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Assay Detail

CHEMBL1817022

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Binding
Inhibition of human platelet-type 12-lipoxygenase
5
Total Activities
5
Compounds Tested
2
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 4 5.73 6.96
Ki 1 5.80 5.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL52 NORDIHYDROGUAIARETIC ACID 1 6.96
CHEMBL8260 BAICALEIN 2.0 1 5.80
CHEMBL362761 1 5.75
CHEMBL184398 1 5.30
CHEMBL381149 1 4.91

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL52 NORDIHYDROGUAIARETIC ACID IC50 = 110.0 nM 6.96
CHEMBL8260 BAICALEIN Ki = 1600.0 nM 5.80
CHEMBL362761 IC50 = 1800.0 nM 5.75
CHEMBL184398 IC50 = 5000.0 nM 5.30
CHEMBL381149 IC50 = 12300.0 nM 4.91