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Assay Detail

CHEMBL666489

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

Binding
Inhibition constant for displacement of [3H]LTD4 on guinea pig lung parenchymal membranes.
8
Total Activities
8
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 8 6.57 7.39

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL50422 1 7.39
CHEMBL422404 1 7.24
CHEMBL301928 1 7.10
CHEMBL298727 1 6.80
CHEMBL50733 1 6.63
CHEMBL298939 1 5.95
CHEMBL52906 1 5.74
CHEMBL298642 1 5.72

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL50422 Ki = 41.0 nM 7.39
CHEMBL422404 Ki = 58.0 nM 7.24
CHEMBL301928 Ki = 80.0 nM 7.10
CHEMBL298727 Ki = 157.0 nM 6.80
CHEMBL50733 Ki = 236.0 nM 6.63
CHEMBL298939 Ki = 1119.0 nM 5.95
CHEMBL52906 Ki = 1830.0 nM 5.74
CHEMBL298642 Ki = 1900.0 nM 5.72