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Assay Detail

CHEMBL5055971

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

Binding
Positive allosteric modulation of human recombinant alpha4beta1delta GABAA receptor expressed in delta-HEK cells assessed as potentiation of GABA-induced response in presence of GABA EC20 by FMP assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 7 — Homologous single protein target
Curated By Autocuration

Publication

Structural Determinants for the Mode of Action of Imidazopyridine DS2 at δ-Containing γ-Aminobutyric Acid Type A Receptors.
Rostrup F, Falk-Petersen CB, Harpso E K, Buchleithner S, Conforti I, Jung S, Gloriam DE, Schirmeister T, Wellendorph P, Fro Lund B.
J Med Chem (2021) 64 : 4730 -4743
PubMed 33847501 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 6 6.43 7.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5072077 1 7.22
CHEMBL5088746 1 6.85
CHEMBL5081682 1 6.80
CHEMBL4212818 1 6.01
CHEMBL5090382 1 5.96
CHEMBL5069550 1 5.72

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5072077 EC50 = 60.0 nM 7.22
CHEMBL5088746 EC50 = 140.0 nM 6.85
CHEMBL5081682 EC50 = 160.0 nM 6.80
CHEMBL4212818 EC50 = 980.0 nM 6.01
CHEMBL5090382 EC50 = 1100.0 nM 5.96
CHEMBL5069550 EC50 = 1920.0 nM 5.72