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Assay Detail

CHEMBL5035311

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

Functional
Antitrypanosomal activity against bloodstream form of Trypanosoma brucei brucei measured after 3 to 4 days by Z2 coulter counter based analysis
15
Total Activities
15
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

Self-Masked Aldehyde Inhibitors: A Novel Strategy for Inhibiting Cysteine Proteases.
Li L, Chenna BC, Yang KS, Cole TR, Goodall ZT, Giardini M, Moghadamchargari Z, Hernandez EA, Gomez J, Calvet CM, Bernatchez JA, Mellott DM, Zhu J, Rademacher A, Thomas D, Blankenship LR, Drelich A, Laganowsky A, Tseng CK, Liu WR, Wand AJ, Cruz-Reyes J, Siqueira-Neto JL, Meek TD.
J Med Chem (2021) 64 : 11267 -11287
PubMed 34288674 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 15 5.61 7.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL91704 K-777 2.0 1 7.05
CHEMBL5089591 1 6.30
CHEMBL5084365 1 6.22
CHEMBL124025 DIMINAZEN ACETURATE 1 6.00
CHEMBL5079029 1 5.58
CHEMBL5080091 1 5.57
CHEMBL5092503 1 5.51
CHEMBL128135 1 5.48
CHEMBL5091908 1 5.43
CHEMBL5081709 1 5.40
CHEMBL5079476 1 5.40
CHEMBL5082439 1 5.24
CHEMBL5076256 1 5.17
CHEMBL5082504 1 4.92
CHEMBL5077312 1 4.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL91704 K-777 EC50 = 90.0 nM 7.05
CHEMBL5089591 EC50 = 500.0 nM 6.30
CHEMBL5084365 EC50 = 600.0 nM 6.22
CHEMBL124025 DIMINAZEN ACETURATE EC50 = 990.0 nM 6.00
CHEMBL5079029 EC50 = 2600.0 nM 5.58
CHEMBL5080091 EC50 = 2700.0 nM 5.57
CHEMBL5092503 EC50 = 3100.0 nM 5.51
CHEMBL128135 EC50 = 3300.0 nM 5.48
CHEMBL5091908 EC50 = 3700.0 nM 5.43
CHEMBL5081709 EC50 = 4000.0 nM 5.40
CHEMBL5079476 EC50 = 4000.0 nM 5.40
CHEMBL5082439 EC50 = 5800.0 nM 5.24
CHEMBL5076256 EC50 = 6800.0 nM 5.17
CHEMBL5082504 EC50 = 12000.0 nM 4.92
CHEMBL5077312 EC50 = 14000.0 nM 4.85