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Assay Detail

CHEMBL4683799

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

Functional
Antitrypanosomal activity against Trypanosoma brucei brucei assessed as reduction in parasite growth incubated for 3 days by resazurin dye based fluorescence assay
38
Total Activities
38
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

C6-O-alkylated 7-deazainosine nucleoside analogues: Discovery of potent and selective anti-sleeping sickness agents.
Hulpia F,Bouton J,Campagnaro GD,Alfayez IA,Mabille D,Maes L,de Koning HP,Caljon G,Van Calenbergh S
Eur J Med Chem (2020) 188 : 112018 -112018
PubMed 31931339 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 38 6.28 7.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL265502 SURAMIN 3.0 1 7.55
CHEMBL4798238 1 7.24
CHEMBL4761450 1 7.16
CHEMBL4746708 1 7.15
CHEMBL4787682 1 7.09
CHEMBL4759567 1 7.06
CHEMBL4764835 1 7.05
CHEMBL4796615 1 7.02
CHEMBL4776070 1 7.00
CHEMBL4756706 1 6.92
CHEMBL4748068 1 6.89
CHEMBL4750953 1 6.89
CHEMBL4793350 1 6.89
CHEMBL4780795 1 6.80
CHEMBL4789184 1 6.77
CHEMBL4750292 1 6.72
CHEMBL4798411 1 6.70
CHEMBL3127048 1 6.66
CHEMBL4793729 1 6.40
CHEMBL4062813 1 6.31
CHEMBL4743800 1 5.96
CHEMBL4793826 1 5.70
CHEMBL4782040 1 5.58
CHEMBL1688967 IMMUNICILLIN H 1 5.38
CHEMBL4788754 1 5.09
CHEMBL4750096 1 4.97
CHEMBL4750345 1 4.53
CHEMBL3126882 1 4.49
CHEMBL4752787 1 4.28
CHEMBL4779408 1 4.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL265502 SURAMIN EC50 = 28.0 nM 7.55
CHEMBL4798238 EC50 = 58.0 nM 7.24
CHEMBL4761450 EC50 = 69.0 nM 7.16
CHEMBL4746708 EC50 = 71.0 nM 7.15
CHEMBL4787682 EC50 = 81.0 nM 7.09
CHEMBL4759567 EC50 = 88.0 nM 7.06
CHEMBL4764835 EC50 = 90.0 nM 7.05
CHEMBL4796615 EC50 = 95.0 nM 7.02
CHEMBL4776070 EC50 = 100.0 nM 7.00
CHEMBL4756706 EC50 = 120.0 nM 6.92
CHEMBL4750953 EC50 = 130.0 nM 6.89
CHEMBL4793350 EC50 = 130.0 nM 6.89
CHEMBL4748068 EC50 = 130.0 nM 6.89
CHEMBL4780795 EC50 = 160.0 nM 6.80
CHEMBL4789184 EC50 = 170.0 nM 6.77
CHEMBL4750292 EC50 = 190.0 nM 6.72
CHEMBL4798411 EC50 = 200.0 nM 6.70
CHEMBL3127048 EC50 = 220.0 nM 6.66
CHEMBL4793729 EC50 = 400.0 nM 6.40
CHEMBL4062813 EC50 = 490.0 nM 6.31
CHEMBL4743800 EC50 = 1100.0 nM 5.96
CHEMBL4793826 EC50 = 2010.0 nM 5.70
CHEMBL4782040 EC50 = 2600.0 nM 5.58
CHEMBL1688967 IMMUNICILLIN H EC50 = 4200.0 nM 5.38
CHEMBL4788754 EC50 = 8100.0 nM 5.09
CHEMBL4750096 EC50 = 10700.0 nM 4.97
CHEMBL4750345 EC50 = 29600.0 nM 4.53
CHEMBL3126882 EC50 = 32200.0 nM 4.49
CHEMBL4752787 EC50 = 52400.0 nM 4.28
CHEMBL4779408 EC50 = 57300.0 nM 4.24
CHEMBL4798285 EC50 > 64000.0 nM -
CHEMBL4797695 EC50 > 64000.0 nM -
CHEMBL519587 EC50 > 64000.0 nM -
CHEMBL4757825 EC50 > 64000.0 nM -
CHEMBL179482 EC50 > 64000.0 nM -
CHEMBL4753445 EC50 > 64000.0 nM -
CHEMBL3127045 EC50 > 64000.0 nM -
CHEMBL4782563 EC50 > 64000.0 nM -