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Assay Detail

CHEMBL4194693

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

Binding
Modulation of rat eGFP-fused GABA-A receptor alpha4beta3delta expressed in HEK293 cells in presence of GABA by patch-clamp assay
2
Total Activities
2
Compounds Tested
1
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
EC50 2 6.42 6.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4213357 1 6.82
CHEMBL4212818 1 6.01

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4213357 EC50 = 150.0 nM 6.82
CHEMBL4212818 EC50 = 970.0 nM 6.01