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Assay Detail

CHEMBL706933

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

Binding
Inhibitory concentration against [3H]Leukotriene D4 binding to guinea-pig lung membranes was determined
20
Total Activities
19
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

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
IC50 20 8.73 9.44

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL14819 1 9.44
CHEMBL15232 1 9.40
CHEMBL280310 1 9.35
CHEMBL15120 1 9.33
CHEMBL15132 1 9.28
CHEMBL278411 1 9.22
CHEMBL15161 L-695499 1 9.05
CHEMBL15513 1 9.02
CHEMBL279773 1 9.02
CHEMBL416161 1 9.00
CHEMBL15500 1 8.89
CHEMBL430147 1 8.72
CHEMBL15177 MK-571 2 8.52
CHEMBL276584 1 8.44
CHEMBL15419 1 8.20
CHEMBL15481 1 8.19
CHEMBL15485 1 8.07
CHEMBL277332 1 7.85
CHEMBL15491 1 7.12

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL14819 IC50 = 0.36 nM 9.44
CHEMBL15232 IC50 = 0.4 nM 9.40
CHEMBL280310 IC50 = 0.45 nM 9.35
CHEMBL15120 IC50 = 0.47 nM 9.33
CHEMBL15132 IC50 = 0.52 nM 9.28
CHEMBL278411 IC50 = 0.6 nM 9.22
CHEMBL15161 L-695499 IC50 = 0.9 nM 9.05
CHEMBL15513 IC50 = 0.95 nM 9.02
CHEMBL279773 IC50 = 0.95 nM 9.02
CHEMBL416161 IC50 = 1.0 nM 9.00
CHEMBL15500 IC50 = 1.3 nM 8.89
CHEMBL430147 IC50 = 1.9 nM 8.72
CHEMBL15177 MK-571 IC50 = 3.0 nM 8.52
CHEMBL276584 IC50 = 3.6 nM 8.44
CHEMBL15177 MK-571 IC50 = 3.9 nM 8.41
CHEMBL15419 IC50 = 6.3 nM 8.20
CHEMBL15481 IC50 = 6.5 nM 8.19
CHEMBL15485 IC50 = 8.6 nM 8.07
CHEMBL277332 IC50 = 14.0 nM 7.85
CHEMBL15491 IC50 = 75.0 nM 7.12