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Assay Detail

CHEMBL702328

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

Functional
Compound was evaluated for production of leukotriene B4 in human whole blood (HWB) activated with ionophore A-23187.
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Tissue Blood
Confidence 1 — Organism
Curated By Intermediate

Target

Homo sapiens (CHEMBL372)
Type ORGANISM
Organism Homo sapiens

Publication

Substituted (pyridylmethoxy)naphthalenes as potent and orally active 5-lipoxygenase inhibitors; synthesis, biological profile, and pharmacokinetics of L-739,010.
Hamel P, Riendeau D, Brideau C, Chan CC, Desmarais S, Delorme D, Dubé D, Ducharme Y, Ethier D, Grimm E, Falgueyret JP, Guay J, Jones TR, Kwong E, McAuliffe M, McFarlane CS, Piechuta H, Roumi M, Tagari P, Young RN, Girard Y.
J Med Chem (1997) 40 : 2866 -2875
PubMed 9288168 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 6.94 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL99469 1 8.00
CHEMBL99217 1 7.52
CHEMBL278293 1 7.38
CHEMBL99942 1 7.30
CHEMBL95470 1 7.17
CHEMBL316641 1 7.00
CHEMBL97380 1 6.82
CHEMBL97923 1 6.60
CHEMBL418775 1 6.52
CHEMBL16596 QUIFLAPON 2.0 1 6.30
CHEMBL93 ZILEUTON 4.0 1 5.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL99469 IC50 = 10.0 nM 8.00
CHEMBL99217 IC50 = 30.0 nM 7.52
CHEMBL278293 IC50 = 42.0 nM 7.38
CHEMBL99942 IC50 = 50.0 nM 7.30
CHEMBL95470 IC50 = 67.0 nM 7.17
CHEMBL316641 IC50 = 100.0 nM 7.00
CHEMBL97380 IC50 = 150.0 nM 6.82
CHEMBL97923 IC50 = 250.0 nM 6.60
CHEMBL418775 IC50 = 300.0 nM 6.52
CHEMBL16596 QUIFLAPON IC50 = 500.0 nM 6.30
CHEMBL93 ZILEUTON IC50 = 2000.0 nM 5.70