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Assay Detail

CHEMBL824877

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

Functional
Inhibition of 5-lipoxygenase mediated LTB4 synthesis in A-23187 simulated human whole blood
9
Total Activities
9
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

5-Lipoxygenase inhibitors: convenient synthesis of 4-[3-(4-heterocyclylphenylthio)phenyl]-3,4,5,6-tetrahydro-2H-pyran-4-carboxamide analogues.
Mano T, Stevens RW, Okumura Y, Kawai M, Okumura T, Sakakibara M.
Bioorg Med Chem Lett (2005) 15 : 2611 -2615
PubMed 15863327 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 6.44 6.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL191859 1 6.85
CHEMBL427532 1 6.82
CHEMBL195309 1 6.64
CHEMBL362978 1 6.57
CHEMBL192207 1 6.08
CHEMBL195206 1 5.70
CHEMBL191621 1 -
CHEMBL370268 1 -
CHEMBL365166 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL191859 IC50 = 140.0 nM 6.85
CHEMBL427532 IC50 = 150.0 nM 6.82
CHEMBL195309 IC50 = 230.0 nM 6.64
CHEMBL362978 IC50 = 270.0 nM 6.57
CHEMBL192207 IC50 = 830.0 nM 6.08
CHEMBL195206 IC50 = 2000.0 nM 5.70
CHEMBL191621 IC50 > 1000.0 nM -
CHEMBL370268 IC50 > 1000.0 nM -
CHEMBL365166 IC50 > 1000.0 nM -