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Assay Detail

CHEMBL620873

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

Binding
5-lipoxygenase Inhibitory activity was measured by enzyme immunoassay using human whole blood stimulated with calcium ionophore (A23187) and LTB4 (leukotriene B4)
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Blood
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

(R)-(+)-N-[3-[5-[(4-fluorophenyl)methyl]-2-thienyl]-1-methyl- 2-propynyl]-N-hydroxyurea (ABT-761), a second-generation 5-lipoxygenase inhibitor.
Brooks CD, Stewart AO, Basha A, Bhatia P, Ratajczyk JD, Martin JG, Craig RA, Kolasa T, Bouska JB, Lanni C.
J Med Chem (1995) 38 : 4768 -4775
PubMed 7490726 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 6.87 7.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1907933 1 7.30
CHEMBL264717 1 7.22
CHEMBL90552 1 7.10
CHEMBL59598 1 7.10
CHEMBL145318 1 6.80
CHEMBL59356 ATRELEUTON 2.0 1 6.80
CHEMBL144028 1 6.70
CHEMBL145306 1 6.70
CHEMBL93 ZILEUTON 4.0 1 6.13

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1907933 IC50 = 50.0 nM 7.30
CHEMBL264717 IC50 = 60.0 nM 7.22
CHEMBL90552 IC50 = 80.0 nM 7.10
CHEMBL59598 IC50 = 80.0 nM 7.10
CHEMBL145318 IC50 = 160.0 nM 6.80
CHEMBL59356 ATRELEUTON IC50 = 160.0 nM 6.80
CHEMBL144028 IC50 = 200.0 nM 6.70
CHEMBL145306 IC50 = 200.0 nM 6.70
CHEMBL93 ZILEUTON IC50 = 740.0 nM 6.13