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Assay Detail

CHEMBL706791

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; experiment 1
13
Total Activities
13
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 13 9.00 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL275357 1 9.70
CHEMBL15292 1 9.40
CHEMBL15370 1 9.40
CHEMBL279630 1 9.30
CHEMBL15035 1 9.30
CHEMBL274049 1 9.25
CHEMBL15344 1 9.22
CHEMBL278210 1 9.10
CHEMBL429975 1 8.85
CHEMBL15306 1 8.70
CHEMBL280260 1 8.70
CHEMBL277533 1 8.30
CHEMBL274913 1 7.77

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL275357 IC50 = 0.2 nM 9.70
CHEMBL15292 IC50 = 0.4 nM 9.40
CHEMBL15370 IC50 = 0.4 nM 9.40
CHEMBL279630 IC50 = 0.5 nM 9.30
CHEMBL15035 IC50 = 0.5 nM 9.30
CHEMBL274049 IC50 = 0.56 nM 9.25
CHEMBL15344 IC50 = 0.6 nM 9.22
CHEMBL278210 IC50 = 0.8 nM 9.10
CHEMBL429975 IC50 = 1.4 nM 8.85
CHEMBL15306 IC50 = 2.0 nM 8.70
CHEMBL280260 IC50 = 2.0 nM 8.70
CHEMBL277533 IC50 = 5.0 nM 8.30
CHEMBL274913 IC50 = 17.0 nM 7.77