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Assay Detail

CHEMBL4194716

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

Binding
Displacement of [3H]EBOB from rat GABA-A receptor alpha6beta3delta expressed in HEK293 cell membranes after 90 mins in presence of GABA by liquid scintillation counting analysis
6
Total Activities
3
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Cell Type HEK293
Confidence 7 — Homologous single protein target
Curated By Intermediate

Publication

Structure-Function Evaluation of Imidazopyridine Derivatives Selective for δ-Subunit-Containing γ-Aminobutyric Acid Type A (GABAA) Receptors.
Yakoub K, Jung S, Sattler C, Damerow H, Weber J, Kretzschmann A, Cankaya AS, Piel M, Rösch F, Haugaard AS, Frølund B, Schirmeister T, Lüddens H.
J Med Chem (2018) 61 : 1951 -1968
PubMed 29451785 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Imax 3 - -
IC50 3 6.27 6.43

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4213357 2 6.43
CHEMBL4213793 2 6.31
CHEMBL4208971 2 6.06

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4213357 IC50 = 370.0 nM 6.43
CHEMBL4213793 IC50 = 490.0 nM 6.31
CHEMBL4208971 IC50 = 870.0 nM 6.06
CHEMBL4213357 Imax = 88.0 % -
CHEMBL4208971 Imax = 51.0 % -
CHEMBL4213793 Imax = 55.0 % -