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Assay Detail

CHEMBL870099

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

Functional
Inhibition of LTB4 production in calcium ionophore A-23187-stimulated human whole blood
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
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

Substituted coumarins as potent 5-lipoxygenase inhibitors.
Grimm EL, Brideau C, Chauret N, Chan CC, Delorme D, Ducharme Y, Ethier D, Falgueyret JP, Friesen RW, Guay J, Hamel P, Riendeau D, Soucy-Breau C, Tagari P, Girard Y.
Bioorg Med Chem Lett (2006) 16 : 2528 -2531
PubMed 16464579 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 6.79 7.44

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL207057 1 7.44
CHEMBL207109 1 7.32
CHEMBL377094 1 7.28
CHEMBL205800 1 7.16
CHEMBL377821 1 7.06
CHEMBL204365 1 7.05
CHEMBL205189 1 6.82
CHEMBL204633 1 6.44
CHEMBL206632 1 6.40
CHEMBL205222 1 6.40
CHEMBL204781 1 6.36
CHEMBL204890 1 5.77
CHEMBL380473 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL207057 IC50 = 36.0 nM 7.44
CHEMBL207109 IC50 = 48.0 nM 7.32
CHEMBL377094 IC50 = 52.0 nM 7.28
CHEMBL205800 IC50 = 70.0 nM 7.16
CHEMBL377821 IC50 = 88.0 nM 7.06
CHEMBL204365 IC50 = 89.0 nM 7.05
CHEMBL205189 IC50 = 150.0 nM 6.82
CHEMBL204633 IC50 = 360.0 nM 6.44
CHEMBL206632 IC50 = 400.0 nM 6.40
CHEMBL205222 IC50 = 400.0 nM 6.40
CHEMBL204781 IC50 = 440.0 nM 6.36
CHEMBL204890 IC50 = 1700.0 nM 5.77
CHEMBL380473 IC50 - -