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Assay Detail

CHEMBL3405049

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

Functional
Inhibition of degranulation in human LAD2 cells assessed as inhibition of IgE-induced beta-hexosaminidase release preincubated for 30 mins by p-nitrophenyl-N-acetyl-D-glucosamide-based spectrophotometric assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type LAD2
Confidence 1 — Organism
Curated By Autocuration

Target

LAD2 (CHEMBL4483253)
Type CELL-LINE
Organism Homo sapiens

Publication

Discovery of 7-azaindole derivatives as potent Orai inhibitors showing efficacy in a preclinical model of asthma.
Esteve C, González J, Gual S, Vidal L, Alzina S, Sentellas S, Jover I, Horrillo R, De Alba J, Miralpeix M, Tarrasón G, Vidal B.
Bioorg Med Chem Lett (2015) 25 : 1217 -1222
PubMed 25690784 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 6.33 6.43

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3403744 1 6.43
CHEMBL3403751 1 6.35
CHEMBL3403753 1 6.20

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3403744 IC50 = 372.0 nM 6.43
CHEMBL3403751 IC50 = 443.0 nM 6.35
CHEMBL3403753 IC50 = 630.0 nM 6.20