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Assay Detail

CHEMBL1663717

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Functional
Antiprotozoal activity against bloodstream forms of Trypanosoma brucei rhodesiense STIB900 by alamar blue assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Synthesis and antiprotozoal activity of N-alkoxy analogues of the trypanocidal lead compound 4,4'-bis(imidazolinylamino)diphenylamine with improved human blood-brain barrier permeability.
Nieto L, Mascaraque A, Miller F, Glacial F, Ríos Martínez C, Kaiser M, Brun R, Dardonville C.
J Med Chem (2011) 54 : 485 -494
PubMed 21175162 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 5.49 7.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL242102 1 7.16
CHEMBL1650072 1 6.50
CHEMBL1650074 1 6.43
CHEMBL1650071 1 6.14
CHEMBL1650070 1 6.08
CHEMBL1650073 1 5.93
CHEMBL1650075 1 4.96
CHEMBL1650079 1 4.83
CHEMBL1650078 1 4.21
CHEMBL1650077 1 4.13
CHEMBL1650076 1 4.06

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL242102 IC50 = 69.0 nM 7.16
CHEMBL1650072 IC50 = 320.0 nM 6.50
CHEMBL1650074 IC50 = 370.0 nM 6.43
CHEMBL1650071 IC50 = 730.0 nM 6.14
CHEMBL1650070 IC50 = 830.0 nM 6.08
CHEMBL1650073 IC50 = 1180.0 nM 5.93
CHEMBL1650075 IC50 = 11100.0 nM 4.96
CHEMBL1650079 IC50 = 14900.0 nM 4.83
CHEMBL1650078 IC50 = 61300.0 nM 4.21
CHEMBL1650077 IC50 = 73800.0 nM 4.13
CHEMBL1650076 IC50 = 86700.0 nM 4.06