K, Li P, Akk G, Manion BD, Benz A, Taylor A, Rath NP, Evers AS, Zorumski CF, Mennerick S, Covey DF.
J Med Chem (2008) 51 : 1309 -1318
PubMed 18275132 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 6.28 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL259246 1 7.40
CHEMBL271371 1 7.22
CHEMBL429756 1 6.96
CHEMBL406188 1 6.60
CHEMBL87285 ANDROSTERONE 1 6.39
CHEMBL271599 1 5.93
CHEMBL272037 1 5.84
CHEMBL258825 1 5.80
CHEMBL211898 1 5.38
CHEMBL379925 1 5.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL259246 IC50 = 40.0 nM 7.40
CHEMBL271371 IC50 = 60.0 nM 7.22
CHEMBL429756 IC50 = 110.0 nM 6.96
CHEMBL406188 IC50 = 250.0 nM 6.60
CHEMBL87285 ANDROSTERONE IC50 = 410.0 nM 6.39
CHEMBL271599 IC50 = 1170.0 nM 5.93
CHEMBL272037 IC50 = 1440.0 nM 5.84
CHEMBL258825 IC50 = 1580.0 nM 5.80
CHEMBL211898 IC50 = 4170.0 nM 5.38
CHEMBL379925 IC50 = 5010.0 nM 5.30