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Assay Detail

CHEMBL4350264

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

Functional
Antitrypanosomal activity against suramin sensitive Trypanosoma brucei Squib427 trypomastigotes assessed as reduction in parasitic cell viability measured after 72 hrs by resazurin dye based fluorimetric analysis
9
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Trypanosoma brucei (CHEMBL612849)
Type ORGANISM
Organism Trypanosoma brucei

Publication

Alkynamide phthalazinones as a new class of TbrPDEB1 inhibitors.
de Heuvel E, Singh AK, Edink E, van der Meer T, van der Woude M, Sadek P, Krell-Jørgensen MP, van den Bergh T, Veerman J, Caljon G, Kalejaiye TD, Wijtmans M, Maes L, de Koning HP, Jan Sterk G, Siderius M, de Esch IJP, Brown DG, Leurs R.
Bioorg Med Chem (2019) 27 : 3998 -4012
PubMed 31327675 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 5.84 6.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4519708 2 6.22
CHEMBL4464777 2 6.22
CHEMBL4465919 1 6.00
CHEMBL4473824 1 5.40
CHEMBL4210475 1 5.30
CHEMBL4204999 1 5.20
CHEMBL4520514 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4519708 IC50 = 600.0 nM 6.22
CHEMBL4464777 IC50 = 600.0 nM 6.22
CHEMBL4519708 IC50 = 630.96 nM 6.20
CHEMBL4464777 IC50 = 630.96 nM 6.20
CHEMBL4465919 IC50 = 1000.0 nM 6.00
CHEMBL4473824 IC50 = 3981.07 nM 5.40
CHEMBL4210475 IC50 = 5011.87 nM 5.30
CHEMBL4204999 IC50 = 6309.57 nM 5.20
CHEMBL4520514 IC50 > 63095.73 nM -