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Assay Detail

CHEMBL711839

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

Binding
Inhibition of [3H]LTD4 binding on guinea-pig lung membranes
38
Total Activities
24
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

Evolution of a series of non-quinoline leukotriene D4 receptor antagonist; synthesis and sar of benzothiazoles and thiazoles substituted benzyl alcohols as potent LTD4 antagonists
Lau C, Dufresne C, Gareau Y, Zamboni R, Labelle M, Young R, Metters K, Rochette C, Sawyer N, Slipetz D, Charette L, Jones T, McAuliffe M, McFarlane C, Ford-Hutchinson A
Bioorg Med Chem Lett (1995) 5 : 1615 -1620
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 38 8.14 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL416251 2 9.30
CHEMBL287722 2 9.15
CHEMBL43602 2 9.10
CHEMBL42051 1 9.10
CHEMBL288369 1 8.82
CHEMBL295281 2 8.77
CHEMBL41620 1 8.72
CHEMBL416249 2 8.70
CHEMBL40213 1 8.68
CHEMBL43874 2 8.52
CHEMBL43509 1 8.48
CHEMBL280481 VERLUKAST 2.0 1 8.41
CHEMBL40992 2 8.28
CHEMBL39077 2 8.22
CHEMBL262391 2 8.17
CHEMBL42520 2 8.17
CHEMBL41395 2 8.12
CHEMBL41230 1 7.78
CHEMBL40686 1 7.38
CHEMBL42410 1 7.32
CHEMBL43821 2 7.10
CHEMBL40836 2 7.01
CHEMBL297396 2 6.77
CHEMBL415903 1 6.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL416251 IC50 = 0.5 nM 9.30
CHEMBL416251 IC50 = 0.6 nM 9.22
CHEMBL287722 IC50 = 0.7 nM 9.15
CHEMBL42051 IC50 = 0.8 nM 9.10
CHEMBL43602 IC50 = 0.8 nM 9.10
CHEMBL287722 IC50 = 1.0 nM 9.00
CHEMBL43602 IC50 = 1.4 nM 8.85
CHEMBL288369 IC50 = 1.5 nM 8.82
CHEMBL295281 IC50 = 1.7 nM 8.77
CHEMBL41620 IC50 = 1.9 nM 8.72
CHEMBL416249 IC50 = 2.0 nM 8.70
CHEMBL40213 IC50 = 2.1 nM 8.68
CHEMBL43874 IC50 = 3.0 nM 8.52
CHEMBL43509 IC50 = 3.3 nM 8.48
CHEMBL295281 IC50 = 3.3 nM 8.48
CHEMBL416249 IC50 = 3.3 nM 8.48
CHEMBL280481 VERLUKAST IC50 = 3.9 nM 8.41
CHEMBL43874 IC50 = 4.6 nM 8.34
CHEMBL40992 IC50 = 5.2 nM 8.28
CHEMBL39077 IC50 = 6.0 nM 8.22
CHEMBL42520 IC50 = 6.7 nM 8.17
CHEMBL262391 IC50 = 6.7 nM 8.17
CHEMBL41395 IC50 = 7.5 nM 8.12
CHEMBL39077 IC50 = 7.7 nM 8.11
CHEMBL42520 IC50 = 11.0 nM 7.96
CHEMBL41395 IC50 = 11.6 nM 7.94
CHEMBL40992 IC50 = 12.8 nM 7.89
CHEMBL262391 IC50 = 15.4 nM 7.81
CHEMBL41230 IC50 = 16.8 nM 7.78
CHEMBL40686 IC50 = 42.2 nM 7.38
CHEMBL42410 IC50 = 47.6 nM 7.32
CHEMBL43821 IC50 = 79.3 nM 7.10
CHEMBL40836 IC50 = 98.7 nM 7.01
CHEMBL43821 IC50 = 99.7 nM 7.00
CHEMBL40836 IC50 = 138.0 nM 6.86
CHEMBL297396 IC50 = 170.0 nM 6.77
CHEMBL297396 IC50 = 197.0 nM 6.71
CHEMBL415903 IC50 = 381.0 nM 6.42