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Assay Detail

CHEMBL2168415

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

Binding
Displacement of [3H]R-(-)-14 from human FLAG-tagged alpha1 GABA A receptor expressed in HEK293S cells
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293S
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Gamma-aminobutyric acid receptor subunit alpha-1 (CHEMBL1962)
Type SINGLE PROTEIN
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
IC50 3 5.42 5.42

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2163548 1 5.42
CHEMBL2163549 1 -
CHEMBL448 PENTOBARBITAL 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2163548 IC50 = 3800.0 nM 5.42
CHEMBL2163549 IC50 = 120000.0 nM -
CHEMBL448 PENTOBARBITAL IC50 = 1000000.0 nM -