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Assay Detail

CHEMBL2168418

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

Binding
Activation of human alpha1beta3gamma2L GABA A receptor expressed in HEK293 cells assessed as increase in [3H]muscimol binding by scintillation counting assay
4
Total Activities
2
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

GABA-A receptor; alpha-1/beta-3/gamma-2 (CHEMBL2094121)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Allyl m-trifluoromethyldiazirine mephobarbital: an unusually potent enantioselective and photoreactive barbiturate general anesthetic.
Savechenkov PY, Zhang X, Chiara DC, Stewart DS, Ge R, Zhou X, Raines DE, Cohen JB, Forman SA, Miller KW, Bruzik KS.
J Med Chem (2012) 55 : 6554 -6565
PubMed 22734650 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Activity 2 - -
EC50 2 5.39 5.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2163548 2 5.92
CHEMBL2163549 2 4.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2163548 EC50 = 1200.0 nM 5.92
CHEMBL2163549 EC50 = 14100.0 nM 4.85
CHEMBL2163549 Activity - -
CHEMBL2163548 Activity - -