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Assay Detail

CHEMBL826973

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

Binding
Inhibition of 5-lipoxygenase activity in human whole blood assay
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Tissue Blood
Confidence 9 — Direct single protein target
Curated By Expert

Target

Polyunsaturated fatty acid 5-lipoxygenase (CHEMBL215)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Cetirizine and loratadine-based antihistamines with 5-lipoxygenase inhibitory activity.
Lewis TA, Young MA, Arrington MP, Bayless L, Cai X, Collart P, Eckman JB, Ellis JL, Ene DG, Libertine L, Nicolas JM, Scannell RT, Wels BF, Wenberg K, Wypij DM.
Bioorg Med Chem Lett (2004) 14 : 5591 -5594
PubMed 15482930 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 6.90 7.32

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL187637 1 7.32
CHEMBL360202 1 7.24
CHEMBL186125 1 7.17
CHEMBL185825 1 7.05
CHEMBL444083 1 7.05
CHEMBL187264 1 7.02
CHEMBL185905 1 6.73
CHEMBL188021 1 6.71
CHEMBL425358 1 6.67
CHEMBL93 ZILEUTON 4.0 1 6.06

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL187637 IC50 = 48.0 nM 7.32
CHEMBL360202 IC50 = 57.0 nM 7.24
CHEMBL186125 IC50 = 68.0 nM 7.17
CHEMBL185825 IC50 = 90.0 nM 7.05
CHEMBL444083 IC50 = 89.0 nM 7.05
CHEMBL187264 IC50 = 96.0 nM 7.02
CHEMBL185905 IC50 = 185.0 nM 6.73
CHEMBL188021 IC50 = 194.0 nM 6.71
CHEMBL425358 IC50 = 213.0 nM 6.67
CHEMBL93 ZILEUTON IC50 = 873.0 nM 6.06