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Assay Detail

CHEMBL618067

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

Binding
Inhibitory activity against 5-lipoxygenase (5-LO) in intact rat barophilic leukemia cells (RBL-1)
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type RBL-1
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Polyunsaturated fatty acid 5-lipoxygenase (CHEMBL312)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

N-hydroxyurea and hydroxamic acid inhibitors of cyclooxygenase and 5-lipoxygenase.
Connolly PJ, Wetter SK, Beers KN, Hamel SC, Chen RH, Wachter MP, Ansell J, Singer MM, Steber M, Ritchie DM, Argentieri DC.
Bioorg Med Chem Lett (1999) 9 : 979 -984
PubMed 10230624 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 5.63 6.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL316040 TEPOXALIN 2.0 1 6.82
CHEMBL368145 1 6.05
CHEMBL173009 1 5.75
CHEMBL368546 1 5.33
CHEMBL178896 1 5.29
CHEMBL435907 1 5.09
CHEMBL174501 1 5.06

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL316040 TEPOXALIN IC50 = 150.0 nM 6.82
CHEMBL368145 IC50 = 900.0 nM 6.05
CHEMBL173009 IC50 = 1800.0 nM 5.75
CHEMBL368546 IC50 = 4700.0 nM 5.33
CHEMBL178896 IC50 = 5100.0 nM 5.29
CHEMBL435907 IC50 = 8100.0 nM 5.09
CHEMBL174501 IC50 = 8700.0 nM 5.06