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Assay Detail

CHEMBL1817023

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

Binding
Inhibition of human platelet-type N-terminally His6-tagged 12-lipoxygenase assessed as conjugated diene product formation using arachidonic acid by UV-vis spectrophotometer analysis
38
Total Activities
34
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 lipoxygenase ALOX12 (CHEMBL3687)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of potent and selective inhibitors of human platelet-type 12- lipoxygenase.
Kenyon V, Rai G, Jadhav A, Schultz L, Armstrong M, Jameson JB, Perry S, Joshi N, Bougie JM, Leister W, Taylor-Fishwick DA, Nadler JL, Holinstat M, Simeonov A, Maloney DJ, Holman TR.
J Med Chem (2011) 54 : 5485 -5497
PubMed 21739938 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 38 5.75 6.42

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1405150 3 6.42
CHEMBL1573436 3 6.37
CHEMBL1369893 1 6.10
CHEMBL528045 1 6.00
CHEMBL580727 1 6.00
CHEMBL1531895 1 5.92
CHEMBL1532739 1 5.92
CHEMBL1487619 1 5.80
CHEMBL1200596 CHLOROXINE 4.0 1 5.72
CHEMBL1561166 1 5.70
CHEMBL1609517 1 5.70
CHEMBL1394624 1 5.70
CHEMBL1572233 1 5.58
CHEMBL1521956 1 5.52
CHEMBL1406616 1 5.52
CHEMBL1813492 1 5.52
CHEMBL1370513 1 5.47
CHEMBL1476391 1 5.46
CHEMBL1512403 1 5.30
CHEMBL1512078 1 4.85
CHEMBL1323844 1 -
CHEMBL1370315 1 -
CHEMBL1437477 1 -
CHEMBL1555876 1 -
CHEMBL1410433 1 -
CHEMBL1319062 1 -
CHEMBL1448145 1 -
CHEMBL1593604 1 -
CHEMBL1323467 1 -
CHEMBL1593083 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1405150 IC50 = 380.0 nM 6.42
CHEMBL1573436 IC50 = 430.0 nM 6.37
CHEMBL1369893 IC50 = 800.0 nM 6.10
CHEMBL1405150 IC50 = 1000.0 nM 6.00
CHEMBL528045 IC50 = 1000.0 nM 6.00
CHEMBL1573436 IC50 = 1000.0 nM 6.00
CHEMBL580727 IC50 = 1000.0 nM 6.00
CHEMBL1532739 IC50 = 1200.0 nM 5.92
CHEMBL1531895 IC50 = 1200.0 nM 5.92
CHEMBL1487619 IC50 = 1600.0 nM 5.80
CHEMBL1200596 CHLOROXINE IC50 = 1900.0 nM 5.72
CHEMBL1561166 IC50 = 2000.0 nM 5.70
CHEMBL1394624 IC50 = 2000.0 nM 5.70
CHEMBL1609517 IC50 = 2000.0 nM 5.70
CHEMBL1572233 IC50 = 2600.0 nM 5.58
CHEMBL1406616 IC50 = 3000.0 nM 5.52
CHEMBL1521956 IC50 = 3000.0 nM 5.52
CHEMBL1813492 IC50 = 3000.0 nM 5.52
CHEMBL1370513 IC50 = 3400.0 nM 5.47
CHEMBL1476391 IC50 = 3500.0 nM 5.46
CHEMBL1512403 IC50 = 5000.0 nM 5.30
CHEMBL1512078 IC50 = 14000.0 nM 4.85
CHEMBL1555876 IC50 > 50000.0 nM -
CHEMBL1405150 IC50 > 25000.0 nM -
CHEMBL1323844 IC50 > 150000.0 nM -
CHEMBL1573436 IC50 > 25000.0 nM -
CHEMBL1370315 IC50 > 75000.0 nM -
CHEMBL1437477 IC50 > 150000.0 nM -
CHEMBL1528315 IC50 > 75000.0 nM -
CHEMBL1528943 IC50 > 75000.0 nM -
CHEMBL1705387 IC50 > 25000.0 nM -
CHEMBL1813491 IC50 > 25000.0 nM -
CHEMBL1593083 IC50 > 50000.0 nM -
CHEMBL1323467 IC50 > 150000.0 nM -
CHEMBL1593604 IC50 > 75000.0 nM -
CHEMBL1448145 IC50 > 75000.0 nM -
CHEMBL1319062 IC50 > 75000.0 nM -
CHEMBL1410433 IC50 > 75000.0 nM -