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Assay Detail

CHEMBL4424072

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

Functional
Antitrypanosomal activity against Trypanosoma brucei brucei Squib 427 after 48 hrs by alamar blue assay
29
Total Activities
29
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

Revisiting tubercidin against kinetoplastid parasites: Aromatic substitutions at position 7 improve activity and reduce toxicity.
Hulpia F, Campagnaro GD, Scortichini M, Van Hecke K, Maes L, de Koning HP, Caljon G, Van Calenbergh S.
Eur J Med Chem (2019) 164 : 689 -705
PubMed 30677668 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 29 5.18 7.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL265502 SURAMIN 3.0 1 7.30
CHEMBL4581647 1 6.51
CHEMBL267099 TUBERCIDIN 1 6.32
CHEMBL4527711 1 5.76
CHEMBL4469727 1 5.71
CHEMBL4580402 1 5.65
CHEMBL4464277 1 5.51
CHEMBL4443838 1 5.32
CHEMBL4577276 1 5.32
CHEMBL4451645 1 5.19
CHEMBL4516812 1 5.12
CHEMBL1814766 1 5.11
CHEMBL4458717 1 5.09
CHEMBL4462675 1 5.05
CHEMBL4547306 1 5.05
CHEMBL4561102 1 5.05
CHEMBL4471148 1 5.00
CHEMBL4518380 1 4.83
CHEMBL4461564 1 4.59
CHEMBL4446941 1 4.54
CHEMBL1814762 1 4.49
CHEMBL4448104 1 4.48
CHEMBL4447530 1 4.48
CHEMBL4579242 1 4.42
CHEMBL1814763 1 4.38
CHEMBL4458987 1 4.28
CHEMBL4586792 1 -
CHEMBL4445584 1 -
CHEMBL4476721 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL265502 SURAMIN EC50 = 50.0 nM 7.30
CHEMBL4581647 EC50 = 310.0 nM 6.51
CHEMBL267099 TUBERCIDIN EC50 = 480.0 nM 6.32
CHEMBL4527711 EC50 = 1750.0 nM 5.76
CHEMBL4469727 EC50 = 1950.0 nM 5.71
CHEMBL4580402 EC50 = 2260.0 nM 5.65
CHEMBL4464277 EC50 = 3070.0 nM 5.51
CHEMBL4443838 EC50 = 4770.0 nM 5.32
CHEMBL4577276 EC50 = 4760.0 nM 5.32
CHEMBL4451645 EC50 = 6450.0 nM 5.19
CHEMBL4516812 EC50 = 7580.0 nM 5.12
CHEMBL1814766 EC50 = 7830.0 nM 5.11
CHEMBL4458717 EC50 = 8170.0 nM 5.09
CHEMBL4462675 EC50 = 8920.0 nM 5.05
CHEMBL4547306 EC50 = 8810.0 nM 5.05
CHEMBL4561102 EC50 = 8970.0 nM 5.05
CHEMBL4471148 EC50 = 9900.0 nM 5.00
CHEMBL4518380 EC50 = 14700.0 nM 4.83
CHEMBL4461564 EC50 = 25500.0 nM 4.59
CHEMBL4446941 EC50 = 29100.0 nM 4.54
CHEMBL1814762 EC50 = 32300.0 nM 4.49
CHEMBL4448104 EC50 = 33300.0 nM 4.48
CHEMBL4447530 EC50 = 33300.0 nM 4.48
CHEMBL4579242 EC50 = 38200.0 nM 4.42
CHEMBL1814763 EC50 = 41600.0 nM 4.38
CHEMBL4458987 EC50 = 52400.0 nM 4.28
CHEMBL4586792 EC50 > 64000.0 nM -
CHEMBL4445584 EC50 > 64000.0 nM -
CHEMBL4476721 EC50 > 64000.0 nM -