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Assay Detail

CHEMBL663971

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

Binding
In vitro binding affinity against cysteinyl leukotriene D4 receptor from guinea pig lung membrane
36
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Tissue Lung
Subcellular Membrane
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

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

Publication

The development of a novel series of (quinolin-2-ylmethoxy)phenyl-containing compounds as high-affinity leukotriene receptor antagonists. 3. Structural variation of the acidic side chain to give antagonists of enhanced potency.
Galemmo RA, Johnson WH, Learn KS, Lee TD, Huang FC, Campbell HF, Youssefyeh R, O'Rourke SV, Schuessler G, Sweeney DM.
J Med Chem (1990) 33 : 2828 -2841
PubMed 2170649 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 36 7.38 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL22033 ICI-198615 1 9.70
CHEMBL93991 1 8.10
CHEMBL317945 1 7.96
CHEMBL97656 1 7.92
CHEMBL97400 1 7.85
CHEMBL328815 1 7.82
CHEMBL98232 1 7.77
CHEMBL97541 1 7.75
CHEMBL264799 1 7.70
CHEMBL97713 1 7.68
CHEMBL421750 1 7.66
CHEMBL97693 1 7.62
CHEMBL96592 1 7.60
CHEMBL420082 1 7.60
CHEMBL97401 1 7.51
CHEMBL98517 1 7.51
CHEMBL329753 1 7.47
CHEMBL418551 1 7.38
CHEMBL93877 1 7.37
CHEMBL97701 1 7.37
CHEMBL95049 1 7.37
CHEMBL420819 1 7.30
CHEMBL94443 1 7.29
CHEMBL94465 1 7.28
CHEMBL97287 1 7.16
CHEMBL318021 1 7.16
CHEMBL97359 1 7.07
CHEMBL94945 1 7.05
CHEMBL94456 1 7.00
CHEMBL94893 1 7.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL22033 ICI-198615 Ki = 0.2 nM 9.70
CHEMBL93991 Ki = 8.0 nM 8.10
CHEMBL317945 Ki = 11.0 nM 7.96
CHEMBL97656 Ki = 12.0 nM 7.92
CHEMBL97400 Ki = 14.0 nM 7.85
CHEMBL328815 Ki = 15.0 nM 7.82
CHEMBL98232 Ki = 17.0 nM 7.77
CHEMBL97541 Ki = 18.0 nM 7.75
CHEMBL264799 Ki = 20.0 nM 7.70
CHEMBL97713 Ki = 21.0 nM 7.68
CHEMBL421750 Ki = 22.0 nM 7.66
CHEMBL97693 Ki = 24.0 nM 7.62
CHEMBL96592 Ki = 25.0 nM 7.60
CHEMBL420082 Ki = 25.0 nM 7.60
CHEMBL98517 Ki = 31.0 nM 7.51
CHEMBL97401 Ki = 31.0 nM 7.51
CHEMBL329753 Ki = 34.0 nM 7.47
CHEMBL418551 Ki = 42.0 nM 7.38
CHEMBL93877 Ki = 43.0 nM 7.37
CHEMBL95049 Ki = 43.0 nM 7.37
CHEMBL97701 Ki = 43.0 nM 7.37
CHEMBL420819 Ki = 50.0 nM 7.30
CHEMBL94443 Ki = 51.0 nM 7.29
CHEMBL94465 Ki = 52.0 nM 7.28
CHEMBL97287 Ki = 69.0 nM 7.16
CHEMBL318021 Ki = 70.0 nM 7.16
CHEMBL97359 Ki = 85.0 nM 7.07
CHEMBL94945 Ki = 90.0 nM 7.05
CHEMBL94456 Ki = 100.0 nM 7.00
CHEMBL94893 Ki = 100.0 nM 7.00
CHEMBL97743 Ki = 110.0 nM 6.96
CHEMBL18471 Ki = 130.0 nM 6.89
CHEMBL94949 Ki = 140.0 nM 6.85
CHEMBL162358 TOMELUKAST Ki = 800.0 nM 6.10
CHEMBL267475 FPL-55712 Ki = 1000.0 nM 6.00
CHEMBL277292 Ki = 1200.0 nM 5.92