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Assay Detail

CHEMBL838372

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

Functional
Enhancement of currents elicited by GABA at EC5 (6-12 uM)
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Confidence 6 — Multiple protein complex / RNA
Curated By Autocuration

Target

GABA-A receptor; alpha-1/beta-2/gamma-2 (CHEMBL2095172)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

2-(3-Methyl-3H-diaziren-3-yl)ethyl 1-(1-phenylethyl)-1H-imidazole-5-carboxylate: a derivative of the stereoselective general anesthetic etomidate for photolabeling ligand-gated ion channels.
Husain SS, Ziebell MR, Ruesch D, Hong F, Arevalo E, Kosterlitz JA, Olsen RW, Forman SA, Cohen JB, Miller KW.
J Med Chem (2003) 46 : 1257 -1265
PubMed 12646036 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 4 5.08 5.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL23497 1 5.70
CHEMBL681 ETOMIDATE 4.0 1 5.60
CHEMBL22676 1 4.70
CHEMBL279678 S-ETOMIDATE -1.0 1 4.33

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL23497 EC50 = 2000.0 nM 5.70
CHEMBL681 ETOMIDATE EC50 = 2500.0 nM 5.60
CHEMBL22676 EC50 = 20000.0 nM 4.70
CHEMBL279678 S-ETOMIDATE EC50 = 47000.0 nM 4.33