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Assay Detail

CHEMBL4395365

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

Functional
Antitrypanosomal activity against bloodstream form of Trypanosoma brucei gambiense Feo reduction in parasite growth after 72 hrs by resazurin dye based fluorescence assay
93
Total Activities
93
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Trypanosoma brucei gambiense (CHEMBL613768)
Type ORGANISM
Organism Trypanosoma brucei gambiense

Publication

Thiazolidinone/thiazole based hybrids - New class of antitrypanosomal agents.
Kryshchyshyn A, Kaminskyy D, Karpenko O, Gzella A, Grellier P, Lesyk R.
Eur J Med Chem (2019) 174 : 292 -308
PubMed 31051403 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 93 5.68 8.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL55 PENTAMIDINE 4.0 1 8.82
CHEMBL4567421 1 6.96
CHEMBL4525222 1 6.85
CHEMBL4584106 1 6.68
CHEMBL4539329 1 6.64
CHEMBL4573628 1 6.64
CHEMBL4448818 1 6.42
CHEMBL4534015 1 6.32
CHEMBL4550734 1 6.29
CHEMBL4590538 1 6.28
CHEMBL4586951 1 6.26
CHEMBL4444305 1 6.20
CHEMBL4465788 1 6.19
CHEMBL4516857 1 6.19
CHEMBL4466415 1 6.18
CHEMBL4542841 1 6.13
CHEMBL4452686 1 6.13
CHEMBL4548473 1 6.09
CHEMBL4529689 1 6.07
CHEMBL4464531 1 6.00
CHEMBL4466329 1 6.00
CHEMBL4465706 1 6.00
CHEMBL4459419 1 5.93
CHEMBL4461037 1 5.92
CHEMBL4555640 1 5.87
CHEMBL4575536 1 5.87
CHEMBL4542097 1 5.87
CHEMBL4575070 1 5.85
CHEMBL4442067 1 5.85
CHEMBL4553912 1 5.83

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL55 PENTAMIDINE IC50 = 1.5 nM 8.82
CHEMBL4567421 IC50 = 110.0 nM 6.96
CHEMBL4525222 IC50 = 140.0 nM 6.85
CHEMBL4584106 IC50 = 210.0 nM 6.68
CHEMBL4539329 IC50 = 230.0 nM 6.64
CHEMBL4573628 IC50 = 230.0 nM 6.64
CHEMBL4448818 IC50 = 380.0 nM 6.42
CHEMBL4534015 IC50 = 476.0 nM 6.32
CHEMBL4550734 IC50 = 510.0 nM 6.29
CHEMBL4590538 IC50 = 530.0 nM 6.28
CHEMBL4586951 IC50 = 549.0 nM 6.26
CHEMBL4444305 IC50 = 631.0 nM 6.20
CHEMBL4465788 IC50 = 652.0 nM 6.19
CHEMBL4516857 IC50 = 639.0 nM 6.19
CHEMBL4466415 IC50 = 660.0 nM 6.18
CHEMBL4542841 IC50 = 745.0 nM 6.13
CHEMBL4452686 IC50 = 740.0 nM 6.13
CHEMBL4548473 IC50 = 820.0 nM 6.09
CHEMBL4529689 IC50 = 860.0 nM 6.07
CHEMBL4464531 IC50 = 1000.0 nM 6.00
CHEMBL4466329 IC50 = 1000.0 nM 6.00
CHEMBL4465706 IC50 = 1000.0 nM 6.00
CHEMBL4459419 IC50 = 1170.0 nM 5.93
CHEMBL4461037 IC50 = 1200.0 nM 5.92
CHEMBL4542097 IC50 = 1350.0 nM 5.87
CHEMBL4575536 IC50 = 1360.0 nM 5.87
CHEMBL4555640 IC50 = 1340.0 nM 5.87
CHEMBL4575070 IC50 = 1400.0 nM 5.85
CHEMBL4442067 IC50 = 1420.0 nM 5.85
CHEMBL4553912 IC50 = 1490.0 nM 5.83
CHEMBL4534243 IC50 = 1500.0 nM 5.82
CHEMBL4534866 IC50 = 1500.0 nM 5.82
CHEMBL4513643 IC50 = 1500.0 nM 5.82
CHEMBL4459719 IC50 = 1500.0 nM 5.82
CHEMBL4453087 IC50 = 1500.0 nM 5.82
CHEMBL4441230 IC50 = 1520.0 nM 5.82
CHEMBL4547259 IC50 = 1590.0 nM 5.80
CHEMBL4471985 IC50 = 1710.0 nM 5.77
CHEMBL4455555 IC50 = 1710.0 nM 5.77
CHEMBL4439331 IC50 = 2220.0 nM 5.65
CHEMBL4469373 IC50 = 2300.0 nM 5.64
CHEMBL4587856 IC50 = 2600.0 nM 5.58
CHEMBL4440961 IC50 = 2600.0 nM 5.58
CHEMBL4461800 IC50 = 2700.0 nM 5.57
CHEMBL4560449 IC50 = 2700.0 nM 5.57
CHEMBL4443875 IC50 = 2820.0 nM 5.55
CHEMBL4449971 IC50 = 3000.0 nM 5.52
CHEMBL4574851 IC50 = 3200.0 nM 5.50
CHEMBL4518463 IC50 = 3340.0 nM 5.48
CHEMBL4569425 IC50 = 3600.0 nM 5.44