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Compound Detail

CHEMBL4871173

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C#Cc1cn([C@@H]2O[C@H](CO)[C@@H](F)[C@H]2O)c2ncnc(N)c12

Basic Information

ChEMBL ID CHEMBL4871173
Phase Preclinical
Structure Type MOL
InChI Key BXFBVBWMXUNDDL-QYVSTXNMSA-N
6
Targets
6
Activities
1
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

292.3
MW (Da)
-0.42
ALogP
7
HBA
3
HBD
106.4
PSA (Ų)
0.65
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C13H13FN4O3
MW 292.27
Aromatic Rings 2
Heavy Atoms 21
NP-Likeness 0.38

Activity Summary

EC50 6 meas. best 7.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Trypanosoma brucei rhodesiense
CHEMBL612348
EC50 7.7 7.7 20.0 1
Trypanosoma cruzi
CHEMBL368
EC50 7.4 7.4 40.0 1
Trypanosoma brucei brucei
CHEMBL612851
EC50 7.4 7.4 40.0 1
Macrophage
CHEMBL5314319
EC50 6.89 6.89 130.0 1
Leishmania infantum
CHEMBL612848
EC50 6.89 6.89 130.0 1
MRC5
CHEMBL614181
EC50 6.8 6.8 160.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
33667845 10.1016/j.ejmech.2021.113290 ADMET 4
33667845 10.1016/j.ejmech.2021.113290 Trypanosoma brucei brucei 1
33667845 10.1016/j.ejmech.2021.113290 Macrophage 1
33667845 10.1016/j.ejmech.2021.113290 Leishmania infantum 1
33667845 10.1016/j.ejmech.2021.113290 MRC5 1
33667845 10.1016/j.ejmech.2021.113290 Trypanosoma cruzi 1
33667845 10.1016/j.ejmech.2021.113290 Trypanosoma brucei rhodesiense 1

Data from ChEMBL 36 via Core Engine