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Assay Detail

CHEMBL4433746

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

Functional
Antitrypanosomal activity against Trypanosoma brucei bloodstream form after 72 hrs by resazurin dye-based assay relative to control
18
Total Activities
18
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

Trypanosoma brucei (CHEMBL612849)
Type ORGANISM
Organism Trypanosoma brucei

Publication

SAR Studies and Biological Characterization of a Chromen-4-one Derivative as an Anti-<i>Trypanosoma brucei</i> Agent.
Borsari C, Santarem N, Macedo S, Jiménez-Antón MD, Torrado JJ, Olías-Molero AI, Corral MJ, Tait A, Ferrari S, Costantino L, Luciani R, Ponterini G, Gul S, Kuzikov M, Ellinger B, Behrens B, Reinshagen J, Alunda JM, Cordeiro-da-Silva A, Costi MP.
ACS Med Chem Lett (2019) 10 : 528 -533
PubMed 30996791 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 17 5.97 6.52
IC50 1 8.81 8.81

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL55 PENTAMIDINE 4.0 1 8.81
CHEMBL4454558 1 6.52
CHEMBL4450031 1 6.40
CHEMBL4438593 1 6.40
CHEMBL4587075 1 6.30
CHEMBL4438244 1 6.30
CHEMBL4472620 1 6.22
CHEMBL4436174 1 5.96
CHEMBL4474158 1 5.62
CHEMBL1523114 1 5.54
CHEMBL4438557 1 5.51
CHEMBL4460239 1 5.42
CHEMBL4585927 1 5.39
CHEMBL4571788 1 -
CHEMBL4585618 1 -
CHEMBL4455272 1 -
CHEMBL4446341 1 -
CHEMBL4476298 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL55 PENTAMIDINE IC50 = 1.55 nM 8.81
CHEMBL4454558 EC50 = 300.0 nM 6.52
CHEMBL4450031 EC50 = 400.0 nM 6.40
CHEMBL4438593 EC50 = 400.0 nM 6.40
CHEMBL4587075 EC50 = 500.0 nM 6.30
CHEMBL4438244 EC50 = 500.0 nM 6.30
CHEMBL4472620 EC50 = 600.0 nM 6.22
CHEMBL4436174 EC50 = 1100.0 nM 5.96
CHEMBL4474158 EC50 = 2400.0 nM 5.62
CHEMBL1523114 EC50 = 2900.0 nM 5.54
CHEMBL4438557 EC50 = 3100.0 nM 5.51
CHEMBL4460239 EC50 = 3800.0 nM 5.42
CHEMBL4585927 EC50 = 4100.0 nM 5.39
CHEMBL4571788 EC50 > 10000.0 nM -
CHEMBL4585618 EC50 > 10000.0 nM -
CHEMBL4455272 EC50 > 10000.0 nM -
CHEMBL4446341 EC50 > 10000.0 nM -
CHEMBL4476298 EC50 > 10000.0 nM -