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Assay Detail

CHEMBL706931

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

Binding
Inhibition of binding of [3H]LTD4 to guinea pig lung membrane
21
Total Activities
21
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

Discovery of L-740,515, a potent thienopyridine cysLT1 receptor (LTD4 receptor) antagonist
Labelle M, Gareau Y, Dufresne C, Lau C, Belley M, Jones T, Leblanc Y, McAuliffe M, McFarlane C, Metters K, Ouimet N, Perrier H, Rochette C, Sawyer N, Slipetz D, Xiang Y, Wang Z, Pickett C, Ford-Hutchinson A, Young R, Zamboni R
Bioorg Med Chem Lett (1995) 5 : 2551 -2556
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 9.00 9.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL86302 1 9.47
CHEMBL316170 1 9.38
CHEMBL85633 1 9.38
CHEMBL314237 1 9.38
CHEMBL313195 1 9.36
CHEMBL86063 1 9.32
CHEMBL84707 1 9.27
CHEMBL313187 1 9.25
CHEMBL414885 1 9.24
CHEMBL314340 1 9.14
CHEMBL315973 1 9.13
CHEMBL87337 1 9.05
CHEMBL87696 1 8.96
CHEMBL86264 1 8.88
CHEMBL87528 1 8.71
CHEMBL82790 1 8.71
CHEMBL85572 1 8.59
CHEMBL84841 1 8.42
CHEMBL313177 1 8.38
CHEMBL83233 1 7.96
CHEMBL313544 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL86302 IC50 = 0.34 nM 9.47
CHEMBL316170 IC50 = 0.42 nM 9.38
CHEMBL85633 IC50 = 0.42 nM 9.38
CHEMBL314237 IC50 = 0.42 nM 9.38
CHEMBL313195 IC50 = 0.44 nM 9.36
CHEMBL86063 IC50 = 0.48 nM 9.32
CHEMBL84707 IC50 = 0.54 nM 9.27
CHEMBL313187 IC50 = 0.56 nM 9.25
CHEMBL414885 IC50 = 0.58 nM 9.24
CHEMBL314340 IC50 = 0.72 nM 9.14
CHEMBL315973 IC50 = 0.74 nM 9.13
CHEMBL87337 IC50 = 0.89 nM 9.05
CHEMBL87696 IC50 = 1.09 nM 8.96
CHEMBL86264 IC50 = 1.31 nM 8.88
CHEMBL87528 IC50 = 1.95 nM 8.71
CHEMBL82790 IC50 = 1.95 nM 8.71
CHEMBL85572 IC50 = 2.6 nM 8.59
CHEMBL84841 IC50 = 3.84 nM 8.42
CHEMBL313177 IC50 = 4.12 nM 8.38
CHEMBL83233 IC50 = 10.9 nM 7.96
CHEMBL313544 IC50 > 150.0 nM -