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Assay Detail

CHEMBL2161726

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

Functional
Trypanocidal activity against Leishmania major promastigote forms infected in sandfly gut assessed as inhibition of parasite growth
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Leishmania major
Confidence 1 — Organism
Curated By Autocuration

Target

Leishmania major (CHEMBL612879)
Type ORGANISM
Organism Leishmania major

Publication

Synthesis and structure-activity relationships of nitrobenzyl phosphoramide mustards as nitroreductase-activated prodrugs.
Hu L, Wu X, Han J, Chen L, Vass SO, Browne P, Hall BS, Bot C, Gobalakrishnapillai V, Searle PF, Knox RJ, Wilkinson SR.
Bioorg Med Chem Lett (2011) 21 : 3986 -3991
PubMed 21620697 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 5.21 5.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1257018 1 5.89
CHEMBL1257017 1 5.51
CHEMBL1256991 1 5.33
CHEMBL1257016 1 5.23
CHEMBL2158073 1 5.08
CHEMBL1256990 1 5.04
CHEMBL1256965 1 4.81
CHEMBL1256401 1 4.79
CHEMBL1256928 1 -
CHEMBL1256964 1 -
CHEMBL2158071 1 -
CHEMBL2158072 1 -
CHEMBL2158074 1 -
CHEMBL2158075 1 -
CHEMBL144896 1 -
CHEMBL1256989 1 -
CHEMBL2158184 1 -
CHEMBL2158185 1 -
CHEMBL2158186 1 -
CHEMBL2158187 1 -
CHEMBL1256966 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1257018 IC50 = 1290.0 nM 5.89
CHEMBL1257017 IC50 = 3100.0 nM 5.51
CHEMBL1256991 IC50 = 4720.0 nM 5.33
CHEMBL1257016 IC50 = 5880.0 nM 5.23
CHEMBL2158073 IC50 = 8300.0 nM 5.08
CHEMBL1256990 IC50 = 9050.0 nM 5.04
CHEMBL1256965 IC50 = 15600.0 nM 4.81
CHEMBL1256401 IC50 = 16230.0 nM 4.79
CHEMBL1256928 IC50 > 30000.0 nM -
CHEMBL1256964 IC50 > 30000.0 nM -
CHEMBL2158071 IC50 > 30000.0 nM -
CHEMBL2158072 IC50 > 30000.0 nM -
CHEMBL2158074 IC50 - -
CHEMBL2158075 IC50 - -
CHEMBL144896 IC50 > 30000.0 nM -
CHEMBL1256989 IC50 > 30000.0 nM -
CHEMBL2158184 IC50 - -
CHEMBL2158185 IC50 - -
CHEMBL2158186 IC50 - -
CHEMBL2158187 IC50 - -
CHEMBL1256966 IC50 > 30000.0 nM -