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Assay Detail

CHEMBL618063

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

Binding
Inhibition of 5-lipoxygenase catalysis in rat basophilic leukemia (RBL) cells by measuring 5-HETE product formation
63
Total Activities
63
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

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 63 5.01 5.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL127109 1 5.96
CHEMBL340896 1 5.82
CHEMBL7660 PHENIDONE 1 5.72
CHEMBL129344 1 5.68
CHEMBL129260 1 5.62
CHEMBL129506 1 5.58
CHEMBL126672 1 5.57
CHEMBL126135 1 5.55
CHEMBL340784 1 5.46
CHEMBL129798 1 5.46
CHEMBL127110 1 5.42
CHEMBL339537 1 5.41
CHEMBL30110 1 5.37
CHEMBL128657 1 5.32
CHEMBL339239 1 5.31
CHEMBL128664 1 5.31
CHEMBL126290 1 5.28
CHEMBL129441 1 5.26
CHEMBL338785 1 5.26
CHEMBL126183 1 5.25
CHEMBL126191 1 5.22
CHEMBL126949 1 5.22
CHEMBL341363 1 5.20
CHEMBL129428 1 5.18
CHEMBL340927 1 5.17
CHEMBL129531 1 5.17
CHEMBL128308 1 5.16
CHEMBL129325 1 5.09
CHEMBL128758 1 5.08
CHEMBL341057 1 5.08

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL127109 IC50 = 1100.0 nM 5.96
CHEMBL340896 IC50 = 1500.0 nM 5.82
CHEMBL7660 PHENIDONE IC50 = 1900.0 nM 5.72
CHEMBL129344 IC50 = 2100.0 nM 5.68
CHEMBL129260 IC50 = 2400.0 nM 5.62
CHEMBL129506 IC50 = 2600.0 nM 5.58
CHEMBL126672 IC50 = 2700.0 nM 5.57
CHEMBL126135 IC50 = 2800.0 nM 5.55
CHEMBL340784 IC50 = 3500.0 nM 5.46
CHEMBL129798 IC50 = 3500.0 nM 5.46
CHEMBL127110 IC50 = 3800.0 nM 5.42
CHEMBL339537 IC50 = 3900.0 nM 5.41
CHEMBL30110 IC50 = 4300.0 nM 5.37
CHEMBL128657 IC50 = 4800.0 nM 5.32
CHEMBL128664 IC50 = 4900.0 nM 5.31
CHEMBL339239 IC50 = 4900.0 nM 5.31
CHEMBL126290 IC50 = 5300.0 nM 5.28
CHEMBL129441 IC50 = 5500.0 nM 5.26
CHEMBL338785 IC50 = 5500.0 nM 5.26
CHEMBL126183 IC50 = 5600.0 nM 5.25
CHEMBL126191 IC50 = 6000.0 nM 5.22
CHEMBL126949 IC50 = 6000.0 nM 5.22
CHEMBL341363 IC50 = 6300.0 nM 5.20
CHEMBL129428 IC50 = 6600.0 nM 5.18
CHEMBL129531 IC50 = 6800.0 nM 5.17
CHEMBL340927 IC50 = 6800.0 nM 5.17
CHEMBL128308 IC50 = 6900.0 nM 5.16
CHEMBL129325 IC50 = 8200.0 nM 5.09
CHEMBL128758 IC50 = 8400.0 nM 5.08
CHEMBL341057 IC50 = 8300.0 nM 5.08
CHEMBL128429 IC50 = 8900.0 nM 5.05
CHEMBL128138 IC50 = 9100.0 nM 5.04
CHEMBL129799 IC50 = 9500.0 nM 5.02
CHEMBL129818 IC50 = 11000.0 nM 4.96
CHEMBL338350 IC50 = 12000.0 nM 4.92
CHEMBL129670 IC50 = 13000.0 nM 4.89
CHEMBL127719 IC50 = 14000.0 nM 4.85
CHEMBL128869 IC50 = 14000.0 nM 4.85
CHEMBL128663 IC50 = 15000.0 nM 4.82
CHEMBL341253 IC50 = 17000.0 nM 4.77
CHEMBL126910 IC50 = 19000.0 nM 4.72
CHEMBL126950 IC50 = 19000.0 nM 4.72
CHEMBL340341 IC50 = 21000.0 nM 4.68
CHEMBL129154 IC50 = 22000.0 nM 4.66
CHEMBL127107 IC50 = 26000.0 nM 4.58
CHEMBL126460 IC50 = 30000.0 nM 4.52
CHEMBL129369 IC50 = 30000.0 nM 4.52
CHEMBL6415 IC50 = 32000.0 nM 4.50
CHEMBL340385 IC50 = 32000.0 nM 4.50
CHEMBL128236 IC50 = 32000.0 nM 4.50