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Assay Detail

CHEMBL3362097

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

Binding
Inhibition of partially purified recombinant 5-lipoxygenase (unknown origin) using arachidonic acid as substrate preincubated for 15 mins before substrate addition measured after 10 mins by HPLC analysis
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Multi-dimensional target profiling of N,4-diaryl-1,3-thiazole-2-amines as potent inhibitors of eicosanoid metabolism.
Rödl CB, Vogt D, Kretschmer SB, Ihlefeld K, Barzen S, Brüggerhoff A, Achenbach J, Proschak E, Steinhilber D, Stark H, Hofmann B.
Eur J Med Chem (2014) 84 : 302 -311
PubMed 25036790 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 30 6.43 7.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3318370 1 7.52
CHEMBL3318371 1 7.52
CHEMBL1076555 1 7.52
CHEMBL1081482 1 7.52
CHEMBL3318382 1 7.30
CHEMBL2023847 1 7.30
CHEMBL3318368 1 7.22
CHEMBL1081479 1 7.22
CHEMBL562493 1 7.00
CHEMBL3318381 1 6.52
CHEMBL3318369 1 6.40
CHEMBL1080391 1 6.40
CHEMBL3318373 1 6.40
CHEMBL3318379 1 6.40
CHEMBL1367191 1 6.40
CHEMBL3318380 1 6.40
CHEMBL3318383 1 6.30
CHEMBL3318378 1 6.30
CHEMBL3318374 1 6.22
CHEMBL3318384 1 6.22
CHEMBL3318377 1 6.22
CHEMBL68504 1 6.16
CHEMBL3318376 1 6.05
CHEMBL1372204 1 5.96
CHEMBL1087624 1 5.92
CHEMBL3318372 1 5.57
CHEMBL3318386 1 5.55
CHEMBL554135 1 5.43
CHEMBL3318385 1 5.17
CHEMBL3318375 1 4.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3318370 IC50 = 30.0 nM 7.52
CHEMBL3318371 IC50 = 30.0 nM 7.52
CHEMBL1076555 IC50 = 30.0 nM 7.52
CHEMBL1081482 IC50 = 30.0 nM 7.52
CHEMBL3318382 IC50 = 50.0 nM 7.30
CHEMBL2023847 IC50 = 50.0 nM 7.30
CHEMBL3318368 IC50 = 60.0 nM 7.22
CHEMBL1081479 IC50 = 60.0 nM 7.22
CHEMBL562493 IC50 = 100.0 nM 7.00
CHEMBL3318381 IC50 = 300.0 nM 6.52
CHEMBL3318369 IC50 = 400.0 nM 6.40
CHEMBL1080391 IC50 = 400.0 nM 6.40
CHEMBL3318373 IC50 = 400.0 nM 6.40
CHEMBL3318379 IC50 = 400.0 nM 6.40
CHEMBL1367191 IC50 = 400.0 nM 6.40
CHEMBL3318380 IC50 = 400.0 nM 6.40
CHEMBL3318383 IC50 = 500.0 nM 6.30
CHEMBL3318378 IC50 = 500.0 nM 6.30
CHEMBL3318374 IC50 = 600.0 nM 6.22
CHEMBL3318384 IC50 = 600.0 nM 6.22
CHEMBL3318377 IC50 = 600.0 nM 6.22
CHEMBL68504 IC50 = 700.0 nM 6.16
CHEMBL3318376 IC50 = 900.0 nM 6.05
CHEMBL1372204 IC50 = 1100.0 nM 5.96
CHEMBL1087624 IC50 = 1200.0 nM 5.92
CHEMBL3318372 IC50 = 2700.0 nM 5.57
CHEMBL3318386 IC50 = 2800.0 nM 5.55
CHEMBL554135 IC50 = 3700.0 nM 5.43
CHEMBL3318385 IC50 = 6700.0 nM 5.17
CHEMBL3318375 IC50 = 15300.0 nM 4.82