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Assay Detail

CHEMBL5326510

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

Binding
Inhibition of recombinant Trypanosoma cruzi Cruzipain using Z-Phe-Arg-AMC as substrate preincubated for 5 mins followed by substrate addition by spectrofluorometry analysis
ChEMBL ↗
34
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Trypanosoma cruzi
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Cruzipain (CHEMBL3563) ↗
Type SINGLE PROTEIN
Organism Trypanosoma cruzi

Publication

Design, synthesis and biological evaluation of novel thiosemicarbazones as cruzipain inhibitors.
Jasinski G, Salas-Sarduy E, Vega D, Fabian L, Florencia Martini M, Moglioni AG.
Eur J Med Chem (2023) 254 : 115345 -115345
PubMed 37054562 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 34 6.53 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL93166 — — 2 7.70
CHEMBL92099 — — 2 7.61
CHEMBL90512 — — 2 7.30
CHEMBL92376 — — 2 7.30
CHEMBL89973 — — 2 7.22
CHEMBL88734 — — 2 6.96
CHEMBL330050 — — 2 6.77
CHEMBL313679 — — 2 6.75
CHEMBL90866 — — 2 6.66
CHEMBL90772 — — 2 6.50
CHEMBL415311 — — 2 6.34
CHEMBL90688 — — 2 6.32
CHEMBL421363 — — 2 6.25
CHEMBL91844 — — 2 5.89
CHEMBL323975 — — 2 5.30
CHEMBL108035 — — 2 5.10
CHEMBL109893 — — 2 5.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL93166 — IC50 = 20.0 nM 7.70
CHEMBL93166 — IC50 = 20.0 nM 7.70
CHEMBL92099 — IC50 = 24.5 nM 7.61
CHEMBL92099 — IC50 = 24.49 nM 7.61
CHEMBL92376 — IC50 = 50.0 nM 7.30
CHEMBL90512 — IC50 = 50.0 nM 7.30
CHEMBL90512 — IC50 = 50.0 nM 7.30
CHEMBL92376 — IC50 = 50.0 nM 7.30
CHEMBL89973 — IC50 = 60.0 nM 7.22
CHEMBL89973 — IC50 = 59.98 nM 7.22
CHEMBL88734 — IC50 = 109.5 nM 6.96
CHEMBL88734 — IC50 = 109.65 nM 6.96
CHEMBL330050 — IC50 = 170.0 nM 6.77
CHEMBL330050 — IC50 = 169.82 nM 6.77
CHEMBL313679 — IC50 = 176.1 nM 6.75
CHEMBL313679 — IC50 = 176.2 nM 6.75
CHEMBL90866 — IC50 = 219.79 nM 6.66
CHEMBL90866 — IC50 = 220.0 nM 6.66
CHEMBL90772 — IC50 = 320.0 nM 6.50
CHEMBL90772 — IC50 = 319.89 nM 6.50
CHEMBL415311 — IC50 = 460.0 nM 6.34
CHEMBL415311 — IC50 = 460.26 nM 6.34
CHEMBL90688 — IC50 = 479.73 nM 6.32
CHEMBL90688 — IC50 = 480.0 nM 6.32
CHEMBL421363 — IC50 = 559.76 nM 6.25
CHEMBL421363 — IC50 = 560.0 nM 6.25
CHEMBL91844 — IC50 = 1300.0 nM 5.89
CHEMBL91844 — IC50 = 1300.17 nM 5.89
CHEMBL323975 — IC50 = 5000.0 nM 5.30
CHEMBL323975 — IC50 = 5000.35 nM 5.30
CHEMBL108035 — IC50 = 8000.0 nM 5.10
CHEMBL108035 — IC50 = 7998.34 nM 5.10
CHEMBL109893 — IC50 = 10000.0 nM 5.00
CHEMBL109893 — IC50 = 10000.0 nM 5.00