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Assay Detail

CHEMBL686876

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

Functional
In vitro inhibition of [3H]LTD4 binding to guinea pig lung membranes.
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Cavia porcellus
Tissue Lung
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Cysteinyl leukotriene receptor (CHEMBL2094254)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Development of a novel series of styrylquinoline compounds as high-affinity leukotriene D4 receptor antagonists: synthetic and structure-activity studies leading to the discovery of (+-)-3-[[[3-[2-(7-chloro-2-quinolinyl)-(E)-ethenyl]phenyl][[3- (dimethylamino)-3-oxopropyl]thio]methyl]thio]propionic acid.
Zamboni R, Belley M, Champion E, Charette L, DeHaven R, Frenette R, Gauthier JY, Jones TR, Leger S, Masson P.
J Med Chem (1992) 35 : 3832 -3844
PubMed 1331447 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 6.63 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL127877 1 8.52
CHEMBL340726 1 7.82
CHEMBL123577 1 7.41
CHEMBL126859 1 7.27
CHEMBL128010 1 7.01
CHEMBL125799 1 6.57
CHEMBL125027 1 6.32
CHEMBL125978 1 6.30
CHEMBL8747 REV-5901 1 6.29
CHEMBL414242 1 6.25
CHEMBL127530 1 6.24
CHEMBL126379 1 6.00
CHEMBL125139 1 5.84
CHEMBL124760 1 5.82
CHEMBL124709 1 5.75
CHEMBL127545 1 -
CHEMBL339304 1 -
CHEMBL127905 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL127877 IC50 = 3.0 nM 8.52
CHEMBL340726 IC50 = 15.0 nM 7.82
CHEMBL123577 IC50 = 39.0 nM 7.41
CHEMBL126859 IC50 = 54.0 nM 7.27
CHEMBL128010 IC50 = 97.0 nM 7.01
CHEMBL125799 IC50 = 270.0 nM 6.57
CHEMBL125027 IC50 = 480.0 nM 6.32
CHEMBL125978 IC50 = 495.0 nM 6.30
CHEMBL8747 REV-5901 IC50 = 510.0 nM 6.29
CHEMBL414242 IC50 = 560.0 nM 6.25
CHEMBL127530 IC50 = 580.0 nM 6.24
CHEMBL126379 IC50 = 1000.0 nM 6.00
CHEMBL125139 IC50 = 1430.0 nM 5.84
CHEMBL124760 IC50 = 1500.0 nM 5.82
CHEMBL124709 IC50 = 1780.0 nM 5.75
CHEMBL127545 IC50 > 50000.0 nM -
CHEMBL339304 IC50 > 50000.0 nM -
CHEMBL127905 IC50 > 50000.0 nM -