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Assay Detail

CHEMBL4269478

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

Functional
Antitrypanosomal activity against Trypanosoma brucei brucei 427 after 48 hrs by presto blue dye based fluorescence assay
14
Total Activities
14
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

Series of Alkynyl-Substituted Thienopyrimidines as Inhibitors of Protozoan Parasite Proliferation.
Woodring JL, Behera R, Sharma A, Wiedeman J, Patel G, Singh B, Guyett P, Amata E, Erath J, Roncal N, Penn E, Leed SE, Rodriguez A, Sciotti RJ, Mensa-Wilmot K, Pollastri MP.
ACS Med Chem Lett (2018) 9 : 996 -1001
PubMed 30344906 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 14 6.12 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL265502 SURAMIN 3.0 1 7.40
CHEMBL495979 1 6.66
CHEMBL496174 1 6.58
CHEMBL4284550 1 6.55
CHEMBL4291341 1 6.12
CHEMBL4291524 1 6.00
CHEMBL4280205 1 6.00
CHEMBL4279269 1 5.92
CHEMBL4287195 1 5.89
CHEMBL4285290 1 5.72
CHEMBL4283656 1 5.60
CHEMBL4279896 1 5.60
CHEMBL4281134 1 5.47
CHEMBL4292440 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL265502 SURAMIN EC50 = 40.0 nM 7.40
CHEMBL495979 EC50 = 220.0 nM 6.66
CHEMBL496174 EC50 = 260.0 nM 6.58
CHEMBL4284550 EC50 = 280.0 nM 6.55
CHEMBL4291341 EC50 = 760.0 nM 6.12
CHEMBL4291524 EC50 = 1000.0 nM 6.00
CHEMBL4280205 EC50 = 1000.0 nM 6.00
CHEMBL4279269 EC50 = 1200.0 nM 5.92
CHEMBL4287195 EC50 = 1300.0 nM 5.89
CHEMBL4285290 EC50 = 1900.0 nM 5.72
CHEMBL4283656 EC50 = 2500.0 nM 5.60
CHEMBL4279896 EC50 = 2500.0 nM 5.60
CHEMBL4281134 EC50 = 3400.0 nM 5.47
CHEMBL4292440 EC50 > 2500.0 nM -