Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL870813

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

Functional
Trypanocidal activity against Trypanosoma brucei brucei after 48 hrs
ChEMBL ↗
56
Total Activities
51
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

Trypanosoma brucei brucei (CHEMBL612851) ↗
Type ORGANISM
Organism Trypanosoma brucei brucei

Publication

Aziridine-2,3-dicarboxylate inhibitors targeting the major cysteine protease of Trypanosoma brucei as lead trypanocidal agents.
Vicik R, Hoerr V, Glaser M, Schultheis M, Hansell E, McKerrow JH, Holzgrabe U, Caffrey CR, Ponte-Sucre A, Moll H, Stich A, Schirmeister T.
Bioorg Med Chem Lett (2006) 16 : 2753 -2757
PubMed 16516467 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 51 4.97 8.59
MIC 5 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL166 MELARSOPROL 3.0 1 8.59
CHEMBL361506 PENTAMIDINE ISETHIONATE 4.0 1 8.54
CHEMBL413376 SURAMIN HEXASODIUM 3.0 2 6.51
CHEMBL290960 NIFURTIMOX 4.0 2 5.47
CHEMBL378288 — — 2 4.96
CHEMBL383647 — — 2 4.96
CHEMBL377682 — — 1 4.69
CHEMBL207838 — — 1 4.69
CHEMBL1201037 EFLORNITHINE HYDROCHLORIDE 4.0 2 4.64
CHEMBL208156 — — 1 4.59
CHEMBL379406 — — 1 4.59
CHEMBL379355 — — 1 4.59
CHEMBL380077 — — 1 4.59
CHEMBL377947 — — 1 4.57
CHEMBL377676 — — 1 4.56
CHEMBL382910 — — 1 4.55
CHEMBL379509 — — 1 4.52
CHEMBL439510 — — 1 4.51
CHEMBL208129 — — 1 4.51
CHEMBL380076 — — 1 4.50
CHEMBL208297 — — 1 4.47
CHEMBL379571 — — 1 4.47
CHEMBL379572 — — 1 4.46
CHEMBL382388 — — 1 4.46
CHEMBL378902 — — 1 4.45
CHEMBL208263 — — 1 4.44
CHEMBL184629 — — 1 4.44
CHEMBL207643 — — 1 -
CHEMBL208369 — — 1 -
CHEMBL206043 — — 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL166 MELARSOPROL IC50 = 2.6 nM 8.59
CHEMBL361506 PENTAMIDINE ISETHIONATE IC50 = 2.9 nM 8.54
CHEMBL413376 SURAMIN HEXASODIUM IC50 = 310.0 nM 6.51
CHEMBL290960 NIFURTIMOX IC50 = 3400.0 nM 5.47
CHEMBL378288 — IC50 = 11100.0 nM 4.96
CHEMBL383647 — IC50 = 10900.0 nM 4.96
CHEMBL377682 — IC50 = 20600.0 nM 4.69
CHEMBL207838 — IC50 = 20600.0 nM 4.69
CHEMBL1201037 EFLORNITHINE HYDROCHLORIDE IC50 = 22900.0 nM 4.64
CHEMBL208156 — IC50 = 25700.0 nM 4.59
CHEMBL379355 — IC50 = 25600.0 nM 4.59
CHEMBL379406 — IC50 = 25600.0 nM 4.59
CHEMBL380077 — IC50 = 25800.0 nM 4.59
CHEMBL377947 — IC50 = 26700.0 nM 4.57
CHEMBL377676 — IC50 = 27600.0 nM 4.56
CHEMBL382910 — IC50 = 28300.0 nM 4.55
CHEMBL379509 — IC50 = 30500.0 nM 4.52
CHEMBL208129 — IC50 = 30800.0 nM 4.51
CHEMBL439510 — IC50 = 30800.0 nM 4.51
CHEMBL380076 — IC50 = 31400.0 nM 4.50
CHEMBL208297 — IC50 = 34000.0 nM 4.47
CHEMBL379571 — IC50 = 34000.0 nM 4.47
CHEMBL379572 — IC50 = 34300.0 nM 4.46
CHEMBL382388 — IC50 = 34300.0 nM 4.46
CHEMBL378902 — IC50 = 35200.0 nM 4.45
CHEMBL208263 — IC50 = 36400.0 nM 4.44
CHEMBL184629 — IC50 = 36400.0 nM 4.44
CHEMBL413376 SURAMIN HEXASODIUM MIC = 1000.0 nM -
CHEMBL382431 — IC50 > 100000.0 nM -
CHEMBL380337 — IC50 > 100000.0 nM -
CHEMBL379944 — IC50 > 100000.0 nM -
CHEMBL206360 — IC50 - — -
CHEMBL208182 — IC50 - — -
CHEMBL207643 — IC50 - — -
CHEMBL207391 — IC50 - — -
CHEMBL380466 — IC50 - — -
CHEMBL383647 — MIC = 125000.0 nM -
CHEMBL1201037 EFLORNITHINE HYDROCHLORIDE MIC > 1000000.0 nM -
CHEMBL290960 NIFURTIMOX MIC = 200000.0 nM -
CHEMBL378288 — MIC = 125000.0 nM -
CHEMBL208369 — IC50 - — -
CHEMBL206043 — IC50 > 100000.0 nM -
CHEMBL383531 — IC50 - — -
CHEMBL207070 — IC50 > 100000.0 nM -
CHEMBL207092 — IC50 > 100000.0 nM -
CHEMBL208418 — IC50 > 100000.0 nM -
CHEMBL377650 — IC50 > 100000.0 nM -
CHEMBL441354 — IC50 > 100000.0 nM -
CHEMBL206415 — IC50 > 100000.0 nM -
CHEMBL207526 — IC50 > 100000.0 nM -