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Assay Detail

CHEMBL663192

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

Binding
Displacement of [3H]LTD4 on guinea pig lung parenchymal membranes
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Tissue Lung parenchyma
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 peptidoleukotriene antagonists: synthesis and structure/activity relationships of 1,3,5-substituted indoles and indazoles.
Matassa VG, Maduskuie TP, Shapiro HS, Hesp B, Snyder DW, Aharony D, Krell RD, Keith RA.
J Med Chem (1990) 33 : 1781 -1790
PubMed 2342072 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 13 8.06 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL50370 1 9.52
CHEMBL603 ZAFIRLUKAST 4.0 1 9.52
CHEMBL52492 1 9.30
CHEMBL51891 1 9.30
CHEMBL301498 1 9.10
CHEMBL300846 1 9.00
CHEMBL431348 1 8.85
CHEMBL49519 1 7.30
CHEMBL49298 1 7.10
CHEMBL295268 1 6.80
CHEMBL300940 1 6.80
CHEMBL51544 1 6.70
CHEMBL162358 TOMELUKAST 2.0 1 5.55

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL50370 Ki = 0.3 nM 9.52
CHEMBL603 ZAFIRLUKAST Ki = 0.3 nM 9.52
CHEMBL52492 Ki = 0.5 nM 9.30
CHEMBL51891 Ki = 0.5 nM 9.30
CHEMBL301498 Ki = 0.8 nM 9.10
CHEMBL300846 Ki = 1.0 nM 9.00
CHEMBL431348 Ki = 1.4 nM 8.85
CHEMBL49519 Ki = 50.0 nM 7.30
CHEMBL49298 Ki = 80.0 nM 7.10
CHEMBL295268 Ki = 160.0 nM 6.80
CHEMBL300940 Ki = 160.0 nM 6.80
CHEMBL51544 Ki = 200.0 nM 6.70
CHEMBL162358 TOMELUKAST Ki = 2818.0 nM 5.55