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Assay Detail

CHEMBL689683

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Functional
Inhibition of Leukotriene D4 induced contraction of guinea-pig trachea was determined
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Cavia porcellus
Tissue Trachea
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

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

Publication

The discovery of a new structural class of potent orally active leukotriene D4 antagonists
Labelle M, Prasit P, Belley M, Blouin M, Champion E, Charette L, DeLuca J, Dufresne C, Frenette R, Gauthier J, Grimm E, Grossman S, Guay D, Herold E, Jones T, Lau C, Leblanc Y, Leger S, Lord A, McAuliffe M, McFarlane C, Masson P, Metters K, Ouimet N, Patrick D, Perrier H, Pickett C, Piechuta H, Roy P, Williams H, Wang Z, Xiang Y, Zamboni R, Ford-Hutchinson A, Young R
Bioorg Med Chem Lett (1992) 2 : 1141 -1146
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 6 8.87 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL275357 1 9.40
CHEMBL15306 1 9.10
CHEMBL277533 1 8.80
CHEMBL15177 MK-571 1 8.80
CHEMBL15161 L-695499 1 8.80
CHEMBL274913 1 8.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL275357 Kd = 0.3981 nM 9.40
CHEMBL15306 Kd = 0.7943 nM 9.10
CHEMBL277533 Kd = 1.585 nM 8.80
CHEMBL15177 MK-571 Kd = 1.585 nM 8.80
CHEMBL15161 L-695499 Kd = 1.585 nM 8.80
CHEMBL274913 Kd = 5.012 nM 8.30