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Assay Detail

CHEMBL4684616

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

Functional
Antitrypanosomal activity against bloodstream form of trypanosoma brucei brucei 427 assessed as reduction in parasitic growth after 72 hrs by resazurin staining based fluorescence 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

Identification of a 2,4-diaminopyrimidine scaffold targeting Trypanosoma brucei pteridine reductase 1 from the LIBRA compound library screening campaign.
Linciano P,Cullia G,Borsari C,Santucci M,Ferrari S,Witt G,Gul S,Kuzikov M,Ellinger B,Santarém N,Cordeiro da Silva A,Conti P,Bolognesi ML,Roberti M,Prati F,Bartoccini F,Retini M,Piersanti G,Cavalli A,Goldoni L,Bertozzi SM,Bertozzi F,Brambilla E,Rizzo V,Piomelli D,Pinto A,Bandiera T,Costi MP
Eur J Med Chem (2020) 189 : 112047 -112047
PubMed 31982652 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 6.05 6.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL54725 1 6.57
CHEMBL4785591 1 6.25
CHEMBL4760251 1 6.24
CHEMBL4778279 1 6.21
CHEMBL4753514 1 5.61
CHEMBL4762279 1 5.43
CHEMBL121445 1 -
CHEMBL4753331 1 -
CHEMBL158919 1 -
CHEMBL4748094 1 -
CHEMBL4777938 1 -
CHEMBL4754292 1 -
CHEMBL4797185 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL54725 IC50 = 270.0 nM 6.57
CHEMBL4785591 IC50 = 560.0 nM 6.25
CHEMBL4760251 IC50 = 580.0 nM 6.24
CHEMBL4778279 IC50 = 610.0 nM 6.21
CHEMBL4753514 IC50 = 2450.0 nM 5.61
CHEMBL4762279 IC50 = 3700.0 nM 5.43
CHEMBL121445 IC50 - -
CHEMBL4753331 IC50 - -
CHEMBL158919 IC50 - -
CHEMBL4748094 IC50 - -
CHEMBL4777938 IC50 - -
CHEMBL4754292 IC50 - -
CHEMBL4797185 IC50 - -