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Assay Detail

CHEMBL5388059

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

Functional
Antitrypanosomal activity against wild type Trypanosoma brucei M1.2 Lister 427 trypomastigotes form assessed as parasite growth inhibition incubated for 48 hrs
34
Total Activities
34
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

Design, synthesis and biological evaluations of quinolone amides against African trypanosomiasis with improved solubility.
Weinmann J, Kirchner L, Engstler M, Meinel L, Holzgrabe U.
Eur J Med Chem (2023) 250 : 115176 -115176
PubMed 36805945 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 34 6.24 7.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5406814 1 7.66
CHEMBL2031131 1 7.33
CHEMBL4171343 1 7.30
CHEMBL5400512 1 7.22
CHEMBL5413915 1 7.00
CHEMBL5434449 1 6.89
CHEMBL5433907 1 6.82
CHEMBL5426284 1 6.75
CHEMBL5397254 1 6.75
CHEMBL4161155 1 6.64
CHEMBL5408292 1 6.60
CHEMBL5393768 1 6.52
CHEMBL5414568 1 6.33
CHEMBL5439162 1 6.28
CHEMBL5431717 1 6.26
CHEMBL5413859 1 6.14
CHEMBL5412681 1 6.10
CHEMBL5435312 1 6.07
CHEMBL5412118 1 6.00
CHEMBL5431656 1 5.97
CHEMBL5435951 1 5.95
CHEMBL5394145 1 5.94
CHEMBL5412052 1 5.81
CHEMBL5412770 1 5.74
CHEMBL5406369 1 5.71
CHEMBL5436970 1 5.53
CHEMBL5424089 1 5.43
CHEMBL5439977 1 5.43
CHEMBL5408711 1 5.38
CHEMBL5401587 1 5.38

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5406814 IC50 = 22.0 nM 7.66
CHEMBL2031131 IC50 = 47.0 nM 7.33
CHEMBL4171343 IC50 = 50.0 nM 7.30
CHEMBL5400512 IC50 = 60.0 nM 7.22
CHEMBL5413915 IC50 = 100.0 nM 7.00
CHEMBL5434449 IC50 = 130.0 nM 6.89
CHEMBL5433907 IC50 = 150.0 nM 6.82
CHEMBL5426284 IC50 = 180.0 nM 6.75
CHEMBL5397254 IC50 = 180.0 nM 6.75
CHEMBL4161155 IC50 = 230.0 nM 6.64
CHEMBL5408292 IC50 = 250.0 nM 6.60
CHEMBL5393768 IC50 = 300.0 nM 6.52
CHEMBL5414568 IC50 = 470.0 nM 6.33
CHEMBL5439162 IC50 = 520.0 nM 6.28
CHEMBL5431717 IC50 = 550.0 nM 6.26
CHEMBL5413859 IC50 = 720.0 nM 6.14
CHEMBL5412681 IC50 = 800.0 nM 6.10
CHEMBL5435312 IC50 = 860.0 nM 6.07
CHEMBL5412118 IC50 = 1010.0 nM 6.00
CHEMBL5431656 IC50 = 1080.0 nM 5.97
CHEMBL5435951 IC50 = 1120.0 nM 5.95
CHEMBL5394145 IC50 = 1150.0 nM 5.94
CHEMBL5412052 IC50 = 1550.0 nM 5.81
CHEMBL5412770 IC50 = 1830.0 nM 5.74
CHEMBL5406369 IC50 = 1930.0 nM 5.71
CHEMBL5436970 IC50 = 2970.0 nM 5.53
CHEMBL5424089 IC50 = 3720.0 nM 5.43
CHEMBL5439977 IC50 = 3740.0 nM 5.43
CHEMBL5408711 IC50 = 4220.0 nM 5.38
CHEMBL5401587 IC50 = 4180.0 nM 5.38
CHEMBL5440063 IC50 = 4400.0 nM 5.36
CHEMBL5398475 IC50 = 4720.0 nM 5.33
CHEMBL5401927 IC50 > 20000.0 nM -
CHEMBL5393944 IC50 > 20000.0 nM -