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Assay Detail

CHEMBL3871561

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

Binding
Inhibition of MPO chlorination activity (unknown origin) assessed as taurine chloramine formation after 5 mins in presence of H2O2/Cl- by HTS method
39
Total Activities
39
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

Novel bis-arylalkylamines as myeloperoxidase inhibitors: Design, synthesis, and structure-activity relationship study.
Aldib I, Gelbcke M, Soubhye J, Prévost M, Furtmüller PG, Obinger C, Elfving B, Alard IC, Roos G, Delporte C, Berger G, Dufour D, Zouaoui Boudjeltia K, Nève J, Dufrasne F, Van Antwerpen P.
Eur J Med Chem (2016) 123 : 746 -762
PubMed 27537923 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 39 6.32 7.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2347165 1 7.89
CHEMBL3933129 1 7.27
CHEMBL3929246 1 7.07
CHEMBL3960919 1 6.57
CHEMBL3920217 1 6.46
CHEMBL3892909 1 6.44
CHEMBL3910108 1 6.43
CHEMBL3899797 1 6.43
CHEMBL3980103 1 6.31
CHEMBL1370773 1 6.30
CHEMBL3919858 1 6.19
CHEMBL3890813 1 6.18
CHEMBL3980225 1 6.17
CHEMBL3925807 1 6.16
CHEMBL3981926 1 6.16
CHEMBL3972038 1 5.94
CHEMBL3953437 1 5.92
CHEMBL3956919 1 5.85
CHEMBL3947640 1 5.73
CHEMBL3938850 1 5.60
CHEMBL3901888 1 5.57
CHEMBL3924941 1 -
CHEMBL3929827 1 -
CHEMBL3086915 1 -
CHEMBL3086916 1 -
CHEMBL3951169 1 -
CHEMBL3932693 1 -
CHEMBL3904692 1 -
CHEMBL3943673 1 -
CHEMBL162522 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2347165 IC50 = 13.0 nM 7.89
CHEMBL3933129 IC50 = 54.0 nM 7.27
CHEMBL3929246 IC50 = 85.0 nM 7.07
CHEMBL3960919 IC50 = 270.0 nM 6.57
CHEMBL3920217 IC50 = 350.0 nM 6.46
CHEMBL3892909 IC50 = 360.0 nM 6.44
CHEMBL3910108 IC50 = 370.0 nM 6.43
CHEMBL3899797 IC50 = 370.0 nM 6.43
CHEMBL3980103 IC50 = 490.0 nM 6.31
CHEMBL1370773 IC50 = 500.0 nM 6.30
CHEMBL3919858 IC50 = 650.0 nM 6.19
CHEMBL3890813 IC50 = 660.0 nM 6.18
CHEMBL3980225 IC50 = 670.0 nM 6.17
CHEMBL3925807 IC50 = 700.0 nM 6.16
CHEMBL3981926 IC50 = 700.0 nM 6.16
CHEMBL3972038 IC50 = 1160.0 nM 5.94
CHEMBL3953437 IC50 = 1200.0 nM 5.92
CHEMBL3956919 IC50 = 1400.0 nM 5.85
CHEMBL3947640 IC50 = 1850.0 nM 5.73
CHEMBL3938850 IC50 = 2500.0 nM 5.60
CHEMBL3901888 IC50 = 2700.0 nM 5.57
CHEMBL162522 IC50 > 10000.0 nM -
CHEMBL3920922 IC50 - -
CHEMBL3911982 IC50 - -
CHEMBL3933465 IC50 - -
CHEMBL3221060 IC50 - -
CHEMBL1618762 IC50 - -
CHEMBL3970959 IC50 - -
CHEMBL3942433 IC50 - -
CHEMBL3938741 IC50 > 10000.0 nM -
CHEMBL3138959 IC50 > 10000.0 nM -
CHEMBL3943673 IC50 > 10000.0 nM -
CHEMBL3904692 IC50 > 10000.0 nM -
CHEMBL3932693 IC50 > 10000.0 nM -
CHEMBL3951169 IC50 - -
CHEMBL3086916 IC50 - -
CHEMBL3086915 IC50 - -
CHEMBL3929827 IC50 - -
CHEMBL3924941 IC50 - -