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Assay Detail

CHEMBL4139382

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

Binding
Displacement of [3H]muscimol from human GABAA receptor alpha1beta3gamma2 expressed in HEK293 TetR cell membranes after 1 hr by liquid scintillation counting method
6
Total Activities
3
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 Intermediate

Target

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

Publication

Synthesis and pharmacological evaluation of neurosteroid photoaffinity ligands.
Savechenkov PY, Chiara DC, Desai R, Stern AT, Zhou X, Ziemba AM, Szabo AL, Zhang Y, Cohen JB, Forman SA, Miller KW, Bruzik KS.
Eur J Med Chem (2017) 136 : 334 -347
PubMed 28505538 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 3 6.35 6.60
Inhibition 3 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4163464 2 6.60
CHEMBL190279 ALFAXALONE 2.0 2 6.35
CHEMBL4174166 2 6.11

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4163464 EC50 = 250.0 nM 6.60
CHEMBL190279 ALFAXALONE EC50 = 450.0 nM 6.35
CHEMBL4174166 EC50 = 770.0 nM 6.11
CHEMBL4174166 Inhibition - % -
CHEMBL4163464 Inhibition - % -
CHEMBL190279 ALFAXALONE Inhibition - % -