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Assay Detail

CHEMBL685586

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

Functional
Inhibition of the spasmogenic activity of LTD4 in guinea pig parenchymal strips.
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Cavia porcellus
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Cysteinyl leukotriene receptor (CHEMBL2094254)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Development of a novel series of (2-quinolinylmethoxy)phenyl-containing compounds as high-affinity leukotriene receptor antagonists. 1. Initial structure-activity relationships.
Youssefyeh RD, Magnien E, Lee TD, Chan WK, Lin CJ, Galemmo RA, Johnson WH, Tan J, Campbell HF, Huang FC.
J Med Chem (1990) 33 : 1186 -1194
PubMed 2157009 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 6.59 7.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL278920 1 7.72
CHEMBL18265 1 7.60
CHEMBL97541 1 7.44
CHEMBL418551 1 7.10
CHEMBL18558 1 6.92
CHEMBL18081 1 6.85
CHEMBL18864 1 6.70
CHEMBL18471 1 6.62
CHEMBL18309 1 6.60
CHEMBL97287 1 6.60
CHEMBL406006 1 6.56
CHEMBL18177 1 6.55
CHEMBL19106 1 6.40
CHEMBL267475 FPL-55712 1 6.29
CHEMBL18703 1 6.22
CHEMBL19281 1 6.10
CHEMBL277292 1 6.10
CHEMBL19136 1 6.00
CHEMBL18775 1 5.70
CHEMBL18490 1 5.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL278920 IC50 = 19.0 nM 7.72
CHEMBL18265 IC50 = 25.0 nM 7.60
CHEMBL97541 IC50 = 36.0 nM 7.44
CHEMBL418551 IC50 = 79.0 nM 7.10
CHEMBL18558 IC50 = 120.0 nM 6.92
CHEMBL18081 IC50 = 140.0 nM 6.85
CHEMBL18864 IC50 = 200.0 nM 6.70
CHEMBL18471 IC50 = 240.0 nM 6.62
CHEMBL18309 IC50 = 250.0 nM 6.60
CHEMBL97287 IC50 = 250.0 nM 6.60
CHEMBL406006 IC50 = 275.0 nM 6.56
CHEMBL18177 IC50 = 280.0 nM 6.55
CHEMBL19106 IC50 = 400.0 nM 6.40
CHEMBL267475 FPL-55712 IC50 = 510.0 nM 6.29
CHEMBL18703 IC50 = 600.0 nM 6.22
CHEMBL19281 IC50 = 800.0 nM 6.10
CHEMBL277292 IC50 = 800.0 nM 6.10
CHEMBL19136 IC50 = 1000.0 nM 6.00
CHEMBL18775 IC50 = 2000.0 nM 5.70
CHEMBL18490 IC50 = 2000.0 nM 5.70