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Assay Detail

CHEMBL4182341

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

Functional
Antitrypanosomal activity against Trypanosoma brucei brucei 427 bloodstream forms
34
Total Activities
30
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

Assessment of a pretomanid analogue library for African trypanosomiasis: Hit-to-lead studies on 6-substituted 2-nitro-6,7-dihydro-5H-imidazo[2,1-b][1,3]thiazine 8-oxides.
Thompson AM, Marshall AJ, Maes L, Yarlett N, Bacchi CJ, Gaukel E, Wring SA, Launay D, Braillard S, Chatelain E, Mowbray CE, Denny WA.
Bioorg Med Chem Lett (2018) 28 : 207 -213
PubMed 29191556 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 34 5.65 7.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL480726 1 7.52
CHEMBL4218022 2 7.52
CHEMBL481740 1 7.01
CHEMBL4217401 1 6.85
CHEMBL480569 2 6.57
CHEMBL480727 1 5.96
CHEMBL4211049 2 5.92
CHEMBL480728 1 5.85
CHEMBL4203611 2 5.80
CHEMBL4216414 1 5.37
CHEMBL4204439 1 5.25
CHEMBL4216446 1 4.82
CHEMBL4215751 1 4.80
CHEMBL4208438 1 4.72
CHEMBL4206242 1 4.47
CHEMBL4212632 1 4.40
CHEMBL480559 1 4.36
CHEMBL4211008 1 -
CHEMBL480196 1 -
CHEMBL1836597 1 -
CHEMBL4203482 1 -
CHEMBL4209260 1 -
CHEMBL3608950 1 -
CHEMBL489293 1 -
CHEMBL1836445 1 -
CHEMBL4211261 1 -
CHEMBL3608951 1 -
CHEMBL4207256 1 -
CHEMBL4202539 1 -
CHEMBL2347704 ACOZIBOROLE 2.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4218022 IC50 = 30.0 nM 7.52
CHEMBL480726 IC50 = 30.0 nM 7.52
CHEMBL4218022 IC50 = 75.0 nM 7.12
CHEMBL481740 IC50 = 97.0 nM 7.01
CHEMBL4217401 IC50 = 140.0 nM 6.85
CHEMBL480569 IC50 = 270.0 nM 6.57
CHEMBL480727 IC50 = 1100.0 nM 5.96
CHEMBL4211049 IC50 = 1200.0 nM 5.92
CHEMBL480728 IC50 = 1400.0 nM 5.85
CHEMBL4203611 IC50 = 1600.0 nM 5.80
CHEMBL4216414 IC50 = 4300.0 nM 5.37
CHEMBL4204439 IC50 = 5600.0 nM 5.25
CHEMBL480569 IC50 = 5600.0 nM 5.25
CHEMBL4216446 IC50 = 15000.0 nM 4.82
CHEMBL4215751 IC50 = 16000.0 nM 4.80
CHEMBL4211049 IC50 = 17000.0 nM 4.77
CHEMBL4208438 IC50 = 19000.0 nM 4.72
CHEMBL4206242 IC50 = 34000.0 nM 4.47
CHEMBL4212632 IC50 = 40000.0 nM 4.40
CHEMBL480559 IC50 = 44000.0 nM 4.36
CHEMBL4203611 IC50 = 55000.0 nM 4.26
CHEMBL4211008 IC50 > 64000.0 nM -
CHEMBL480196 IC50 = 3.0 ug.mL-1 -
CHEMBL1836597 IC50 = 2.8 ug.mL-1 -
CHEMBL4203482 IC50 = 2.7 ug.mL-1 -
CHEMBL4209260 IC50 = 2.2 ug.mL-1 -
CHEMBL3608950 IC50 = 0.83 ug.mL-1 -
CHEMBL489293 IC50 = 0.78 ug.mL-1 -
CHEMBL1836445 IC50 = 0.53 ug.mL-1 -
CHEMBL4211261 IC50 = 0.46 ug.mL-1 -
CHEMBL3608951 IC50 = 0.28 ug.mL-1 -
CHEMBL4207256 IC50 = 0.23 ug.mL-1 -
CHEMBL4202539 IC50 = 0.13 ug.mL-1 -
CHEMBL2347704 ACOZIBOROLE IC50 = 0.29 ug.mL-1 -