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Assay Detail

CHEMBL4042580

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

Binding
Modulation of recombinant human GABA alpha1beta3gamma2 receptor expressed in HEK293 cells assessed as change in GABA-induced current at -80 mV holding potential preincubated for 3 mins followed by co-administration of GABA by electrophysiology method
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
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

Synthesis and Characterization of a Novel γ-Aminobutyric Acid Type A (GABAA) Receptor Ligand That Combines Outstanding Metabolic Stability, Pharmacokinetics, and Anxiolytic Efficacy.
Poe MM, Methuku KR, Li G, Verma AR, Teske KA, Stafford DC, Arnold LA, Cramer JW, Jones TM, Cerne R, Krambis MJ, Witkin JM, Jambrina E, Rehman S, Ernst M, Cook JM, Schkeryantz JM.
J Med Chem (2016) 59 : 10800 -10806
PubMed 27933953 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 1 6.31 6.31

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4062225 1 6.31

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4062225 EC50 = 489.0 nM 6.31