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Assay Detail

CHEMBL4712759

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

Functional
Antitrypanosomal activity against Trypanosoma cruzi infected in human MRC-5 SV2 cells
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Trypanosoma cruzi
Cell Type MRC-5 SV2
Confidence 1 — Organism
Curated By Autocuration

Target

Trypanosoma cruzi (CHEMBL368)
Type ORGANISM
Organism Trypanosoma cruzi

Publication

Synthesis and evaluation of a collection of purine-like C-nucleosides as antikinetoplastid agents.
Bouton J,Maes L,Karalic I,Caljon G,Van Calenbergh S
Eur J Med Chem (2021) 212 : 113101 -113101
PubMed 33385837 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 5.73 6.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4764464 1 6.64
CHEMBL4790411 1 6.47
CHEMBL4787773 1 6.34
CHEMBL4634483 1 6.27
CHEMBL4742019 1 6.22
CHEMBL4788848 1 6.21
CHEMBL4744476 1 6.11
CHEMBL4751562 1 5.98
CHEMBL110 BENZNIDAZOLE 4.0 1 5.70
CHEMBL4764594 1 5.61
CHEMBL4758694 1 5.42
CHEMBL4777562 1 5.12
CHEMBL4794928 1 5.00
CHEMBL4751346 1 4.51
CHEMBL4755821 1 4.41
CHEMBL4758898 1 -
CHEMBL4783188 1 -
CHEMBL2016757 GS-441524 1.0 1 -
CHEMBL4753867 1 -
CHEMBL4793136 1 -
CHEMBL4079082 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4764464 IC50 = 230.0 nM 6.64
CHEMBL4790411 IC50 = 340.0 nM 6.47
CHEMBL4787773 IC50 = 460.0 nM 6.34
CHEMBL4634483 IC50 = 540.0 nM 6.27
CHEMBL4742019 IC50 = 600.0 nM 6.22
CHEMBL4788848 IC50 = 620.0 nM 6.21
CHEMBL4744476 IC50 = 780.0 nM 6.11
CHEMBL4751562 IC50 = 1040.0 nM 5.98
CHEMBL110 BENZNIDAZOLE IC50 = 2020.0 nM 5.70
CHEMBL4764594 IC50 = 2450.0 nM 5.61
CHEMBL4758694 IC50 = 3810.0 nM 5.42
CHEMBL4777562 IC50 = 7670.0 nM 5.12
CHEMBL4794928 IC50 = 10100.0 nM 5.00
CHEMBL4751346 IC50 = 30900.0 nM 4.51
CHEMBL4755821 IC50 = 39300.0 nM 4.41
CHEMBL4758898 IC50 > 64000.0 nM -
CHEMBL4783188 IC50 > 64000.0 nM -
CHEMBL2016757 GS-441524 IC50 > 64000.0 nM -
CHEMBL4753867 IC50 > 64000.0 nM -
CHEMBL4793136 IC50 > 64000.0 nM -
CHEMBL4079082 IC50 < 250.0 nM -