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Assay Detail

CHEMBL615630

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Binding
Inhibitory concentration against 5-lipoxygenase from human whole blood
11
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

Conformational analysis of 5-lipoxygenase inhibitors: role of the substituents in chiral recognition and on the active conformations of the (methoxyalkyl)thiazole and methoxytetrahydropyran series.
Lambert-van der Brempt C, Bruneau P, Lamorlette MA, Foster SJ.
J Med Chem (1994) 37 : 113 -124
PubMed 8289184 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 6.45 7.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL21651 1 7.16
CHEMBL283559 1 6.96
CHEMBL21880 1 6.66
CHEMBL20599 1 6.48
CHEMBL440461 1 6.47
CHEMBL442334 1 6.39
CHEMBL277035 2 6.30
CHEMBL418742 1 6.28
CHEMBL21987 1 5.35
CHEMBL21242 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL21651 IC50 = 70.0 nM 7.16
CHEMBL283559 IC50 = 110.0 nM 6.96
CHEMBL21880 IC50 = 220.0 nM 6.66
CHEMBL20599 IC50 = 330.0 nM 6.48
CHEMBL440461 IC50 = 340.0 nM 6.47
CHEMBL442334 IC50 = 410.0 nM 6.39
CHEMBL277035 IC50 = 500.0 nM 6.30
CHEMBL418742 IC50 = 520.0 nM 6.28
CHEMBL21987 IC50 = 4500.0 nM 5.35
CHEMBL21242 IC50 > 10000.0 nM -
CHEMBL277035 IC50 > 40000.0 nM -