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Assay Detail

CHEMBL4773771

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

Functional
Antitrypanosomal activity against bloodstream form Trypanosoma brucei brucei AnTat 1.9 trypomastigotes assessed as reduction in parasite viability incubated for 69 hrs by Alamar Blue dye based assay
25
Total Activities
25
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

Antikinetoplastid SAR study in 3-nitroimidazopyridine series: Identification of a novel non-genotoxic and potent anti-T. b. brucei hit-compound with improved pharmacokinetic properties.
Fersing C,Boudot C,Paoli-Lombardo R,Primas N,Pinault E,Hutter S,Castera-Ducros C,Kabri Y,Pedron J,Bourgeade-Delmas S,Sournia-Saquet A,Stigliani JL,Valentin A,Azqueta A,Muruzabal D,Destere A,Wyllie S,Fairlamb AH,Corvaisier S,Since M,Malzert-Fréon A,Di Giorgio C,Rathelot P,Azas N,Courtioux B,Vanelle P,Verhaeghe P
Eur J Med Chem (2020) 206 : 112668 -112668
PubMed 32795774 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 25 6.36 7.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4776584 1 7.77
CHEMBL4794493 1 7.70
CHEMBL4792432 1 7.60
CHEMBL265502 SURAMIN 3.0 1 7.52
CHEMBL4789978 1 7.17
CHEMBL4793961 1 7.07
CHEMBL4797467 1 6.77
CHEMBL4798187 1 6.52
CHEMBL4783616 1 6.40
CHEMBL4785404 1 6.30
CHEMBL1631694 FEXINIDAZOLE 4.0 1 6.22
CHEMBL4788930 1 5.92
CHEMBL4784988 1 5.92
CHEMBL4777198 1 5.82
CHEMBL4783344 1 5.75
CHEMBL4792857 1 5.66
CHEMBL290960 NIFURTIMOX 4.0 1 5.58
CHEMBL4780635 1 5.40
CHEMBL4791331 1 5.14
CHEMBL830 EFLORNITHINE 4.0 1 4.88
CHEMBL4781188 1 -
CHEMBL4783634 1 -
CHEMBL4791191 1 -
CHEMBL4799356 1 -
CHEMBL4777308 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4776584 EC50 = 17.0 nM 7.77
CHEMBL4794493 EC50 = 20.0 nM 7.70
CHEMBL4792432 EC50 = 25.0 nM 7.60
CHEMBL265502 SURAMIN EC50 = 30.0 nM 7.52
CHEMBL4789978 EC50 = 67.0 nM 7.17
CHEMBL4793961 EC50 = 85.0 nM 7.07
CHEMBL4797467 EC50 = 170.0 nM 6.77
CHEMBL4798187 EC50 = 300.0 nM 6.52
CHEMBL4783616 EC50 = 400.0 nM 6.40
CHEMBL4785404 EC50 = 500.0 nM 6.30
CHEMBL1631694 FEXINIDAZOLE EC50 = 600.0 nM 6.22
CHEMBL4788930 EC50 = 1200.0 nM 5.92
CHEMBL4784988 EC50 = 1200.0 nM 5.92
CHEMBL4777198 EC50 = 1500.0 nM 5.82
CHEMBL4783344 EC50 = 1800.0 nM 5.75
CHEMBL4792857 EC50 = 2200.0 nM 5.66
CHEMBL290960 NIFURTIMOX EC50 = 2600.0 nM 5.58
CHEMBL4780635 EC50 = 4000.0 nM 5.40
CHEMBL4791331 EC50 = 7200.0 nM 5.14
CHEMBL830 EFLORNITHINE EC50 = 13300.0 nM 4.88
CHEMBL4781188 EC50 > 50000.0 nM -
CHEMBL4783634 EC50 > 50000.0 nM -
CHEMBL4791191 EC50 > 50000.0 nM -
CHEMBL4799356 EC50 > 50000.0 nM -
CHEMBL4777308 EC50 > 50000.0 nM -