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Assay Detail

CHEMBL663217

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Functional
Antagonism of Cysteinyl leukotriene receptor 1 from guinea pig lung membranes
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Cavia porcellus
Tissue Lung
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Cysteinyl leukotriene receptor 1 (CHEMBL5645)
Type SINGLE PROTEIN
Organism Cavia porcellus

Publication

Development of 2,2-dimethylchromanol cysteinyl LT1 receptor antagonists.
Chambers RJ, Antognoli GW, Cheng JB, Kuperman AV, Liston TC, Marfat A, Owens BS, Pillar JS, Shirley JT, Watson JW.
Bioorg Med Chem Lett (1998) 8 : 3577 -3582
PubMed 9934474 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 8.53 9.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL300701 1 9.15
CHEMBL21333 PRANLUKAST 4.0 1 9.10
CHEMBL332680 1 8.70
CHEMBL603 ZAFIRLUKAST 4.0 1 8.70
CHEMBL120200 1 8.40
CHEMBL119214 1 8.40
CHEMBL331884 1 8.30
CHEMBL331747 1 8.15
CHEMBL442150 1 7.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL300701 Ki = 0.7 nM 9.15
CHEMBL21333 PRANLUKAST Ki = 0.8 nM 9.10
CHEMBL332680 Ki = 2.0 nM 8.70
CHEMBL603 ZAFIRLUKAST Ki = 2.0 nM 8.70
CHEMBL120200 Ki = 4.0 nM 8.40
CHEMBL119214 Ki = 4.0 nM 8.40
CHEMBL331884 Ki = 5.0 nM 8.30
CHEMBL331747 Ki = 7.0 nM 8.15
CHEMBL442150 Ki = 14.0 nM 7.85