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Assay Detail

CHEMBL686875

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

Binding
In vitro inhibition of [3H]LTD4 binding to guinea pig lung membranes
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Tissue Lung
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Cysteinyl leukotriene receptor 1 (CHEMBL5645)
Type SINGLE PROTEIN
Organism Cavia porcellus

Publication

Development of a novel series of styrylquinoline compounds as high-affinity leukotriene D4 receptor antagonists: synthetic and structure-activity studies leading to the discovery of (+-)-3-[[[3-[2-(7-chloro-2-quinolinyl)-(E)-ethenyl]phenyl][[3- (dimethylamino)-3-oxopropyl]thio]methyl]thio]propionic acid.
Zamboni R, Belley M, Champion E, Charette L, DeHaven R, Frenette R, Gauthier JY, Jones TR, Leger S, Masson P.
J Med Chem (1992) 35 : 3832 -3844
PubMed 1331447 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 7.78 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL124095 1 9.52
CHEMBL408753 1 8.66
CHEMBL125135 1 7.87
CHEMBL124259 1 7.22
CHEMBL123958 1 7.05
CHEMBL338166 1 6.36

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL124095 IC50 = 0.3 nM 9.52
CHEMBL408753 IC50 = 2.2 nM 8.66
CHEMBL125135 IC50 = 13.6 nM 7.87
CHEMBL124259 IC50 = 60.0 nM 7.22
CHEMBL123958 IC50 = 89.0 nM 7.05
CHEMBL338166 IC50 = 440.0 nM 6.36