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Assay Detail

CHEMBL3626663

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

Functional
Antiparasitic activity against bloodstream form of Trypanosoma brucei brucei 427 infected in macrophages differentiated from human THP1 cells assessed as growth inhibition after 72 hrs by Alamar Blue assay
17
Total Activities
12
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Characterization of 2,4-Diamino-6-oxo-1,6-dihydropyrimidin-5-yl Ureido Based Inhibitors of Trypanosoma brucei FolD and Testing for Antiparasitic Activity.
Eadsforth TC, Pinto A, Luciani R, Tamborini L, Cullia G, De Micheli C, Marinelli L, Cosconati S, Novellino E, Lo Presti L, Cordeiro da Silva A, Conti P, Hunter WN, Costi MP.
J Med Chem (2015) 58 : 7938 -7948
PubMed 26322631 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 4.93 8.80
GI 6 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL55 PENTAMIDINE 4.0 1 8.80
CHEMBL3622702 2 4.31
CHEMBL297258 2 4.24
CHEMBL3622700 2 4.13
CHEMBL3622699 2 4.05
CHEMBL3622701 2 4.04
CHEMBL3622703 1 -
CHEMBL3622704 1 -
CHEMBL3622705 1 -
CHEMBL3622706 1 -
CHEMBL3622707 1 -
CHEMBL265502 SURAMIN 3.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL55 PENTAMIDINE IC50 = 1.6 nM 8.80
CHEMBL3622702 IC50 = 49000.0 nM 4.31
CHEMBL297258 IC50 = 57000.0 nM 4.24
CHEMBL3622700 IC50 = 74000.0 nM 4.13
CHEMBL3622699 IC50 = 89000.0 nM 4.05
CHEMBL3622701 IC50 = 92000.0 nM 4.04
CHEMBL3622703 IC50 - -
CHEMBL3622704 IC50 - -
CHEMBL3622705 IC50 - -
CHEMBL3622706 IC50 - -
CHEMBL3622707 IC50 - -
CHEMBL265502 SURAMIN GI - -
CHEMBL3622699 GI - -
CHEMBL3622700 GI - -
CHEMBL3622701 GI - -
CHEMBL3622702 GI - -
CHEMBL297258 GI - -