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Assay Detail

CHEMBL3243043

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Binding
Inhibition of Trypanosoma cruzi cruzaine expressed in Escherichia coli SG13009 using Z-FR-AMC as substrate after 5 mins
ChEMBL ↗
45
Total Activities
45
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

Synthesis, biological evaluation, and structure-activity relationships of potent noncovalent and nonpeptidic cruzain inhibitors as anti-Trypanosoma cruzi agents.
Ferreira RS, Dessoy MA, Pauli I, Souza ML, Krogh R, Sales AI, Oliva G, Dias LC, Andricopulo AD.
J Med Chem (2014) 57 : 2380 -2392
PubMed 24533839 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 45 5.35 6.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3233095 — — 1 6.68
CHEMBL3233119 — — 1 6.27
CHEMBL3233118 — — 1 6.22
CHEMBL3233120 — — 1 6.21
CHEMBL1173694 — — 1 6.10
CHEMBL3233088 — — 1 6.10
CHEMBL3233083 — — 1 5.80
CHEMBL3233089 — — 1 5.57
CHEMBL3233082 — — 1 5.52
CHEMBL3233091 — — 1 5.52
CHEMBL1346687 — — 1 5.39
CHEMBL3233081 — — 1 5.28
CHEMBL3233090 — — 1 5.28
CHEMBL3233094 — — 1 5.09
CHEMBL3233116 — — 1 5.00
CHEMBL1572619 — — 1 4.96
CHEMBL3233093 — — 1 4.90
CHEMBL3233085 — — 1 4.88
CHEMBL3233092 — — 1 4.87
CHEMBL3233115 — — 1 4.62
CHEMBL3233097 — — 1 4.42
CHEMBL3233084 — — 1 4.19
CHEMBL3233096 — — 1 4.11
CHEMBL3233107 — — 1 -
CHEMBL3233106 — — 1 -
CHEMBL3233105 — — 1 -
CHEMBL3233104 — — 1 -
CHEMBL3233103 — — 1 -
CHEMBL3233102 — — 1 -
CHEMBL3233101 — — 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3233095 — IC50 = 210.0 nM 6.68
CHEMBL3233119 — IC50 = 540.0 nM 6.27
CHEMBL3233118 — IC50 = 600.0 nM 6.22
CHEMBL3233120 — IC50 = 620.0 nM 6.21
CHEMBL1173694 — IC50 = 800.0 nM 6.10
CHEMBL3233088 — IC50 = 800.0 nM 6.10
CHEMBL3233083 — IC50 = 1600.0 nM 5.80
CHEMBL3233089 — IC50 = 2700.0 nM 5.57
CHEMBL3233082 — IC50 = 3000.0 nM 5.52
CHEMBL3233091 — IC50 = 3000.0 nM 5.52
CHEMBL1346687 — IC50 = 4100.0 nM 5.39
CHEMBL3233090 — IC50 = 5200.0 nM 5.28
CHEMBL3233081 — IC50 = 5300.0 nM 5.28
CHEMBL3233094 — IC50 = 8200.0 nM 5.09
CHEMBL3233116 — IC50 = 9900.0 nM 5.00
CHEMBL1572619 — IC50 = 10900.0 nM 4.96
CHEMBL3233093 — IC50 = 12700.0 nM 4.90
CHEMBL3233085 — IC50 = 13200.0 nM 4.88
CHEMBL3233092 — IC50 = 13500.0 nM 4.87
CHEMBL3233115 — IC50 = 23900.0 nM 4.62
CHEMBL3233097 — IC50 = 38400.0 nM 4.42
CHEMBL3233084 — IC50 = 65100.0 nM 4.19
CHEMBL3233096 — IC50 = 77500.0 nM 4.11
CHEMBL3233108 — IC50 - — -
CHEMBL3233086 — IC50 - — -
CHEMBL3233087 — IC50 - — -
CHEMBL3233117 — IC50 - — -
CHEMBL3233098 — IC50 - — -
CHEMBL3233114 — IC50 - — -
CHEMBL3233113 — IC50 - — -
CHEMBL3233112 — IC50 - — -
CHEMBL3233111 — IC50 - — -
CHEMBL3233110 — IC50 - — -
CHEMBL3233109 — IC50 - — -
CHEMBL3233107 — IC50 - — -
CHEMBL1310061 — IC50 - — -
CHEMBL3233100 — IC50 - — -
CHEMBL3233099 — IC50 - — -
CHEMBL3233013 — IC50 - — -
CHEMBL3233101 — IC50 - — -
CHEMBL3233102 — IC50 - — -
CHEMBL3233103 — IC50 - — -
CHEMBL3233104 — IC50 - — -
CHEMBL3233105 — IC50 - — -
CHEMBL3233106 — IC50 - — -