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Assay Detail

CHEMBL4839675

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

Binding
Inhibition of wild type human N-terminal His-tagged 12-LOX using arachidonic acid as substrate by UV-Vis spectroscopy analysis
2
Total Activities
2
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

Docking and mutagenesis studies lead to improved inhibitor development of ML355 for human platelet 12-lipoxygenase.
Tsai WC, Aleem AM, Tena J, Rivera-Velazquez M, Brah HS, Tripathi S, D'silva M, Nadler JL, Kalyanaraman C, Jacobson MP, Holman T.
Bioorg Med Chem (2021) 46 : 116347 -116347
PubMed 34507163 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 6.87 7.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4869861 1 7.30
CHEMBL3113165 VLX-1005 2.0 1 6.44

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4869861 IC50 = 50.0 nM 7.30
CHEMBL3113165 VLX-1005 IC50 = 360.0 nM 6.44