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Assay Detail

CHEMBL619397

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

Binding
Inhibition of rat neutrophil 5- Lipoxygenase (5-LO)
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Substituted arylmethyl phenyl ethers. 1. A novel series of 5-lipoxygenase inhibitors and leukotriene antagonists.
Musser JH, Chakraborty UR, Sciortino S, Gordon RJ, Khandwala A, Neiss ES, Pruss TP, Van Inwegen R, Weinryb I, Coutts SM.
J Med Chem (1987) 30 : 96 -104
PubMed 3806607 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 5.99 6.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL8747 REV-5901 1 6.92
CHEMBL8384 1 6.89
CHEMBL8549 1 6.43
CHEMBL8440 1 6.37
CHEMBL594621 ICOMUCRET 2.0 1 5.84
CHEMBL8841 1 5.72
CHEMBL274852 1 5.70
CHEMBL8257 1 5.40
CHEMBL8622 1 5.40
CHEMBL8797 1 5.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL8747 REV-5901 IC50 = 120.0 nM 6.92
CHEMBL8384 IC50 = 130.0 nM 6.89
CHEMBL8549 IC50 = 370.0 nM 6.43
CHEMBL8440 IC50 = 430.0 nM 6.37
CHEMBL594621 ICOMUCRET IC50 = 1450.0 nM 5.84
CHEMBL8841 IC50 = 1900.0 nM 5.72
CHEMBL274852 IC50 = 2000.0 nM 5.70
CHEMBL8257 IC50 = 4000.0 nM 5.40
CHEMBL8622 IC50 = 4000.0 nM 5.40
CHEMBL8797 IC50 = 6000.0 nM 5.22