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Assay Detail

CHEMBL4384236

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

Functional
Antiparasitic activity against bloodstream form of Trypanosoma brucei brucei strain 427 after 48 hrs by resazurin dye-based assay
91
Total Activities
48
Compounds Tested
2
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

Design, Synthesis, and Biological Evaluation of 2-Nitroimidazopyrazin-one/-es with Antitubercular and Antiparasitic Activity.
Jarrad AM, Ang CW, Debnath A, Hahn HJ, Woods K, Tan L, Sykes ML, Jones AJ, Pelingon R, Butler MS, Avery VM, West NP, Karoli T, Blaskovich MAT, Cooper MA.
J Med Chem (2018) 61 : 11349 -11371
PubMed 30468386 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 89 5.90 8.70
Activity 2 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL55 PENTAMIDINE 4.0 2 8.70
CHEMBL469912 PUROMYCIN 2.0 2 7.30
CHEMBL380216 DIMINAZENE DIACETURATE 2 7.21
CHEMBL4539535 2 6.70
CHEMBL4580469 2 6.62
CHEMBL4435234 2 6.60
CHEMBL4469243 2 6.40
CHEMBL4466152 2 6.39
CHEMBL4579641 2 6.30
CHEMBL4434831 2 6.20
CHEMBL4453745 2 6.11
CHEMBL4453153 2 6.10
CHEMBL4562001 2 6.00
CHEMBL4563622 2 5.96
CHEMBL4587216 2 5.92
CHEMBL4516883 2 5.90
CHEMBL4580019 2 5.90
CHEMBL4549044 2 5.90
CHEMBL4468508 2 5.82
CHEMBL4527225 2 5.72
CHEMBL4530876 2 5.70
CHEMBL4455542 2 5.66
CHEMBL4474388 2 5.60
CHEMBL4548055 2 5.54
CHEMBL4434866 2 5.54
CHEMBL4514632 2 5.44
CHEMBL4467473 2 5.40
CHEMBL4575552 2 5.34
CHEMBL4456553 2 5.30
CHEMBL4437138 2 5.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL55 PENTAMIDINE IC50 = 2.0 nM 8.70
CHEMBL55 PENTAMIDINE IC50 = 1.995 nM 8.70
CHEMBL469912 PUROMYCIN IC50 = 50.0 nM 7.30
CHEMBL469912 PUROMYCIN IC50 = 50.12 nM 7.30
CHEMBL380216 DIMINAZENE DIACETURATE IC50 = 62.0 nM 7.21
CHEMBL380216 DIMINAZENE DIACETURATE IC50 = 63.1 nM 7.20
CHEMBL4539535 IC50 = 199.53 nM 6.70
CHEMBL4539535 IC50 = 220.0 nM 6.66
CHEMBL4580469 IC50 = 240.0 nM 6.62
CHEMBL4435234 IC50 = 250.0 nM 6.60
CHEMBL4435234 IC50 = 251.19 nM 6.60
CHEMBL4469243 IC50 = 398.11 nM 6.40
CHEMBL4469243 IC50 = 400.0 nM 6.40
CHEMBL4466152 IC50 = 410.0 nM 6.39
CHEMBL4579641 IC50 = 501.19 nM 6.30
CHEMBL4579641 IC50 = 560.0 nM 6.25
CHEMBL4434831 IC50 = 630.96 nM 6.20
CHEMBL4434831 IC50 = 650.0 nM 6.19
CHEMBL4453745 IC50 = 780.0 nM 6.11
CHEMBL4453745 IC50 = 794.33 nM 6.10
CHEMBL4453153 IC50 = 794.33 nM 6.10
CHEMBL4453153 IC50 = 860.0 nM 6.07
CHEMBL4562001 IC50 = 1000.0 nM 6.00
CHEMBL4563622 IC50 = 1100.0 nM 5.96
CHEMBL4562001 IC50 = 1100.0 nM 5.96
CHEMBL4587216 IC50 = 1200.0 nM 5.92
CHEMBL4563622 IC50 = 1258.93 nM 5.90
CHEMBL4587216 IC50 = 1258.93 nM 5.90
CHEMBL4580019 IC50 = 1258.93 nM 5.90
CHEMBL4516883 IC50 = 1258.93 nM 5.90
CHEMBL4549044 IC50 = 1258.93 nM 5.90
CHEMBL4549044 IC50 = 1400.0 nM 5.85
CHEMBL4580019 IC50 = 1400.0 nM 5.85
CHEMBL4516883 IC50 = 1400.0 nM 5.85
CHEMBL4468508 IC50 = 1500.0 nM 5.82
CHEMBL4468508 IC50 = 1584.89 nM 5.80
CHEMBL4527225 IC50 = 1900.0 nM 5.72
CHEMBL4527225 IC50 = 1995.26 nM 5.70
CHEMBL4580469 IC50 = 1995.26 nM 5.70
CHEMBL4530876 IC50 = 1995.26 nM 5.70
CHEMBL4530876 IC50 = 2100.0 nM 5.68
CHEMBL4455542 IC50 = 2200.0 nM 5.66
CHEMBL4455542 IC50 = 2511.89 nM 5.60
CHEMBL4474388 IC50 = 2511.89 nM 5.60
CHEMBL4474388 IC50 = 2600.0 nM 5.58
CHEMBL4434866 IC50 = 2900.0 nM 5.54
CHEMBL4548055 IC50 = 2900.0 nM 5.54
CHEMBL4434866 IC50 = 3162.28 nM 5.50
CHEMBL4548055 IC50 = 3162.28 nM 5.50
CHEMBL4514632 IC50 = 3600.0 nM 5.44