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Assay Detail

CHEMBL706929

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

Binding
Concentration required for inhibition of binding of [3H]LTD4 to guinea pig lung membranes
15
Total Activities
15
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

Discovery of MK-0476, a potent and orally active leukotriene D4 receptor antagonist devoid of peroxisomal enxyme induction
Labelle M, Belley M, Gareau Y, Gauthier J, Guay D, Gordon R, Grossman S, Jones T, Leblanc Y, McAuliffe M, McFarlane C, Masson P, Metters K, Ouimet N, Patrick D, Piechuta H, Rochette C, Sawyer N, Xiang Y, Pickett C, Ford-Hutchinson A, Zamboni R, Young R
Bioorg Med Chem Lett (1995) 5 : 283 -288
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 9.22 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL330649 1 9.70
CHEMBL99775 1 9.52
CHEMBL95234 1 9.52
CHEMBL96986 1 9.48
CHEMBL319802 1 9.37
CHEMBL603 ZAFIRLUKAST 4.0 1 9.36
CHEMBL97576 1 9.36
CHEMBL787 MONTELUKAST 4.0 1 9.30
CHEMBL95362 1 9.24
CHEMBL95317 1 9.22
CHEMBL316688 1 9.17
CHEMBL98676 1 9.10
CHEMBL89768 1 8.82
CHEMBL327942 1 8.64
CHEMBL89340 1 8.51

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL330649 IC50 = 0.2 nM 9.70
CHEMBL99775 IC50 = 0.3 nM 9.52
CHEMBL95234 IC50 = 0.3 nM 9.52
CHEMBL96986 IC50 = 0.33 nM 9.48
CHEMBL319802 IC50 = 0.43 nM 9.37
CHEMBL603 ZAFIRLUKAST IC50 = 0.44 nM 9.36
CHEMBL97576 IC50 = 0.44 nM 9.36
CHEMBL787 MONTELUKAST IC50 = 0.5 nM 9.30
CHEMBL95362 IC50 = 0.58 nM 9.24
CHEMBL95317 IC50 = 0.6 nM 9.22
CHEMBL316688 IC50 = 0.68 nM 9.17
CHEMBL98676 IC50 = 0.79 nM 9.10
CHEMBL89768 IC50 = 1.5 nM 8.82
CHEMBL327942 IC50 = 2.3 nM 8.64
CHEMBL89340 IC50 = 3.1 nM 8.51