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Assay Detail

CHEMBL1044758

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

Functional
Antitrypanosomal activity against Trypanosoma cruzi Tulahuen infected in mouse 3T3 cells
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Trypanosoma cruzi
Cell Type NIH3T3
Confidence 1 — Organism
Curated By Autocuration

Target

Trypanosoma cruzi (CHEMBL368)
Type ORGANISM
Organism Trypanosoma cruzi

Publication

Isoquinoline-based analogs of the cancer drug clinical candidate tipifarnib as anti-Trypanosoma cruzi agents.
Chennamaneni NK, Arif J, Buckner FS, Gelb MH.
Bioorg Med Chem Lett (2009) 19 : 6582 -6584
PubMed 19875282 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 5 8.64 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1397 POSACONAZOLE 4.0 1 9.52
CHEMBL583404 1 9.30
CHEMBL567210 1 9.05
CHEMBL289228 TIPIFARNIB 3.0 1 8.40
CHEMBL566126 1 6.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1397 POSACONAZOLE EC50 = 0.3 nM 9.52
CHEMBL583404 EC50 = 0.5 nM 9.30
CHEMBL567210 EC50 = 0.9 nM 9.05
CHEMBL289228 TIPIFARNIB EC50 = 4.0 nM 8.40
CHEMBL566126 EC50 = 120.0 nM 6.92