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Assay Detail

CHEMBL887576

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

Binding
Inhibition of 5-LOX in rat peritoneal leukocytes
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

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

Publication

Indole derivatives as potent inhibitors of 5-lipoxygenase: design, synthesis, biological evaluation, and molecular modeling.
Zheng M, Zheng M, Ye D, Deng Y, Qiu S, Luo X, Chen K, Liu H, Jiang H.
Bioorg Med Chem Lett (2007) 17 : 2414 -2420
PubMed 17336065 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 5.69 6.13

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL230375 1 6.13
CHEMBL93 ZILEUTON 4.0 1 6.08
CHEMBL230483 1 6.07
CHEMBL388490 1 6.06
CHEMBL230922 1 6.02
CHEMBL389770 1 5.88
CHEMBL395709 1 5.69
CHEMBL230921 1 5.65
CHEMBL390665 1 5.62
CHEMBL230374 1 5.50
CHEMBL230604 1 5.50
CHEMBL230392 1 4.13

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL230375 IC50 = 740.0 nM 6.13
CHEMBL93 ZILEUTON IC50 = 830.0 nM 6.08
CHEMBL230483 IC50 = 850.0 nM 6.07
CHEMBL388490 IC50 = 870.0 nM 6.06
CHEMBL230922 IC50 = 950.0 nM 6.02
CHEMBL389770 IC50 = 1330.0 nM 5.88
CHEMBL395709 IC50 = 2060.0 nM 5.69
CHEMBL230921 IC50 = 2250.0 nM 5.65
CHEMBL390665 IC50 = 2380.0 nM 5.62
CHEMBL230374 IC50 = 3160.0 nM 5.50
CHEMBL230604 IC50 = 3170.0 nM 5.50
CHEMBL230392 IC50 = 74000.0 nM 4.13