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Assay Detail

CHEMBL4143002

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

Functional
Antitrypanosomal activity against beta-galactosidase expressing nifurtimox-sensitive Trypanosoma cruzi Tulahuen CL2 infected in human MRC5 SV2 cells assessed as decrease in parasite burden after 168 hrs by spectrophotometric method
62
Total Activities
62
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Trypanosoma cruzi
Confidence 1 — Organism
Curated By Intermediate

Target

Trypanosoma cruzi (CHEMBL368)
Type ORGANISM
Organism Trypanosoma cruzi

Publication

Novel triazine dimers with potent antitrypanosomal activity.
Venkatraj M, Salado IG, Heeres J, Joossens J, Lewi PJ, Caljon G, Maes L, Van der Veken P, Augustyns K.
Eur J Med Chem (2018) 143 : 306 -319
PubMed 29197735 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 62 5.25 6.23

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2207879 1 6.23
CHEMBL290960 NIFURTIMOX 4.0 1 6.16
CHEMBL2207895 1 5.76
CHEMBL2207899 1 5.75
CHEMBL2207914 1 5.61
CHEMBL2207897 1 5.60
CHEMBL110 BENZNIDAZOLE 4.0 1 5.59
CHEMBL3338054 1 5.35
CHEMBL2207898 1 5.33
CHEMBL3338023 1 5.31
CHEMBL2207915 1 5.27
CHEMBL470025 1 5.18
CHEMBL302791 1 5.17
CHEMBL2207894 1 5.16
CHEMBL71659 1 5.15
CHEMBL3338026 1 5.13
CHEMBL71521 1 5.13
CHEMBL2207885 1 5.08
CHEMBL3338022 1 5.06
CHEMBL421114 1 5.06
CHEMBL2207912 1 5.05
CHEMBL74174 1 4.94
CHEMBL3338052 1 4.82
CHEMBL2207594 1 4.77
CHEMBL2207901 1 4.63
CHEMBL2207913 1 4.31
CHEMBL4165796 1 -
CHEMBL2207896 1 -
CHEMBL2207880 1 -
CHEMBL2207881 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2207879 IC50 = 590.0 nM 6.23
CHEMBL290960 NIFURTIMOX IC50 = 700.0 nM 6.16
CHEMBL2207895 IC50 = 1730.0 nM 5.76
CHEMBL2207899 IC50 = 1770.0 nM 5.75
CHEMBL2207914 IC50 = 2470.0 nM 5.61
CHEMBL2207897 IC50 = 2500.0 nM 5.60
CHEMBL110 BENZNIDAZOLE IC50 = 2560.0 nM 5.59
CHEMBL3338054 IC50 = 4510.0 nM 5.35
CHEMBL2207898 IC50 = 4680.0 nM 5.33
CHEMBL3338023 IC50 = 4870.0 nM 5.31
CHEMBL2207915 IC50 = 5410.0 nM 5.27
CHEMBL470025 IC50 = 6650.0 nM 5.18
CHEMBL302791 IC50 = 6800.0 nM 5.17
CHEMBL2207894 IC50 = 6890.0 nM 5.16
CHEMBL71659 IC50 = 7150.0 nM 5.15
CHEMBL3338026 IC50 = 7450.0 nM 5.13
CHEMBL71521 IC50 = 7370.0 nM 5.13
CHEMBL2207885 IC50 = 8320.0 nM 5.08
CHEMBL3338022 IC50 = 8660.0 nM 5.06
CHEMBL421114 IC50 = 8690.0 nM 5.06
CHEMBL2207912 IC50 = 8820.0 nM 5.05
CHEMBL74174 IC50 = 11510.0 nM 4.94
CHEMBL3338052 IC50 = 14980.0 nM 4.82
CHEMBL2207594 IC50 = 17080.0 nM 4.77
CHEMBL2207901 IC50 = 23540.0 nM 4.63
CHEMBL2207913 IC50 = 49050.0 nM 4.31
CHEMBL2203849 IC50 > 64000.0 nM -
CHEMBL2207900 IC50 > 64000.0 nM -
CHEMBL2207909 IC50 > 64000.0 nM -
CHEMBL2207908 IC50 > 64000.0 nM -
CHEMBL2207907 IC50 > 64000.0 nM -
CHEMBL2207906 IC50 > 64000.0 nM -
CHEMBL2207905 IC50 > 64000.0 nM -
CHEMBL2207904 IC50 > 64000.0 nM -
CHEMBL2207903 IC50 > 64000.0 nM -
CHEMBL2207902 IC50 > 64000.0 nM -
CHEMBL2203851 IC50 > 64000.0 nM -
CHEMBL2203850 IC50 > 64000.0 nM -
CHEMBL4165796 IC50 > 64000.0 nM -
CHEMBL2207919 IC50 > 64000.0 nM -
CHEMBL2207910 IC50 > 64000.0 nM -
CHEMBL3338053 IC50 > 64000.0 nM -
CHEMBL3338021 IC50 > 64000.0 nM -
CHEMBL3338007 IC50 > 64000.0 nM -
CHEMBL2207883 IC50 > 64000.0 nM -
CHEMBL2207884 IC50 > 64000.0 nM -
CHEMBL4175939 IC50 > 64000.0 nM -
CHEMBL2207881 IC50 > 64000.0 nM -
CHEMBL2207880 IC50 > 64000.0 nM -
CHEMBL2207896 IC50 > 64000.0 nM -