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Assay Detail

CHEMBL3383480

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

Functional
Trypanocidal activity against wild type bloodstream forms of Trypanosoma brucei brucei Lister 427 clone 221a assessed as inhibition of proliferation after 3 days by resazurin assay
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Trypanosoma brucei brucei (CHEMBL612851)
Type ORGANISM
Organism Trypanosoma brucei brucei

Publication

Novel nitro(triazole/imidazole)-based heteroarylamides/sulfonamides as potential antitrypanosomal agents.
Papadopoulou MV, Bloomer WD, Rosenzweig HS, Wilkinson SR, Kaiser M.
Eur J Med Chem (2014) 87 : 79 -88
PubMed 25240098 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 5.67 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL166 MELARSOPROL 3.0 1 8.22
CHEMBL3358487 1 6.36
CHEMBL3358475 1 6.21
CHEMBL3358488 1 5.87
CHEMBL2070694 1 5.64
CHEMBL3358473 1 5.53
CHEMBL3358480 1 5.52
CHEMBL3358478 1 5.01
CHEMBL3358474 1 4.81
CHEMBL3358472 1 4.64
CHEMBL3358479 1 4.57
CHEMBL3358485 1 -
CHEMBL3358486 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL166 MELARSOPROL IC50 = 6.0 nM 8.22
CHEMBL3358487 IC50 = 440.0 nM 6.36
CHEMBL3358475 IC50 = 610.0 nM 6.21
CHEMBL3358488 IC50 = 1360.0 nM 5.87
CHEMBL2070694 IC50 = 2300.0 nM 5.64
CHEMBL3358473 IC50 = 2940.0 nM 5.53
CHEMBL3358480 IC50 = 3020.0 nM 5.52
CHEMBL3358478 IC50 = 9690.0 nM 5.01
CHEMBL3358474 IC50 = 15460.0 nM 4.81
CHEMBL3358472 IC50 = 22950.0 nM 4.64
CHEMBL3358479 IC50 = 26830.0 nM 4.57
CHEMBL3358485 IC50 > 7990.0 nM -
CHEMBL3358486 IC50 > 930.0 nM -