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Assay Detail

CHEMBL4345836

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

Functional
Antitrypanosomal activity against Trypanosoma brucei brucei AnTat 1.9 trypomastigotes assessed as reduction in parasite viability incubated for 69 hrs by Alamar Blue dye based assay
21
Total Activities
21
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

New 8-Nitroquinolinone Derivative Displaying Submicromolar in Vitro Activities against Both Trypanosoma brucei and cruzi.
Pedron J, Boudot C, Brossas JY, Pinault E, Bourgeade-Delmas S, Sournia-Saquet A, Boutet-Robinet E, Destere A, Tronnet A, Bergé J, Bonduelle C, Deraeve C, Pratviel G, Stigliani JL, Paris L, Mazier D, Corvaisier S, Since M, Malzert-Fréon A, Wyllie S, Milne R, Fairlamb AH, Valentin A, Courtioux B, Verhaeghe P.
ACS Med Chem Lett (2020) 11 : 464 -472
PubMed 32292551 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 21 6.21 7.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4565434 1 7.92
CHEMBL265502 SURAMIN 3.0 1 7.52
CHEMBL4566278 1 7.30
CHEMBL4575234 1 7.16
CHEMBL4482886 1 7.00
CHEMBL4559873 1 6.70
CHEMBL4556532 1 6.70
CHEMBL1631694 FEXINIDAZOLE 4.0 1 6.40
CHEMBL4534870 1 6.24
CHEMBL4449777 1 6.07
CHEMBL4559890 1 6.00
CHEMBL4172543 1 5.92
CHEMBL4547155 1 5.82
CHEMBL4445909 1 5.77
CHEMBL4569720 1 5.06
CHEMBL830 EFLORNITHINE 4.0 1 4.88
CHEMBL4439484 1 4.68
CHEMBL2042573 1 4.63
CHEMBL4537323 1 -
CHEMBL4588561 1 -
CHEMBL4547753 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4565434 EC50 = 12.0 nM 7.92
CHEMBL265502 SURAMIN EC50 = 30.0 nM 7.52
CHEMBL4566278 EC50 = 50.0 nM 7.30
CHEMBL4575234 EC50 = 70.0 nM 7.16
CHEMBL4482886 EC50 = 100.0 nM 7.00
CHEMBL4559873 EC50 = 200.0 nM 6.70
CHEMBL4556532 EC50 = 200.0 nM 6.70
CHEMBL1631694 FEXINIDAZOLE EC50 = 400.0 nM 6.40
CHEMBL4534870 EC50 = 570.0 nM 6.24
CHEMBL4449777 EC50 = 850.0 nM 6.07
CHEMBL4559890 EC50 = 1000.0 nM 6.00
CHEMBL4172543 EC50 = 1200.0 nM 5.92
CHEMBL4547155 EC50 = 1500.0 nM 5.82
CHEMBL4445909 EC50 = 1700.0 nM 5.77
CHEMBL4569720 EC50 = 8700.0 nM 5.06
CHEMBL830 EFLORNITHINE EC50 = 13300.0 nM 4.88
CHEMBL4439484 EC50 = 20900.0 nM 4.68
CHEMBL2042573 EC50 = 23400.0 nM 4.63
CHEMBL4537323 EC50 > 50000.0 nM -
CHEMBL4588561 EC50 > 50000.0 nM -
CHEMBL4547753 EC50 > 50000.0 nM -