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Assay Detail

CHEMBL663193

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

Binding
Binding affinity against LTD4 receptor in guinea pig lung membranes.
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
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 a novel series of (2-quinolinylmethoxy)phenyl-containing compounds as high-affinity leukotriene D4 receptor antagonists. 4. Addition of chromone moiety enhances leukotriene D4 receptor binding affinity.
Huang FC, Galemmo RA, Poli GB, Learn KS, Morrissette MM, Johnson WH, Dankulich WP, Campbell HF, Carnathan GW, VanInwegen RG.
J Med Chem (1991) 34 : 1704 -1707
PubMed 1851845 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 17 8.36 10.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL47430 1 10.00
CHEMBL46663 1 9.92
CHEMBL44734 1 9.52
CHEMBL22033 ICI-198615 1 9.52
CHEMBL47662 1 8.96
CHEMBL296097 1 8.92
CHEMBL46343 1 8.89
CHEMBL49449 1 8.68
CHEMBL47376 1 8.60
CHEMBL18518 RG-12525 1 8.52
CHEMBL295368 1 8.20
CHEMBL45965 1 7.89
CHEMBL49696 1 7.82
CHEMBL295664 1 7.75
CHEMBL45850 1 7.52
CHEMBL267475 FPL-55712 1 6.29
CHEMBL46362 1 5.16

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL47430 Ki = 0.1 nM 10.00
CHEMBL46663 Ki = 0.12 nM 9.92
CHEMBL44734 Ki = 0.3 nM 9.52
CHEMBL22033 ICI-198615 Ki = 0.3 nM 9.52
CHEMBL47662 Ki = 1.1 nM 8.96
CHEMBL296097 Ki = 1.2 nM 8.92
CHEMBL46343 Ki = 1.3 nM 8.89
CHEMBL49449 Ki = 2.1 nM 8.68
CHEMBL47376 Ki = 2.5 nM 8.60
CHEMBL18518 RG-12525 Ki = 3.0 nM 8.52
CHEMBL295368 Ki = 6.3 nM 8.20
CHEMBL45965 Ki = 13.0 nM 7.89
CHEMBL49696 Ki = 15.0 nM 7.82
CHEMBL295664 Ki = 18.0 nM 7.75
CHEMBL45850 Ki = 30.0 nM 7.52
CHEMBL267475 FPL-55712 Ki = 510.0 nM 6.29
CHEMBL46362 Ki = 7000.0 nM 5.16