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Assay Detail

CHEMBL710517

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

Binding
Inhibition of [3H]LTD4 binding to LTD4 receptor in guinea pig lung membranes
5
Total Activities
5
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

Synthesis and pharmacological profile of two novel heterocyclic chromanols, CP-80,798 and CP-85,958, as potent LTD4 receptor antagonists
Andrews E, Antognoli G, Breslow R, Carta M, Carty T, Chambers R, Cheng J, Cohan V, Collins J, Damon D, Delehunt J, Eggler J, Eskra J, Freiert K, Hada W, Marfat A, Masamune H, Melvin L, Mularski C, Naclerio B, Pazoles C, Pillar J, Rappach L, Reiche P, Rusek F, Sherman H, Shirley J, Sweeney F, Tickner J, Watson J, Wright C
Bioorg Med Chem Lett (1995) 5 : 1365 -1370
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 5.38 6.19

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL282524 1 6.19
CHEMBL283455 1 5.82
CHEMBL28797 1 5.17
CHEMBL8747 REV-5901 1 5.10
CHEMBL442150 1 4.62

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL282524 Ki = 650.0 nM 6.19
CHEMBL283455 Ki = 1500.0 nM 5.82
CHEMBL28797 Ki = 6800.0 nM 5.17
CHEMBL8747 REV-5901 Ki = 8000.0 nM 5.10
CHEMBL442150 Ki = 24000.0 nM 4.62