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Assay Detail

CHEMBL663210

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

Binding
In vitro inhibitory activity against Cysteinyl leukotriene D4 receptor from human lung membrane
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Lung
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Cysteinyl leukotriene receptor 1 (CHEMBL1798)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Stereospecific synthesis, assignment of absolute configuration, and biological activity of the enantiomers of 3-[[[3-[2-(7-chloroquinolin-2-yl)-(E)-ethenyl]phenyl] [[3-(dimethylamino)-3-oxopropyl]thio]methyl]thio]propionic acid, a potent and specific leukotriene D4 receptor antagonist.
Gauthier JY, Jones T, Champion E, Charette L, Dehaven R, Ford-Hutchinson AW, Hoogsteen K, Lord A, Masson P, Piechuta H.
J Med Chem (1990) 33 : 2841 -2845
PubMed 2170650 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 8.31 8.51

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL89768 1 8.51
CHEMBL280481 VERLUKAST 2.0 1 8.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL89768 IC50 = 3.1 nM 8.51
CHEMBL280481 VERLUKAST IC50 = 8.0 nM 8.10