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Assay Detail

CHEMBL932865

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

Binding
Activity at rat GABAA alpha-1-beta-2-gamma-2L receptor expressed in HEK293 cells assessed as macroscopic current amplitude by electrophysiological method
6
Total Activities
3
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Cell Type HEK293
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
Activity 3 - -
EC50 3 6.41 6.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL259246 2 6.47
CHEMBL271371 2 6.39
CHEMBL429756 2 6.36

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL259246 EC50 = 340.0 nM 6.47
CHEMBL271371 EC50 = 410.0 nM 6.39
CHEMBL429756 EC50 = 440.0 nM 6.36
CHEMBL429756 Activity = 269.0 % -
CHEMBL271371 Activity = 294.0 % -
CHEMBL259246 Activity = 262.0 % -