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Assay Detail

CHEMBL2352940

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

Binding
Inhibition of human recombinant MPO-mediated taurine chlorination after 5 mins by microplate assay
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Tissue Urine
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Myeloperoxidase (CHEMBL2439)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, synthesis, and structure-activity relationship studies of novel 3-alkylindole derivatives as selective and highly potent myeloperoxidase inhibitors.
Soubhye J, Aldib I, Elfving B, Gelbcke M, Furtmüller PG, Podrecca M, Conotte R, Colet JM, Rousseau A, Reye F, Sarakbi A, Vanhaeverbeek M, Kauffmann JM, Obinger C, Nève J, Prévost M, Zouaoui Boudjeltia K, Dufrasne F, Van Antwerpen P.
J Med Chem (2013) 56 : 3943 -3958
PubMed 23581551 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 34 7.57 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2347170 1 8.52
CHEMBL2347168 1 8.40
CHEMBL2347177 1 8.30
CHEMBL2347032 1 8.22
CHEMBL2347166 1 8.00
CHEMBL2347167 1 8.00
CHEMBL2347176 1 7.96
CHEMBL2347165 1 7.89
CHEMBL2346670 1 7.85
CHEMBL2347181 1 7.75
CHEMBL2347034 1 7.66
CHEMBL2347030 1 7.62
CHEMBL2347024 1 7.58
CHEMBL205229 1 7.54
CHEMBL2347027 1 7.47
CHEMBL2347169 1 7.46
CHEMBL2347175 1 7.43
CHEMBL2347026 1 7.41
CHEMBL2347028 1 7.40
CHEMBL2347178 1 7.22
CHEMBL2347179 1 7.20
CHEMBL2347025 1 6.88
CHEMBL2347029 1 6.74
CHEMBL2347182 1 6.57
CHEMBL6640 TRYPTAMINE 1 6.11
CHEMBL39 SEROTONIN 3.0 1 -
CHEMBL925 TYROSINE 4.0 1 -
CHEMBL2347171 1 -
CHEMBL2347172 1 -
CHEMBL2347033 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2347170 IC50 = 3.0 nM 8.52
CHEMBL2347168 IC50 = 4.0 nM 8.40
CHEMBL2347177 IC50 = 5.0 nM 8.30
CHEMBL2347032 IC50 = 6.0 nM 8.22
CHEMBL2347166 IC50 = 10.0 nM 8.00
CHEMBL2347167 IC50 = 10.0 nM 8.00
CHEMBL2347176 IC50 = 11.0 nM 7.96
CHEMBL2347165 IC50 = 13.0 nM 7.89
CHEMBL2346670 IC50 = 14.0 nM 7.85
CHEMBL2347181 IC50 = 18.0 nM 7.75
CHEMBL2347034 IC50 = 22.0 nM 7.66
CHEMBL2347030 IC50 = 24.0 nM 7.62
CHEMBL2347024 IC50 = 26.0 nM 7.58
CHEMBL205229 IC50 = 29.0 nM 7.54
CHEMBL2347027 IC50 = 34.0 nM 7.47
CHEMBL2347169 IC50 = 35.0 nM 7.46
CHEMBL2347175 IC50 = 37.0 nM 7.43
CHEMBL2347026 IC50 = 39.0 nM 7.41
CHEMBL2347028 IC50 = 40.0 nM 7.40
CHEMBL2347178 IC50 = 60.0 nM 7.22
CHEMBL2347179 IC50 = 63.0 nM 7.20
CHEMBL2347025 IC50 = 132.0 nM 6.88
CHEMBL2347029 IC50 = 182.0 nM 6.74
CHEMBL2347182 IC50 = 271.0 nM 6.57
CHEMBL6640 TRYPTAMINE IC50 = 770.0 nM 6.11
CHEMBL39 SEROTONIN IC50 - -
CHEMBL925 TYROSINE IC50 - -
CHEMBL2347171 IC50 > 100.0 nM -
CHEMBL2347172 IC50 > 100.0 nM -
CHEMBL2347033 IC50 - -
CHEMBL2347173 IC50 > 100.0 nM -
CHEMBL2347031 IC50 - -
CHEMBL2347174 IC50 > 100.0 nM -
CHEMBL2347180 IC50 - -