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Assay Detail

CHEMBL4274064

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

Functional
Antitrypanosomal activity against trypomastigote stage of Trypanosoma brucei brucei AnTat 1.9 assessed as decrease in parasite viability after 69 hrs by Alamar blue assay
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

8-Aryl-6-chloro-3-nitro-2-(phenylsulfonylmethyl)imidazo[1,2-a]pyridines as potent antitrypanosomatid molecules bioactivated by type 1 nitroreductases.
Fersing C, Boudot C, Pedron J, Hutter S, Primas N, Castera-Ducros C, Bourgeade-Delmas S, Sournia-Saquet A, Moreau A, Cohen A, Stigliani JL, Pratviel G, Crozet MD, Wyllie S, Fairlamb A, Valentin A, Rathelot P, Azas N, Courtioux B, Verhaeghe P, Vanelle P.
Eur J Med Chem (2018) 157 : 115 -126
PubMed 30092366 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 6.58 7.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL265502 SURAMIN 3.0 1 7.52
CHEMBL4288624 1 7.40
CHEMBL4280716 1 7.16
CHEMBL4290803 1 7.10
CHEMBL4282515 1 7.05
CHEMBL4290387 1 6.82
CHEMBL4280330 1 6.80
CHEMBL4278089 1 6.70
CHEMBL4285279 1 6.64
CHEMBL4277324 1 6.60
CHEMBL4290964 1 6.51
CHEMBL4280160 1 6.39
CHEMBL4294199 1 6.37
CHEMBL1631694 FEXINIDAZOLE 4.0 1 6.22
CHEMBL4276734 1 6.21
CHEMBL2441910 1 5.54
CHEMBL222838 EFLORNITHINE, (S)- 2.0 1 4.88

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL265502 SURAMIN IC50 = 30.0 nM 7.52
CHEMBL4288624 IC50 = 40.0 nM 7.40
CHEMBL4280716 IC50 = 70.0 nM 7.16
CHEMBL4290803 IC50 = 80.0 nM 7.10
CHEMBL4282515 IC50 = 90.0 nM 7.05
CHEMBL4290387 IC50 = 150.0 nM 6.82
CHEMBL4280330 IC50 = 160.0 nM 6.80
CHEMBL4278089 IC50 = 200.0 nM 6.70
CHEMBL4285279 IC50 = 230.0 nM 6.64
CHEMBL4277324 IC50 = 250.0 nM 6.60
CHEMBL4290964 IC50 = 310.0 nM 6.51
CHEMBL4280160 IC50 = 410.0 nM 6.39
CHEMBL4294199 IC50 = 430.0 nM 6.37
CHEMBL1631694 FEXINIDAZOLE IC50 = 600.0 nM 6.22
CHEMBL4276734 IC50 = 610.0 nM 6.21
CHEMBL2441910 IC50 = 2900.0 nM 5.54
CHEMBL222838 EFLORNITHINE, (S)- IC50 = 13300.0 nM 4.88