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Assay Detail

CHEMBL618012

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

Binding
Potency to inhibit oxidation of arachidonic acid by recombinant human 5-lipoxygenase
ChEMBL ↗
53
Total Activities
52
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Dioxabicyclooctanyl naphthalenenitriles as nonredox 5-lipoxygenase inhibitors: structure-activity relationship study directed toward the improvement of metabolic stability.
Delorme D, Ducharme Y, Brideau C, Chan CC, Chauret N, Desmarais S, Dubé D, Falgueyret JP, Fortin R, Guay J, Hamel P, Jones TR, Lépine C, Li C, McAuliffe M, McFarlane CS, Nicoll-Griffith DA, Riendeau D, Yergey JA, Girard Y.
J Med Chem (1996) 39 : 3951 -3970
PubMed 8831761 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 53 6.59 7.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL129292 — — 1 7.85
CHEMBL131135 — — 1 7.64
CHEMBL129018 — — 1 7.58
CHEMBL339993 — — 1 7.57
CHEMBL99469 — — 1 7.52
CHEMBL127779 — — 1 7.30
CHEMBL128300 — — 1 7.30
CHEMBL338461 — — 1 7.16
CHEMBL129056 — — 1 7.16
CHEMBL414244 — — 1 7.16
CHEMBL338132 — — 1 7.10
CHEMBL434057 — — 1 7.10
CHEMBL129478 — — 1 6.94
CHEMBL340737 — — 1 6.92
CHEMBL129916 — — 1 6.92
CHEMBL129167 — — 1 6.92
CHEMBL128821 — — 1 6.89
CHEMBL414375 — — 1 6.85
CHEMBL339970 — — 1 6.85
CHEMBL128238 — — 2 6.85
CHEMBL436595 — — 1 6.80
CHEMBL128751 — — 1 6.75
CHEMBL97380 — — 1 6.72
CHEMBL128105 — — 1 6.72
CHEMBL129253 — — 1 6.62
CHEMBL128666 — — 1 6.58
CHEMBL340795 — — 1 6.55
CHEMBL128143 — — 1 6.50
CHEMBL20403 ZD-2138 — 1 6.48
CHEMBL129517 — — 1 6.44

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL129292 — IC50 = 14.0 nM 7.85
CHEMBL131135 — IC50 = 23.0 nM 7.64
CHEMBL129018 — IC50 = 26.0 nM 7.58
CHEMBL339993 — IC50 = 27.0 nM 7.57
CHEMBL99469 — IC50 = 30.0 nM 7.52
CHEMBL127779 — IC50 = 50.0 nM 7.30
CHEMBL128300 — IC50 = 50.0 nM 7.30
CHEMBL338461 — IC50 = 70.0 nM 7.16
CHEMBL129056 — IC50 = 70.0 nM 7.16
CHEMBL414244 — IC50 = 70.0 nM 7.16
CHEMBL338132 — IC50 = 80.0 nM 7.10
CHEMBL434057 — IC50 = 80.0 nM 7.10
CHEMBL129478 — IC50 = 115.0 nM 6.94
CHEMBL129916 — IC50 = 120.0 nM 6.92
CHEMBL340737 — IC50 = 120.0 nM 6.92
CHEMBL129167 — IC50 = 120.0 nM 6.92
CHEMBL128821 — IC50 = 130.0 nM 6.89
CHEMBL414375 — IC50 = 140.0 nM 6.85
CHEMBL339970 — IC50 = 140.0 nM 6.85
CHEMBL128238 — IC50 = 140.0 nM 6.85
CHEMBL436595 — IC50 = 160.0 nM 6.80
CHEMBL128751 — IC50 = 180.0 nM 6.75
CHEMBL97380 — IC50 = 190.0 nM 6.72
CHEMBL128105 — IC50 = 190.0 nM 6.72
CHEMBL129253 — IC50 = 240.0 nM 6.62
CHEMBL128666 — IC50 = 260.0 nM 6.58
CHEMBL340795 — IC50 = 280.0 nM 6.55
CHEMBL128143 — IC50 = 320.0 nM 6.50
CHEMBL20403 ZD-2138 IC50 = 330.0 nM 6.48
CHEMBL128238 — IC50 = 340.0 nM 6.47
CHEMBL129517 — IC50 = 360.0 nM 6.44
CHEMBL340333 — IC50 = 380.0 nM 6.42
CHEMBL129351 — IC50 = 390.0 nM 6.41
CHEMBL128094 — IC50 = 400.0 nM 6.40
CHEMBL129669 — IC50 = 520.0 nM 6.28
CHEMBL129566 — IC50 = 640.0 nM 6.19
CHEMBL340805 — IC50 = 720.0 nM 6.14
CHEMBL128716 — IC50 = 760.0 nM 6.12
CHEMBL420145 — IC50 = 810.0 nM 6.09
CHEMBL130963 — IC50 = 1200.0 nM 5.92
CHEMBL338549 — IC50 = 1300.0 nM 5.89
CHEMBL339953 — IC50 = 1500.0 nM 5.82
CHEMBL340957 — IC50 = 2200.0 nM 5.66
CHEMBL128793 — IC50 = 3000.0 nM 5.52
CHEMBL93 ZILEUTON IC50 = 3700.0 nM 5.43
CHEMBL16596 QUIFLAPON IC50 = 5000.0 nM 5.30
CHEMBL421447 — IC50 = 5500.0 nM 5.26
CHEMBL338489 — IC50 = 6000.0 nM 5.22
CHEMBL129111 — IC50 > 6000.0 nM -
CHEMBL128271 — IC50 > 6000.0 nM -