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Assay Detail

CHEMBL3878511

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

Functional
Antitrypanosomal activity against Trypanosoma brucei 427 bloodstream forms assessed as parasitic growth inhibition after 48 hrs by alamar blue assay
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Publication

Structure-guided design of novel Trypanosoma brucei Methionyl-tRNA synthetase inhibitors.
Huang W, Zhang Z, Barros-Álvarez X, Koh CY, Ranade RM, Gillespie JR, Creason SA, Shibata S, Verlinde CLMJ, Hol WGJ, Buckner FS, Fan E.
Eur J Med Chem (2016) 124 : 1081 -1092
PubMed 27788467 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 30 6.06 9.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL55 PENTAMIDINE 4.0 1 9.05
CHEMBL3978033 1 7.66
CHEMBL3953659 1 7.41
CHEMBL3969840 1 7.21
CHEMBL3962406 1 7.09
CHEMBL3938391 1 6.51
CHEMBL3963464 1 6.46
CHEMBL3920674 1 6.45
CHEMBL3940296 1 6.27
CHEMBL3902001 1 6.24
CHEMBL3893388 1 6.00
CHEMBL3925534 1 5.98
CHEMBL3973685 1 5.86
CHEMBL3968743 1 5.85
CHEMBL3964014 1 5.81
CHEMBL3982490 1 5.74
CHEMBL3926341 1 5.71
CHEMBL3957698 1 5.67
CHEMBL3952954 1 5.49
CHEMBL3942072 1 5.48
CHEMBL3937165 1 5.42
CHEMBL3970772 1 5.34
CHEMBL3919401 1 5.05
CHEMBL3982361 1 5.05
CHEMBL3930540 1 5.04
CHEMBL3965873 1 4.88
CHEMBL3893578 1 4.82
CHEMBL3935989 1 -
CHEMBL3974359 1 -
CHEMBL3944785 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL55 PENTAMIDINE EC50 = 0.9 nM 9.05
CHEMBL3978033 EC50 = 22.0 nM 7.66
CHEMBL3953659 EC50 = 39.0 nM 7.41
CHEMBL3969840 EC50 = 61.0 nM 7.21
CHEMBL3962406 EC50 = 82.0 nM 7.09
CHEMBL3938391 EC50 = 307.0 nM 6.51
CHEMBL3963464 EC50 = 343.0 nM 6.46
CHEMBL3920674 EC50 = 359.0 nM 6.45
CHEMBL3940296 EC50 = 539.0 nM 6.27
CHEMBL3902001 EC50 = 580.0 nM 6.24
CHEMBL3893388 EC50 = 999.0 nM 6.00
CHEMBL3925534 EC50 = 1058.0 nM 5.98
CHEMBL3973685 EC50 = 1397.0 nM 5.86
CHEMBL3968743 EC50 = 1399.0 nM 5.85
CHEMBL3964014 EC50 = 1539.0 nM 5.81
CHEMBL3982490 EC50 = 1813.0 nM 5.74
CHEMBL3926341 EC50 = 1952.0 nM 5.71
CHEMBL3957698 EC50 = 2154.0 nM 5.67
CHEMBL3952954 EC50 = 3260.0 nM 5.49
CHEMBL3942072 EC50 = 3334.0 nM 5.48
CHEMBL3937165 EC50 = 3763.0 nM 5.42
CHEMBL3970772 EC50 = 4603.0 nM 5.34
CHEMBL3919401 EC50 = 8810.0 nM 5.05
CHEMBL3982361 EC50 = 8802.0 nM 5.05
CHEMBL3930540 EC50 = 9013.0 nM 5.04
CHEMBL3965873 EC50 = 13311.0 nM 4.88
CHEMBL3893578 EC50 = 15263.0 nM 4.82
CHEMBL3935989 EC50 > 20000.0 nM -
CHEMBL3974359 EC50 > 20000.0 nM -
CHEMBL3944785 EC50 > 5000.0 nM -