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Assay Detail

CHEMBL4388231

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

ADMET
Growth inhibition of Trypanosoma brucei bloodstream forms measured after 72 hrs by resazurin-based fluorescence assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Trypanosoma brucei
Confidence 1 — Organism
Curated By Autocuration

Target

Trypanosoma brucei (CHEMBL612849)
Type ORGANISM
Organism Trypanosoma brucei

Publication

Enhancement of Benzothiazoles as Pteridine Reductase-1 Inhibitors for the Treatment of Trypanosomatidic Infections.
Linciano P, Pozzi C, Iacono LD, di Pisa F, Landi G, Bonucci A, Gul S, Kuzikov M, Ellinger B, Witt G, Santarem N, Baptista C, Franco C, Moraes CB, Müller W, Wittig U, Luciani R, Sesenna A, Quotadamo A, Ferrari S, Pöhner I, Cordeiro-da-Silva A, Mangani S, Costantino L, Costi MP.
J Med Chem (2019) 62 : 3989 -4012
PubMed 30908048 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 4 5.96 8.42

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL55 PENTAMIDINE 4.0 1 8.42
CHEMBL4549839 1 5.23
CHEMBL4469761 1 5.16
CHEMBL4462566 1 5.01

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL55 PENTAMIDINE EC50 = 3.8 nM 8.42
CHEMBL4549839 EC50 = 5900.0 nM 5.23
CHEMBL4469761 EC50 = 7000.0 nM 5.16
CHEMBL4462566 EC50 = 9700.0 nM 5.01