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Assay Detail

CHEMBL619878

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

Functional
In vitro 5-lipoxygenase inhibitory activity against calcium ionophore (A23187) induced LTB4 formation in human polymorphonuclear leukocytes.
38
Total Activities
37
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Polyunsaturated fatty acid 5-lipoxygenase (CHEMBL215)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

5-Lipoxygenase inhibitors: synthesis and structure-activity relationships of a series of 1-aryl-2H,4H-tetrahydro-1,2,4-triazin-3-ones.
Bhatia PA, Brooks CD, Basha A, Ratajczyk JD, Gunn BP, Bouska JB, Lanni C, Young PR, Bell RL, Carter GW.
J Med Chem (1996) 39 : 3938 -3950
PubMed 8831760 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 38 5.38 6.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL127109 1 6.70
CHEMBL30110 1 6.00
CHEMBL7660 PHENIDONE 1 5.89
CHEMBL129798 1 5.80
CHEMBL127110 1 5.77
CHEMBL341363 1 5.75
CHEMBL128663 1 5.70
CHEMBL126290 1 5.68
CHEMBL127719 1 5.66
CHEMBL129701 1 5.58
CHEMBL341291 1 5.58
CHEMBL126672 1 5.57
CHEMBL128138 1 5.52
CHEMBL129260 1 5.51
CHEMBL129799 1 5.46
CHEMBL339537 1 5.44
CHEMBL128308 1 5.42
CHEMBL340784 1 5.34
CHEMBL128429 1 5.34
CHEMBL128758 1 5.32
CHEMBL126183 1 5.32
CHEMBL339239 1 5.28
CHEMBL129506 1 5.28
CHEMBL126135 1 5.26
CHEMBL340341 2 5.24
CHEMBL129818 1 5.24
CHEMBL129428 1 5.22
CHEMBL338785 1 5.15
CHEMBL129441 1 5.10
CHEMBL128657 1 5.08

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL127109 IC50 = 200.0 nM 6.70
CHEMBL30110 IC50 = 1000.0 nM 6.00
CHEMBL7660 PHENIDONE IC50 = 1300.0 nM 5.89
CHEMBL129798 IC50 = 1600.0 nM 5.80
CHEMBL127110 IC50 = 1700.0 nM 5.77
CHEMBL341363 IC50 = 1800.0 nM 5.75
CHEMBL128663 IC50 = 2000.0 nM 5.70
CHEMBL126290 IC50 = 2100.0 nM 5.68
CHEMBL127719 IC50 = 2200.0 nM 5.66
CHEMBL129701 IC50 = 2600.0 nM 5.58
CHEMBL341291 IC50 = 2600.0 nM 5.58
CHEMBL126672 IC50 = 2700.0 nM 5.57
CHEMBL128138 IC50 = 3000.0 nM 5.52
CHEMBL129260 IC50 = 3100.0 nM 5.51
CHEMBL129799 IC50 = 3500.0 nM 5.46
CHEMBL339537 IC50 = 3600.0 nM 5.44
CHEMBL128308 IC50 = 3800.0 nM 5.42
CHEMBL340784 IC50 = 4600.0 nM 5.34
CHEMBL128429 IC50 = 4600.0 nM 5.34
CHEMBL128758 IC50 = 4800.0 nM 5.32
CHEMBL126183 IC50 = 4800.0 nM 5.32
CHEMBL339239 IC50 = 5300.0 nM 5.28
CHEMBL129506 IC50 = 5200.0 nM 5.28
CHEMBL126135 IC50 = 5500.0 nM 5.26
CHEMBL340341 IC50 = 5800.0 nM 5.24
CHEMBL129818 IC50 = 5800.0 nM 5.24
CHEMBL129428 IC50 = 6000.0 nM 5.22
CHEMBL338785 IC50 = 7100.0 nM 5.15
CHEMBL129441 IC50 = 7900.0 nM 5.10
CHEMBL128657 IC50 = 8400.0 nM 5.08
CHEMBL127107 IC50 = 8600.0 nM 5.07
CHEMBL129344 IC50 = 8800.0 nM 5.06
CHEMBL340341 IC50 = 9200.0 nM 5.04
CHEMBL126191 IC50 = 13000.0 nM 4.89
CHEMBL340927 IC50 = 20000.0 nM 4.70
CHEMBL128869 IC50 = 24000.0 nM 4.62
CHEMBL129325 IC50 = 37000.0 nM 4.43
CHEMBL126949 IC50 > 50000.0 nM -