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Assay Detail

CHEMBL4673724

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

Functional
Antitrypanosomal activity against Trypanosoma brucei brucei 427 assessed as parasite growth inhibition incubated for 48 hrs by resazurin dye based assay
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Investigation of thiazolyl-benzothiophenamides as potential agents for African sleeping sickness
Brown, Ronald W., Abdel-Megeed, Ashraf M., Keller, Paul A., Jones, Amy J., Sykes, Melissa L., Kaiser, Marcel, Baell, Jonathan B., Avery, Vicky M., Hyland, Christopher J. T.
RSC Med Chem (2020) 11 : 1413 -1422
PubMed 34095848 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 5.92 8.67

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL55 PENTAMIDINE 4.0 1 8.67
CHEMBL469912 PUROMYCIN 2.0 1 7.28
CHEMBL35241 DIMINAZENE 2.0 1 7.19
CHEMBL4785398 1 6.50
CHEMBL2095053 1 6.14
CHEMBL4761032 1 6.12
CHEMBL4786148 1 5.85
CHEMBL4781989 1 5.66
CHEMBL4790578 1 5.64
CHEMBL4741937 1 5.60
CHEMBL4784166 1 5.55
CHEMBL4789055 1 5.54
CHEMBL4754984 1 5.23
CHEMBL4749932 1 5.20
CHEMBL4759609 1 5.18
CHEMBL4741005 1 5.14
CHEMBL4791691 1 5.11
CHEMBL4796387 1 5.03
CHEMBL4751801 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL55 PENTAMIDINE IC50 = 2.13 nM 8.67
CHEMBL469912 PUROMYCIN IC50 = 51.97 nM 7.28
CHEMBL35241 DIMINAZENE IC50 = 64.1 nM 7.19
CHEMBL4785398 IC50 = 320.0 nM 6.50
CHEMBL2095053 IC50 = 730.0 nM 6.14
CHEMBL4761032 IC50 = 750.0 nM 6.12
CHEMBL4786148 IC50 = 1410.0 nM 5.85
CHEMBL4781989 IC50 = 2210.0 nM 5.66
CHEMBL4790578 IC50 = 2270.0 nM 5.64
CHEMBL4741937 IC50 = 2500.0 nM 5.60
CHEMBL4784166 IC50 = 2790.0 nM 5.55
CHEMBL4789055 IC50 = 2910.0 nM 5.54
CHEMBL4754984 IC50 = 5860.0 nM 5.23
CHEMBL4749932 IC50 = 6380.0 nM 5.20
CHEMBL4759609 IC50 = 6530.0 nM 5.18
CHEMBL4741005 IC50 = 7230.0 nM 5.14
CHEMBL4791691 IC50 = 7770.0 nM 5.11
CHEMBL4796387 IC50 = 9390.0 nM 5.03
CHEMBL4751801 IC50 - -