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Assay Detail

CHEMBL660279

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Binding
Inhibitory activity against Trypanosoma cruzi cathepsin L-like protease (cruzain) was determined using purified recombinant protein
ChEMBL ↗
79
Total Activities
78
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Cruzipain (CHEMBL3563) ↗
Type SINGLE PROTEIN
Organism Trypanosoma cruzi

Publication

Synthesis and structure-activity relationship study of potent trypanocidal thio semicarbazone inhibitors of the trypanosomal cysteine protease cruzain.
Du X, Guo C, Hansell E, Doyle PS, Caffrey CR, Holler TP, McKerrow JH, Cohen FE.
J Med Chem (2002) 45 : 2695 -2707
PubMed 12061873 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 79 6.50 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL93166 — — 1 7.70
CHEMBL92099 — — 1 7.70
CHEMBL91003 — — 1 7.40
CHEMBL90512 — — 1 7.30
CHEMBL92376 — — 1 7.30
CHEMBL329346 — — 1 7.22
CHEMBL89973 — — 1 7.22
CHEMBL91544 — — 1 7.16
CHEMBL91640 — — 1 7.10
CHEMBL406038 — — 1 7.10
CHEMBL313679 — — 1 7.00
CHEMBL329128 — — 1 6.85
CHEMBL330050 — — 1 6.77
CHEMBL88734 — — 1 6.70
CHEMBL314026 — — 1 6.70
CHEMBL90866 — — 1 6.66
CHEMBL90428 — — 1 6.64
CHEMBL90197 — — 1 6.57
CHEMBL93774 — — 1 6.55
CHEMBL90060 — — 1 6.55
CHEMBL327577 — — 1 6.52
CHEMBL90772 — — 1 6.50
CHEMBL415311 — — 1 6.34
CHEMBL90688 — — 1 6.32
CHEMBL90867 — — 1 6.25
CHEMBL421363 — — 1 6.25
CHEMBL90475 — — 1 6.00
CHEMBL91844 — — 1 5.89
CHEMBL91347 — — 1 5.85
CHEMBL420616 — — 2 5.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL93166 — IC50 = 20.0 nM 7.70
CHEMBL92099 — IC50 = 20.0 nM 7.70
CHEMBL91003 — IC50 = 40.0 nM 7.40
CHEMBL90512 — IC50 = 50.0 nM 7.30
CHEMBL92376 — IC50 = 50.0 nM 7.30
CHEMBL329346 — IC50 = 60.0 nM 7.22
CHEMBL89973 — IC50 = 60.0 nM 7.22
CHEMBL91544 — IC50 = 70.0 nM 7.16
CHEMBL91640 — IC50 = 80.0 nM 7.10
CHEMBL406038 — IC50 = 80.0 nM 7.10
CHEMBL313679 — IC50 = 100.0 nM 7.00
CHEMBL329128 — IC50 = 140.0 nM 6.85
CHEMBL330050 — IC50 = 170.0 nM 6.77
CHEMBL88734 — IC50 = 200.0 nM 6.70
CHEMBL314026 — IC50 = 200.0 nM 6.70
CHEMBL90866 — IC50 = 220.0 nM 6.66
CHEMBL90428 — IC50 = 230.0 nM 6.64
CHEMBL90197 — IC50 = 270.0 nM 6.57
CHEMBL93774 — IC50 = 280.0 nM 6.55
CHEMBL90060 — IC50 = 280.0 nM 6.55
CHEMBL327577 — IC50 = 300.0 nM 6.52
CHEMBL90772 — IC50 = 320.0 nM 6.50
CHEMBL415311 — IC50 = 460.0 nM 6.34
CHEMBL90688 — IC50 = 480.0 nM 6.32
CHEMBL421363 — IC50 = 560.0 nM 6.25
CHEMBL90867 — IC50 = 560.0 nM 6.25
CHEMBL90475 — IC50 = 1000.0 nM 6.00
CHEMBL91844 — IC50 = 1300.0 nM 5.89
CHEMBL91347 — IC50 = 1400.0 nM 5.85
CHEMBL420616 — IC50 = 1600.0 nM 5.80
CHEMBL90354 — IC50 = 1700.0 nM 5.77
CHEMBL90181 — IC50 = 1900.0 nM 5.72
CHEMBL90808 — IC50 = 2800.0 nM 5.55
CHEMBL94235 — IC50 = 2800.0 nM 5.55
CHEMBL89990 — IC50 = 3800.0 nM 5.42
CHEMBL90819 — IC50 = 3900.0 nM 5.41
CHEMBL91830 — IC50 = 7000.0 nM 5.16
CHEMBL91201 — IC50 > 10000.0 nM -
CHEMBL90250 — IC50 > 10000.0 nM -
CHEMBL420616 — IC50 > 10000.0 nM -
CHEMBL91267 — IC50 > 10000.0 nM -
CHEMBL330453 — IC50 > 10000.0 nM -
CHEMBL91266 — IC50 > 10000.0 nM -
CHEMBL89974 — IC50 > 10000.0 nM -
CHEMBL92375 — IC50 > 10000.0 nM -
CHEMBL90859 — IC50 > 10000.0 nM -
CHEMBL330503 — IC50 > 10000.0 nM -
CHEMBL93490 — IC50 > 10000.0 nM -
CHEMBL242103 — IC50 > 10000.0 nM -
CHEMBL91439 — IC50 > 10000.0 nM -