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Assay Detail

CHEMBL4143003

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

Functional
Antileishmanial activity against amastigote stage of Leishmania infantum MHOM/MA(BE)/67 infected in mouse primary peritoneal macrophages assessed as decrease in parasite burden after 120 hrs by Giemsa staining-based microscopic method
61
Total Activities
61
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Leishmania infantum
Confidence 1 — Organism
Curated By Intermediate

Target

Leishmania infantum (CHEMBL612848)
Type ORGANISM
Organism Leishmania infantum

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 61 4.90 7.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2207914 1 7.05
CHEMBL2207899 1 5.73
CHEMBL2207897 1 5.71
CHEMBL2207895 1 5.62
CHEMBL2207915 1 5.52
CHEMBL2207894 1 5.36
CHEMBL2207898 1 5.28
CHEMBL125 MILTEFOSINE 4.0 1 5.21
CHEMBL4176046 1 5.10
CHEMBL2207884 1 5.04
CHEMBL2207886 1 5.04
CHEMBL3338023 1 5.01
CHEMBL2207896 1 5.00
CHEMBL3338026 1 5.00
CHEMBL421114 1 5.00
CHEMBL2207594 1 4.92
CHEMBL2207883 1 4.88
CHEMBL2207916 1 4.88
CHEMBL3338053 1 4.78
CHEMBL3338054 1 4.74
CHEMBL2207885 1 4.71
CHEMBL2207909 1 4.69
CHEMBL2207902 1 4.69
CHEMBL2207900 1 4.69
CHEMBL2207911 1 4.65
CHEMBL302791 1 4.65
CHEMBL3338052 1 4.64
CHEMBL2207917 1 4.60
CHEMBL2207889 1 4.59
CHEMBL2207893 1 4.59

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2207914 IC50 = 90.0 nM 7.05
CHEMBL2207899 IC50 = 1880.0 nM 5.73
CHEMBL2207897 IC50 = 1970.0 nM 5.71
CHEMBL2207895 IC50 = 2410.0 nM 5.62
CHEMBL2207915 IC50 = 3000.0 nM 5.52
CHEMBL2207894 IC50 = 4420.0 nM 5.36
CHEMBL2207898 IC50 = 5260.0 nM 5.28
CHEMBL125 MILTEFOSINE IC50 = 6170.0 nM 5.21
CHEMBL4176046 IC50 = 8000.0 nM 5.10
CHEMBL2207884 IC50 = 9040.0 nM 5.04
CHEMBL2207886 IC50 = 9040.0 nM 5.04
CHEMBL3338023 IC50 = 9830.0 nM 5.01
CHEMBL3338026 IC50 = 10080.0 nM 5.00
CHEMBL421114 IC50 = 10080.0 nM 5.00
CHEMBL2207896 IC50 = 10080.0 nM 5.00
CHEMBL2207594 IC50 = 12000.0 nM 4.92
CHEMBL2207883 IC50 = 13040.0 nM 4.88
CHEMBL2207916 IC50 = 13040.0 nM 4.88
CHEMBL3338053 IC50 = 16700.0 nM 4.78
CHEMBL3338054 IC50 = 18160.0 nM 4.74
CHEMBL2207885 IC50 = 19310.0 nM 4.71
CHEMBL2207909 IC50 = 20290.0 nM 4.69
CHEMBL2207902 IC50 = 20320.0 nM 4.69
CHEMBL2207900 IC50 = 20320.0 nM 4.69
CHEMBL302791 IC50 = 22180.0 nM 4.65
CHEMBL2207911 IC50 = 22260.0 nM 4.65
CHEMBL3338052 IC50 = 23100.0 nM 4.64
CHEMBL2207917 IC50 = 25340.0 nM 4.60
CHEMBL2207889 IC50 = 25400.0 nM 4.59
CHEMBL2207893 IC50 = 25660.0 nM 4.59
CHEMBL2207887 IC50 = 26160.0 nM 4.58
CHEMBL71659 IC50 = 26160.0 nM 4.58
CHEMBL2207918 IC50 = 27270.0 nM 4.56
CHEMBL2203850 IC50 = 27270.0 nM 4.56
CHEMBL2207912 IC50 = 27890.0 nM 4.55
CHEMBL2207903 IC50 = 29980.0 nM 4.52
CHEMBL2207891 IC50 = 32000.0 nM 4.50
CHEMBL2207901 IC50 = 36160.0 nM 4.44
CHEMBL2207910 IC50 = 37300.0 nM 4.43
CHEMBL74174 IC50 = 38160.0 nM 4.42
CHEMBL3338022 IC50 = 41000.0 nM 4.39
CHEMBL2207913 IC50 > 64000.0 nM -
CHEMBL2207905 IC50 > 64000.0 nM -
CHEMBL2207890 IC50 > 64000.0 nM -
CHEMBL2207892 IC50 > 64000.0 nM -
CHEMBL2207919 IC50 > 64000.0 nM -
CHEMBL71521 IC50 > 64000.0 nM -
CHEMBL2203849 IC50 > 64000.0 nM -
CHEMBL2207908 IC50 > 64000.0 nM -
CHEMBL3338021 IC50 > 64000.0 nM -