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Assay Detail

CHEMBL3783536

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Functional
Antiparasitic activity against suramin-sensitive trypomastigote stage of Trypanosoma brucei rhodesiense squib-427 infected in human MRC5 cells after 4 days by Alamar blue staining based fluorimetric analysis
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Trypanosoma brucei rhodesiense
Cell Type MRC5
Confidence 1 — Organism
Curated By Autocuration

Target

Trypanosoma brucei rhodesiense (CHEMBL612348)
Type ORGANISM
Organism Trypanosoma brucei rhodesiense

Publication

In vitro screening of 2-(1H-imidazol-1-yl)-1-phenylethanol derivatives as antiprotozoal agents and docking studies on Trypanosoma cruzi CYP51.
De Vita D, Moraca F, Zamperini C, Pandolfi F, Di Santo R, Matheeussen A, Maes L, Tortorella S, Scipione L.
Eur J Med Chem (2016) 113 : 28 -33
PubMed 26922226 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 4.82 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL265502 SURAMIN 3.0 1 7.70
CHEMBL3291243 1 5.10
CHEMBL3291242 1 4.57
CHEMBL3780605 1 4.54
CHEMBL3781870 1 4.52
CHEMBL3781446 1 4.49
CHEMBL1946739 1 4.49
CHEMBL1946740 1 4.49
CHEMBL3780946 1 4.49
CHEMBL3781706 1 4.49
CHEMBL3291250 1 4.48
CHEMBL3781420 1 4.47
CHEMBL3291241 1 -
CHEMBL3780620 1 -
CHEMBL3780819 1 -
CHEMBL3781877 1 -
CHEMBL3291249 1 -
CHEMBL3780533 1 -
CHEMBL3780260 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL265502 SURAMIN IC50 = 20.0 nM 7.70
CHEMBL3291243 IC50 = 8000.0 nM 5.10
CHEMBL3291242 IC50 = 27200.0 nM 4.57
CHEMBL3780605 IC50 = 29100.0 nM 4.54
CHEMBL3781870 IC50 = 30100.0 nM 4.52
CHEMBL3781446 IC50 = 32400.0 nM 4.49
CHEMBL1946739 IC50 = 32200.0 nM 4.49
CHEMBL1946740 IC50 = 32400.0 nM 4.49
CHEMBL3780946 IC50 = 32200.0 nM 4.49
CHEMBL3781706 IC50 = 32200.0 nM 4.49
CHEMBL3291250 IC50 = 32900.0 nM 4.48
CHEMBL3781420 IC50 = 33700.0 nM 4.47
CHEMBL3291241 IC50 > 64000.0 nM -
CHEMBL3780620 IC50 > 64000.0 nM -
CHEMBL3780819 IC50 > 64000.0 nM -
CHEMBL3781877 IC50 > 64000.0 nM -
CHEMBL3291249 IC50 > 64000.0 nM -
CHEMBL3780533 IC50 > 64000.0 nM -
CHEMBL3780260 IC50 > 64000.0 nM -