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Assay Detail

CHEMBL666435

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

Binding
Inhibitory activity to block binding of [3H]leukotriene D4 to LTD4 receptor sites in homogenized guinea pig lung
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

3,4-Dihydro-2H-1-benzopyran-2-carboxylic acids and related compounds as leukotriene antagonists.
Cohen N, Weber G, Banner BL, Lopresti RJ, Schaer B, Focella A, Zenchoff GB, Chiu AM, Todaro L, O'Donnell M.
J Med Chem (1989) 32 : 1842 -1860
PubMed 2547071 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 5.76 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL22033 ICI-198615 1 9.00
CHEMBL21983 CGP-35949 1 6.00
CHEMBL55714 1 5.70
CHEMBL417028 1 5.70
CHEMBL267475 FPL-55712 1 5.40
CHEMBL53333 1 5.40
CHEMBL293529 1 5.30
CHEMBL54688 1 5.30
CHEMBL53512 1 5.22
CHEMBL17344 RITOLUKAST 2.0 1 5.22
CHEMBL52877 1 5.16

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL22033 ICI-198615 IC50 = 1.0 nM 9.00
CHEMBL21983 CGP-35949 IC50 = 1000.0 nM 6.00
CHEMBL55714 IC50 = 2000.0 nM 5.70
CHEMBL417028 IC50 = 2000.0 nM 5.70
CHEMBL267475 FPL-55712 IC50 = 4000.0 nM 5.40
CHEMBL53333 IC50 = 4000.0 nM 5.40
CHEMBL293529 IC50 = 5000.0 nM 5.30
CHEMBL54688 IC50 = 5000.0 nM 5.30
CHEMBL53512 IC50 = 6000.0 nM 5.22
CHEMBL17344 RITOLUKAST IC50 = 6000.0 nM 5.22
CHEMBL52877 IC50 = 7000.0 nM 5.16