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Assay Detail

CHEMBL3859765

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

Functional
Antitrypanosomal activity against Trypanosoma brucei brucei Lister 427 VSG 221 [TetR T7RNAP] transgenic bloodstream forms assessed as reduction in cell viability after 48 hrs by alamar blue assay
53
Total Activities
53
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Publication

Targeting the HSP60/10 chaperonin systems of Trypanosoma brucei as a strategy for treating African sleeping sickness.
Abdeen S, Salim N, Mammadova N, Summers CM, Goldsmith-Pestana K, McMahon-Pratt D, Schultz PG, Horwich AL, Chapman E, Johnson SM.
Bioorg Med Chem Lett (2016) 26 : 5247 -5253
PubMed 27720295 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 53 5.13 6.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL265502 SURAMIN 3.0 1 6.92
CHEMBL3950773 1 5.75
CHEMBL3934460 1 5.68
CHEMBL3979736 1 5.62
CHEMBL3978830 1 5.57
CHEMBL290960 NIFURTIMOX 4.0 1 5.55
CHEMBL3115908 1 5.51
CHEMBL3975683 1 5.50
CHEMBL3954893 1 5.48
CHEMBL3947198 1 5.48
CHEMBL3952406 1 5.43
CHEMBL3908434 1 5.39
CHEMBL3913878 1 5.37
CHEMBL3904891 1 5.35
CHEMBL3970551 1 5.32
CHEMBL3890411 1 5.31
CHEMBL3910488 1 5.30
CHEMBL3919412 1 5.29
CHEMBL3983712 1 5.23
CHEMBL3903813 1 5.19
CHEMBL3942054 1 5.10
CHEMBL3938421 1 5.05
CHEMBL3894879 1 5.00
CHEMBL3928317 1 4.96
CHEMBL3919336 1 4.89
CHEMBL3966262 1 4.82
CHEMBL3955935 1 4.82
CHEMBL3906378 1 4.80
CHEMBL3975456 1 4.77
CHEMBL3937258 1 4.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL265502 SURAMIN EC50 = 120.0 nM 6.92
CHEMBL3950773 EC50 = 1800.0 nM 5.75
CHEMBL3934460 EC50 = 2100.0 nM 5.68
CHEMBL3979736 EC50 = 2400.0 nM 5.62
CHEMBL3978830 EC50 = 2700.0 nM 5.57
CHEMBL290960 NIFURTIMOX EC50 = 2800.0 nM 5.55
CHEMBL3115908 EC50 = 3100.0 nM 5.51
CHEMBL3975683 EC50 = 3200.0 nM 5.50
CHEMBL3954893 EC50 = 3300.0 nM 5.48
CHEMBL3947198 EC50 = 3300.0 nM 5.48
CHEMBL3952406 EC50 = 3700.0 nM 5.43
CHEMBL3908434 EC50 = 4100.0 nM 5.39
CHEMBL3913878 EC50 = 4300.0 nM 5.37
CHEMBL3904891 EC50 = 4500.0 nM 5.35
CHEMBL3970551 EC50 = 4800.0 nM 5.32
CHEMBL3890411 EC50 = 4900.0 nM 5.31
CHEMBL3910488 EC50 = 5000.0 nM 5.30
CHEMBL3919412 EC50 = 5100.0 nM 5.29
CHEMBL3983712 EC50 = 5900.0 nM 5.23
CHEMBL3903813 EC50 = 6400.0 nM 5.19
CHEMBL3942054 EC50 = 8000.0 nM 5.10
CHEMBL3938421 EC50 = 8900.0 nM 5.05
CHEMBL3894879 EC50 = 10000.0 nM 5.00
CHEMBL3928317 EC50 = 11000.0 nM 4.96
CHEMBL3919336 EC50 = 13000.0 nM 4.89
CHEMBL3966262 EC50 = 15000.0 nM 4.82
CHEMBL3955935 EC50 = 15000.0 nM 4.82
CHEMBL3906378 EC50 = 16000.0 nM 4.80
CHEMBL3975456 EC50 = 17000.0 nM 4.77
CHEMBL3937258 EC50 = 18000.0 nM 4.75
CHEMBL3922861 EC50 = 19000.0 nM 4.72
CHEMBL3986320 EC50 = 21000.0 nM 4.68
CHEMBL3943318 EC50 = 22000.0 nM 4.66
CHEMBL3915348 EC50 = 23000.0 nM 4.64
CHEMBL3952045 EC50 = 23000.0 nM 4.64
CHEMBL3951335 EC50 = 25000.0 nM 4.60
CHEMBL3983061 EC50 = 28000.0 nM 4.55
CHEMBL3960743 EC50 = 28000.0 nM 4.55
CHEMBL3899371 EC50 = 28000.0 nM 4.55
CHEMBL3934352 EC50 = 39000.0 nM 4.41
CHEMBL3967047 EC50 > 42000.0 nM -
CHEMBL3894125 EC50 > 42000.0 nM -
CHEMBL3924724 EC50 > 42000.0 nM -
CHEMBL3933283 EC50 > 42000.0 nM -
CHEMBL3980253 EC50 > 42000.0 nM -
CHEMBL3912547 EC50 > 42000.0 nM -
CHEMBL3907505 EC50 > 42000.0 nM -
CHEMBL3924343 EC50 > 42000.0 nM -
CHEMBL3978029 EC50 > 42000.0 nM -
CHEMBL830 EFLORNITHINE EC50 > 42000.0 nM -