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Assay Detail

CHEMBL5135073

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

Functional
Antitrypanosomal activity against intracellular Trypanosoma cruzi Tulahuen amastigotes expressing CL2 beta-galactosidase in human MRC5 cells assessed as parasite growth inhibition using chlorophenol red beta-D-galactopyranoside as substrate treated for 7 days by spectrophotometry
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Trypanosoma cruzi
Cell Type MRC5
Confidence 1 — Organism
Curated By Autocuration

Target

Trypanosoma cruzi (CHEMBL368)
Type ORGANISM
Organism Trypanosoma cruzi

Publication

N<sup>6</sup>-modification of 7-Deazapurine nucleoside analogues as Anti-Trypanosoma cruzi and anti-Leishmania agents: Structure-activity relationship exploration and In vivo evaluation.
Lin C, Jaén Batista DDG, Mazzeti AL, Donola Girão R, de Oliveira GM, Karalic I, Hulpia F, Soeiro MNC, Maes L, Caljon G, Van Calenbergh S.
Eur J Med Chem (2022) 231 : 114165 -114165
PubMed 35144125 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 30 5.31 6.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL267099 TUBERCIDIN 1 6.47
CHEMBL3126898 1 6.35
CHEMBL5174803 1 5.87
CHEMBL3126906 1 5.78
CHEMBL110 BENZNIDAZOLE 4.0 1 5.64
CHEMBL4436060 1 5.64
CHEMBL5200044 1 5.64
CHEMBL5205233 1 5.59
CHEMBL5199723 1 5.38
CHEMBL5195584 1 5.29
CHEMBL5196805 1 5.18
CHEMBL5182317 1 5.13
CHEMBL5207202 1 5.11
CHEMBL262874 1 5.11
CHEMBL5174504 1 5.11
CHEMBL98424 1 5.10
CHEMBL5170491 1 4.85
CHEMBL5203151 1 4.84
CHEMBL5187821 1 4.49
CHEMBL5178932 1 4.48
CHEMBL4782563 1 4.47
CHEMBL5189880 1 -
CHEMBL2023963 1 -
CHEMBL5207667 1 -
CHEMBL5191825 1 -
CHEMBL5194808 1 -
CHEMBL5184615 1 -
CHEMBL5180850 1 -
CHEMBL5169613 1 -
CHEMBL5209135 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL267099 TUBERCIDIN EC50 = 340.0 nM 6.47
CHEMBL3126898 EC50 = 450.0 nM 6.35
CHEMBL5174803 EC50 = 1360.0 nM 5.87
CHEMBL3126906 EC50 = 1650.0 nM 5.78
CHEMBL110 BENZNIDAZOLE EC50 = 2280.0 nM 5.64
CHEMBL4436060 EC50 = 2270.0 nM 5.64
CHEMBL5200044 EC50 = 2280.0 nM 5.64
CHEMBL5205233 EC50 = 2580.0 nM 5.59
CHEMBL5199723 EC50 = 4130.0 nM 5.38
CHEMBL5195584 EC50 = 5080.0 nM 5.29
CHEMBL5196805 EC50 = 6670.0 nM 5.18
CHEMBL5182317 EC50 = 7480.0 nM 5.13
CHEMBL5207202 EC50 = 7820.0 nM 5.11
CHEMBL262874 EC50 = 7740.0 nM 5.11
CHEMBL5174504 EC50 = 7840.0 nM 5.11
CHEMBL98424 EC50 = 7890.0 nM 5.10
CHEMBL5170491 EC50 = 14200.0 nM 4.85
CHEMBL5203151 EC50 = 14500.0 nM 4.84
CHEMBL5187821 EC50 = 32300.0 nM 4.49
CHEMBL5178932 EC50 = 33000.0 nM 4.48
CHEMBL4782563 EC50 = 33800.0 nM 4.47
CHEMBL5189880 EC50 > 64000.0 nM -
CHEMBL2023963 EC50 > 64000.0 nM -
CHEMBL5207667 EC50 > 64000.0 nM -
CHEMBL5191825 EC50 > 64000.0 nM -
CHEMBL5194808 EC50 > 64000.0 nM -
CHEMBL5184615 EC50 > 64000.0 nM -
CHEMBL5180850 EC50 > 64000.0 nM -
CHEMBL5169613 EC50 > 64000.0 nM -
CHEMBL5209135 EC50 > 64000.0 nM -