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Assay Detail

CHEMBL1119971

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

Binding
Inhibition of Trypanosoma cruzi cruzaine preincubated for 5 mins before substrate addition by fluorescence assay in absence of Triton X-100
22
Total Activities
22
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

Colloid formation by drugs in simulated intestinal fluid.
Doak AK, Wille H, Prusiner SB, Shoichet BK.
J Med Chem (2010) 53 : 4259 -4265
PubMed 20426472 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 4.78 5.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL64391 ITRACONAZOLE 4.0 1 5.52
CHEMBL1083993 AMIODARONE HYDROCHLORIDE 4.0 1 5.40
CHEMBL308954 ETRAVIRINE 4.0 1 5.40
CHEMBL1292 CLOFAZIMINE 4.0 1 5.22
CHEMBL1085699 MANIDIPINE 6300 3.0 1 5.22
CHEMBL21333 PRANLUKAST 4.0 1 5.16
CHEMBL1086440 TRICLABENDAZOLE 4.0 1 4.82
CHEMBL259223 MENATETRENONE 3.0 1 4.75
CHEMBL81 RALOXIFENE 4.0 1 4.48
CHEMBL1014 CANDESARTAN CILEXETIL 4.0 1 4.38
CHEMBL405110 METHYLENE BLUE ANHYDROUS 4.0 1 4.26
CHEMBL672 FENOFIBRATE 4.0 1 4.21
CHEMBL939 GEFITINIB 4.0 1 4.06
CHEMBL1084541 1 4.01
CHEMBL941 IMATINIB 4.0 1 -
CHEMBL929 DELAVIRDINE MESYLATE 4.0 1 -
CHEMBL1085765 MECLIZINE DIHCL 1 -
CHEMBL1083385 CLOPIDOGREL BISULFATE 4.0 1 -
CHEMBL584 NELFINAVIR 4.0 1 -
CHEMBL43064 CINNARIZINE 2.0 1 -
CHEMBL1713 CHLORPROMAZINE HYDROCHLORIDE 4.0 1 -
CHEMBL118 CELECOXIB 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL64391 ITRACONAZOLE IC50 = 3000.0 nM 5.52
CHEMBL1083993 AMIODARONE HYDROCHLORIDE IC50 = 4000.0 nM 5.40
CHEMBL308954 ETRAVIRINE IC50 = 4000.0 nM 5.40
CHEMBL1292 CLOFAZIMINE IC50 = 6000.0 nM 5.22
CHEMBL1085699 MANIDIPINE 6300 IC50 = 6000.0 nM 5.22
CHEMBL21333 PRANLUKAST IC50 = 7000.0 nM 5.16
CHEMBL1086440 TRICLABENDAZOLE IC50 = 15000.0 nM 4.82
CHEMBL259223 MENATETRENONE IC50 = 18000.0 nM 4.75
CHEMBL81 RALOXIFENE IC50 = 33000.0 nM 4.48
CHEMBL1014 CANDESARTAN CILEXETIL IC50 = 42000.0 nM 4.38
CHEMBL405110 METHYLENE BLUE ANHYDROUS IC50 = 55000.0 nM 4.26
CHEMBL672 FENOFIBRATE IC50 = 61000.0 nM 4.21
CHEMBL939 GEFITINIB IC50 = 88000.0 nM 4.06
CHEMBL1084541 IC50 = 98000.0 nM 4.01
CHEMBL941 IMATINIB IC50 = 207000.0 nM -
CHEMBL929 DELAVIRDINE MESYLATE IC50 = 122000.0 nM -
CHEMBL1085765 MECLIZINE DIHCL IC50 = 129000.0 nM -
CHEMBL1083385 CLOPIDOGREL BISULFATE IC50 = 123000.0 nM -
CHEMBL584 NELFINAVIR IC50 = 144000.0 nM -
CHEMBL43064 CINNARIZINE IC50 = 124000.0 nM -
CHEMBL1713 CHLORPROMAZINE HYDROCHLORIDE IC50 = 189000.0 nM -
CHEMBL118 CELECOXIB IC50 = 126000.0 nM -