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Assay Detail

CHEMBL619227

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Binding
Inhibitory activity against 5-lipoxygenase (5-LO) using broken rat barophilic leukemia cells (RBL-1)
10
Total Activities
10
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 Expert

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 10 6.84 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL369848 1 8.00
CHEMBL175150 1 7.16
CHEMBL177727 1 7.16
CHEMBL175153 1 7.10
CHEMBL368682 1 7.00
CHEMBL366595 1 6.62
CHEMBL367010 1 6.57
CHEMBL174684 1 6.55
CHEMBL173939 1 6.43
CHEMBL264200 1 5.78

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL369848 IC50 = 10.0 nM 8.00
CHEMBL175150 IC50 = 70.0 nM 7.16
CHEMBL177727 IC50 = 70.0 nM 7.16
CHEMBL175153 IC50 = 80.0 nM 7.10
CHEMBL368682 IC50 = 100.0 nM 7.00
CHEMBL366595 IC50 = 240.0 nM 6.62
CHEMBL367010 IC50 = 270.0 nM 6.57
CHEMBL174684 IC50 = 280.0 nM 6.55
CHEMBL173939 IC50 = 370.0 nM 6.43
CHEMBL264200 IC50 = 1660.0 nM 5.78