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Assay Detail

CHEMBL5505339

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

Functional
Antitrypanosomal activity against bloodstream-stage Trypanosoma brucei measured after 72 hrs by alamar blue assay
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Trypanosoma brucei (CHEMBL612849)
Type ORGANISM
Organism Trypanosoma brucei

Publication

Structure-Activity Study on Substituted, Core-Extended, and Dyad Naphthalene Diimide G-Quadruplex Ligands Leading to Potent Antitrypanosomal Agents.
Benassi A, Peñalver P, Pérez-Soto M, Pirota V, Freccero M, Morales JC, Doria F.
J Med Chem (2024) 67 : 10643 -10654
PubMed 38924701 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 6.96 10.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5505832 1 10.05
CHEMBL4594805 1 9.59
CHEMBL4095630 1 8.05
CHEMBL4597995 1 7.82
CHEMBL4068055 1 7.77
CHEMBL5542928 1 7.68
CHEMBL4079866 1 7.62
CHEMBL5556792 1 7.50
CHEMBL255733 1 7.27
CHEMBL5518020 1 7.24
CHEMBL5531983 1 7.21
CHEMBL5542708 1 6.54
CHEMBL5557605 1 6.26
CHEMBL5557014 1 5.60
CHEMBL5555465 1 5.07
CHEMBL5557778 1 5.02
CHEMBL257367 1 4.67
CHEMBL5523407 1 4.37

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5505832 IC50 = 0.09 nM 10.05
CHEMBL4594805 IC50 = 0.26 nM 9.59
CHEMBL4095630 IC50 = 9.0 nM 8.05
CHEMBL4597995 IC50 = 15.0 nM 7.82
CHEMBL4068055 IC50 = 17.0 nM 7.77
CHEMBL5542928 IC50 = 21.0 nM 7.68
CHEMBL4079866 IC50 = 24.0 nM 7.62
CHEMBL5556792 IC50 = 32.0 nM 7.50
CHEMBL255733 IC50 = 54.0 nM 7.27
CHEMBL5518020 IC50 = 57.0 nM 7.24
CHEMBL5531983 IC50 = 61.0 nM 7.21
CHEMBL5542708 IC50 = 290.0 nM 6.54
CHEMBL5557605 IC50 = 550.0 nM 6.26
CHEMBL5557014 IC50 = 2500.0 nM 5.60
CHEMBL5555465 IC50 = 8500.0 nM 5.07
CHEMBL5557778 IC50 = 9500.0 nM 5.02
CHEMBL257367 IC50 = 21500.0 nM 4.67
CHEMBL5523407 IC50 = 42700.0 nM 4.37