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Assay Detail

CHEMBL710518

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

Binding
In vitro inhibition of [3H]-LTD4 binding to LTD4 receptor of DMSO differentiated human U937 cell membranes
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type U-937
Confidence 9 — Direct single protein target
Curated By Expert

Target

Cysteinyl leukotriene receptor 1 (CHEMBL1798)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

A series of non-quinoline cysLT1 receptor antagonists: SAR study on pyridyl analogs of Singulair.
Guay D, Gauthier JY, Dufresne C, Jones TR, McAuliffe M, McFarlane C, Metters KM, Prasit P, Rochette C, Roy P, Sawyer N, Zamboni R.
Bioorg Med Chem Lett (1998) 8 : 453 -458
PubMed 9871597 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 9.04 9.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL344180 1 9.60
CHEMBL343934 1 9.38
CHEMBL143515 1 9.36
CHEMBL342705 1 9.33
CHEMBL341603 1 9.25
CHEMBL139757 1 9.21
CHEMBL787 MONTELUKAST 4.0 1 9.11
CHEMBL141640 1 8.96
CHEMBL141405 1 8.77
CHEMBL140381 1 8.70
CHEMBL140058 1 8.54
CHEMBL348229 1 8.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL344180 IC50 = 0.25 nM 9.60
CHEMBL343934 IC50 = 0.42 nM 9.38
CHEMBL143515 IC50 = 0.44 nM 9.36
CHEMBL342705 IC50 = 0.47 nM 9.33
CHEMBL341603 IC50 = 0.56 nM 9.25
CHEMBL139757 IC50 = 0.61 nM 9.21
CHEMBL787 MONTELUKAST IC50 = 0.78 nM 9.11
CHEMBL141640 IC50 = 1.1 nM 8.96
CHEMBL141405 IC50 = 1.7 nM 8.77
CHEMBL140381 IC50 = 2.0 nM 8.70
CHEMBL140058 IC50 = 2.9 nM 8.54
CHEMBL348229 IC50 = 5.0 nM 8.30