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Assay Detail

CHEMBL3074979

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

Functional
Trypanocidal activity against Trypanosoma brucei brucei 427 bloodstream form assessed as inhibition of parasite proliferation after 72 hr by Lilit Alamar Blue method
31
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Trypanosoma brucei brucei
Confidence 1 — Organism
Curated By Autocuration

Target

Trypanosoma brucei brucei (CHEMBL612851)
Type ORGANISM
Organism Trypanosoma brucei brucei

Publication

Structureactivity relationship study of thiosemicarbazones on an African trypanosome: Trypanosoma brucei brucei
Fatondji HR, Kpoviessi S, Gbaguidi F, Bero J, Hannaert V, Quetin-Leclercq J, Poupaert J, Moudachirou M, Accrombessi GC
Med Chem Res (2013) 22 : 2151 -2162
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 31 4.60 5.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2297585 1 5.40
CHEMBL2297586 1 5.29
CHEMBL162738 1 5.08
CHEMBL1974077 ACETONAPHTHONE-THIOSEMICARBAZONE 1 5.02
CHEMBL310957 P-CHLOROPHENYL(METHYL)THIOSEMICARBAZONE 1 4.96
CHEMBL2297582 1 4.75
CHEMBL258261 1 4.57
CHEMBL2297580 CARVONE-THIOSEMICARBAZONE 1 4.40
CHEMBL2297579 1 4.34
CHEMBL1269809 BENZOPHENONE-THIOSEMICARBAZONE 1 4.17
CHEMBL2297590 1 4.15
CHEMBL388025 CINNAMALDEHYDE THIOSEMICARBAZONE 1 4.12
CHEMBL2297594 1 4.08
CHEMBL404699 1 4.04
CHEMBL1341853 1 -
CHEMBL2297583 1 -
CHEMBL2297581 1 -
CHEMBL2297600 1 -
CHEMBL2297599 1 -
CHEMBL2297598 1 -
CHEMBL2297597 1 -
CHEMBL2297596 1 -
CHEMBL2297595 1 -
CHEMBL2297593 1 -
CHEMBL2297592 1 -
CHEMBL2297591 BENZALDEHYDE-THIOSEMICARBAZONE 1 -
CHEMBL2297587 1 -
CHEMBL2297589 1 -
CHEMBL256868 ACETOPHENONE-THIOSEMICARBAZONE 1 -
CHEMBL2297588 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2297585 IC50 = 3970.0 nM 5.40
CHEMBL2297586 IC50 = 5190.0 nM 5.29
CHEMBL162738 IC50 = 8380.0 nM 5.08
CHEMBL1974077 ACETONAPHTHONE-THIOSEMICARBAZONE IC50 = 9620.0 nM 5.02
CHEMBL310957 P-CHLOROPHENYL(METHYL)THIOSEMICARBAZONE IC50 = 11060.0 nM 4.96
CHEMBL2297582 IC50 = 17710.0 nM 4.75
CHEMBL258261 IC50 = 26890.0 nM 4.57
CHEMBL2297580 CARVONE-THIOSEMICARBAZONE IC50 = 39710.0 nM 4.40
CHEMBL2297579 IC50 = 45580.0 nM 4.34
CHEMBL1269809 BENZOPHENONE-THIOSEMICARBAZONE IC50 = 68340.0 nM 4.17
CHEMBL2297590 IC50 = 70400.0 nM 4.15
CHEMBL388025 CINNAMALDEHYDE THIOSEMICARBAZONE IC50 = 76280.0 nM 4.12
CHEMBL2297594 IC50 = 82640.0 nM 4.08
CHEMBL404699 IC50 = 91140.0 nM 4.04
CHEMBL2297584 IC50 - -
CHEMBL1341853 IC50 = 146800.0 nM -
CHEMBL2297583 IC50 = 135850.0 nM -
CHEMBL2297581 IC50 = 260210.0 nM -
CHEMBL2297600 IC50 = 292530.0 nM -
CHEMBL2297599 IC50 = 170350.0 nM -
CHEMBL2297598 IC50 = 221500.0 nM -
CHEMBL2297597 IC50 = 123600.0 nM -
CHEMBL2297596 IC50 = 132400.0 nM -
CHEMBL2297595 IC50 = 258800.0 nM -
CHEMBL2297593 IC50 = 163640.0 nM -
CHEMBL2297592 IC50 = 220000.0 nM -
CHEMBL2297591 BENZALDEHYDE-THIOSEMICARBAZONE IC50 = 443540.0 nM -
CHEMBL2297587 IC50 - -
CHEMBL2297589 IC50 = 199370.0 nM -
CHEMBL256868 ACETOPHENONE-THIOSEMICARBAZONE IC50 = 211880.0 nM -
CHEMBL2297588 IC50 - -