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Assay Detail

CHEMBL817915

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

Functional
In vitro activity against bloodstream from trypomastigotes.
4
Total Activities
4
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

An approach to use an unusual adenosine transporter to selectively deliver polyamine analogues to trypanosomes.
Tye CK, Kasinathan G, Barrett MP, Brun R, Doyle VE, Fairlamb AH, Weaver R, Gilbert IH.
Bioorg Med Chem Lett (1998) 8 : 811 -816
PubMed 9871546 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 5.94 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL35241 DIMINAZENE 2.0 1 8.52
CHEMBL166618 1 4.68
CHEMBL167202 1 4.62
CHEMBL355685 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL35241 DIMINAZENE IC50 = 3.0 nM 8.52
CHEMBL166618 IC50 = 21000.0 nM 4.68
CHEMBL167202 IC50 = 24000.0 nM 4.62
CHEMBL355685 IC50 = 110000.0 nM -