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Assay Detail

CHEMBL706928

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 guinea pig lung membrane without human serum albumin (HSA).
32
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Cysteinyl leukotriene receptor (CHEMBL2094254)
Type PROTEIN FAMILY
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 32 8.63 9.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL344180 1 9.72
CHEMBL343934 1 9.72
CHEMBL139757 1 9.68
CHEMBL341603 1 9.47
CHEMBL143515 1 9.30
CHEMBL143597 1 9.30
CHEMBL342705 1 9.29
CHEMBL141640 1 9.24
CHEMBL787 MONTELUKAST 4.0 1 9.19
CHEMBL141405 1 9.14
CHEMBL140058 1 9.13
CHEMBL143326 1 9.10
CHEMBL141234 1 9.10
CHEMBL140381 1 9.06
CHEMBL341547 1 9.05
CHEMBL141841 1 9.05
CHEMBL140761 1 8.92
CHEMBL341814 1 8.92
CHEMBL342784 1 8.85
CHEMBL341657 1 8.62
CHEMBL358142 1 8.62
CHEMBL348229 1 8.59
CHEMBL345093 1 8.57
CHEMBL344169 1 8.31
CHEMBL140644 1 7.93
CHEMBL139560 1 7.90
CHEMBL424108 1 7.64
CHEMBL342588 1 7.60
CHEMBL143115 1 7.60
CHEMBL434445 1 6.71

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL344180 IC50 = 0.19 nM 9.72
CHEMBL343934 IC50 = 0.19 nM 9.72
CHEMBL139757 IC50 = 0.21 nM 9.68
CHEMBL341603 IC50 = 0.34 nM 9.47
CHEMBL143515 IC50 = 0.5 nM 9.30
CHEMBL143597 IC50 = 0.5 nM 9.30
CHEMBL342705 IC50 = 0.51 nM 9.29
CHEMBL141640 IC50 = 0.58 nM 9.24
CHEMBL787 MONTELUKAST IC50 = 0.64 nM 9.19
CHEMBL141405 IC50 = 0.73 nM 9.14
CHEMBL140058 IC50 = 0.74 nM 9.13
CHEMBL143326 IC50 = 0.8 nM 9.10
CHEMBL141234 IC50 = 0.8 nM 9.10
CHEMBL140381 IC50 = 0.87 nM 9.06
CHEMBL141841 IC50 = 0.9 nM 9.05
CHEMBL341547 IC50 = 0.9 nM 9.05
CHEMBL140761 IC50 = 1.2 nM 8.92
CHEMBL341814 IC50 = 1.2 nM 8.92
CHEMBL342784 IC50 = 1.4 nM 8.85
CHEMBL341657 IC50 = 2.4 nM 8.62
CHEMBL358142 IC50 = 2.4 nM 8.62
CHEMBL348229 IC50 = 2.6 nM 8.59
CHEMBL345093 IC50 = 2.7 nM 8.57
CHEMBL344169 IC50 = 4.9 nM 8.31
CHEMBL140644 IC50 = 11.8 nM 7.93
CHEMBL139560 IC50 = 12.7 nM 7.90
CHEMBL424108 IC50 = 22.8 nM 7.64
CHEMBL342588 IC50 = 25.0 nM 7.60
CHEMBL143115 IC50 = 25.2 nM 7.60
CHEMBL434445 IC50 = 194.0 nM 6.71
CHEMBL335332 IC50 = 410.0 nM 6.39
CHEMBL141300 IC50 = 421.0 nM 6.38