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Assay Detail

CHEMBL4771960

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

Functional
Antileishmanial activity against Trypanosoma brucei brucei AnTat 1.9 measured after 74 hrs by Alamar blue assay
18
Total Activities
18
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

8-Alkynyl-3-nitroimidazopyridines display potent antitrypanosomal activity against both T. b. brucei and cruzi.
Fersing C,Boudot C,Castera-Ducros C,Pinault E,Hutter S,Paoli-Lombardo R,Primas N,Pedron J,Seguy L,Bourgeade-Delmas S,Sournia-Saquet A,Stigliani JL,Brossas JY,Paris L,Valentin A,Wyllie S,Fairlamb AH,Boutet-Robinet É,Corvaisier S,Since M,Malzert-Fréon A,Destere A,Mazier D,Rathelot P,Courtioux B,Azas N,Verhaeghe P,Vanelle P
Eur J Med Chem (2020) 202 : 112558 -112558
PubMed 32652409 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 18 6.45 7.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL265502 SURAMIN 3.0 1 7.52
CHEMBL4779309 1 7.40
CHEMBL4787217 1 7.16
CHEMBL4780415 1 7.00
CHEMBL4791697 1 7.00
CHEMBL4786409 1 6.92
CHEMBL4798919 1 6.92
CHEMBL4786627 1 6.89
CHEMBL4782051 1 6.80
CHEMBL4781286 1 6.80
CHEMBL4277324 1 6.60
CHEMBL1631694 FEXINIDAZOLE 4.0 1 6.22
CHEMBL4795526 1 5.89
CHEMBL4534157 1 5.89
CHEMBL290960 NIFURTIMOX 4.0 1 5.58
CHEMBL2441910 1 5.54
CHEMBL4788481 1 5.17
CHEMBL830 EFLORNITHINE 4.0 1 4.88

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL265502 SURAMIN EC50 = 30.0 nM 7.52
CHEMBL4779309 EC50 = 40.0 nM 7.40
CHEMBL4787217 EC50 = 70.0 nM 7.16
CHEMBL4780415 EC50 = 100.0 nM 7.00
CHEMBL4791697 EC50 = 100.0 nM 7.00
CHEMBL4786409 EC50 = 120.0 nM 6.92
CHEMBL4798919 EC50 = 120.0 nM 6.92
CHEMBL4786627 EC50 = 130.0 nM 6.89
CHEMBL4782051 EC50 = 160.0 nM 6.80
CHEMBL4781286 EC50 = 160.0 nM 6.80
CHEMBL4277324 EC50 = 250.0 nM 6.60
CHEMBL1631694 FEXINIDAZOLE EC50 = 600.0 nM 6.22
CHEMBL4795526 EC50 = 1300.0 nM 5.89
CHEMBL4534157 EC50 = 1300.0 nM 5.89
CHEMBL290960 NIFURTIMOX EC50 = 2600.0 nM 5.58
CHEMBL2441910 EC50 = 2900.0 nM 5.54
CHEMBL4788481 EC50 = 6800.0 nM 5.17
CHEMBL830 EFLORNITHINE EC50 = 13300.0 nM 4.88