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Assay Detail

CHEMBL3636365

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

Binding
Inhibition of peroxidase activity of MPO isolated from human polynuclear leukocytes using Amplex Red as substrate assessed as formation of resorufin after 300 secs by spectrophotometric analysis
1
Total Activities
1
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

Myeloperoxidase (CHEMBL2439)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of 2-(6-(5-Chloro-2-methoxyphenyl)-4-oxo-2-thioxo-3,4-dihydropyrimidin-1(2H)-yl)acetamide (PF-06282999): A Highly Selective Mechanism-Based Myeloperoxidase Inhibitor for the Treatment of Cardiovascular Diseases.
Ruggeri RB, Buckbinder L, Bagley SW, Carpino PA, Conn EL, Dowling MS, Fernando DP, Jiao W, Kung DW, Orr ST, Qi Y, Rocke BN, Smith A, Warmus JS, Zhang Y, Bowles D, Widlicka DW, Eng H, Ryder T, Sharma R, Wolford A, Okerberg C, Walters K, Maurer TS, Zhang Y, Bonin PD, Spath SN, Xing G, Hepworth D, Ahn K, Kalgutkar AS.
J Med Chem (2015) 58 : 8513 -8528
PubMed 26509551 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 5.55 5.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1518 PROPYLTHIOURACIL 4.0 1 5.55

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1518 PROPYLTHIOURACIL IC50 = 2810.0 nM 5.55