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Assay Detail

CHEMBL4183759

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Functional
Antitrypanosomal activity against trypomastigote form of Trypanosoma brucei Squib 427 assessed as parasite growth inhibition after 72 hrs by resazurin assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Trypanosoma brucei (CHEMBL612849)
Type ORGANISM
Organism Trypanosoma brucei

Publication

Targeting a Subpocket in Trypanosoma brucei Phosphodiesterase B1 (TbrPDEB1) Enables the Structure-Based Discovery of Selective Inhibitors with Trypanocidal Activity.
Blaazer AR, Singh AK, de Heuvel E, Edink E, Orrling KM, Veerman JJN, van den Bergh T, Jansen C, Balasubramaniam E, Mooij WJ, Custers H, Sijm M, Tagoe DNA, Kalejaiye TD, Munday JC, Tenor H, Matheeussen A, Wijtmans M, Siderius M, de Graaf C, Maes L, de Koning HP, Bailey DS, Sterk GJ, de Esch IJP, Brown DG, Leurs R.
J Med Chem (2018) 61 : 3870 -3888
PubMed 29672041 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 5.94 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL265502 SURAMIN 3.0 1 7.40
CHEMBL4210475 1 5.26
CHEMBL4204999 1 5.17

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL265502 SURAMIN IC50 = 39.81 nM 7.40
CHEMBL4210475 IC50 = 5500.0 nM 5.26
CHEMBL4204999 IC50 = 6700.0 nM 5.17