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Compound Detail

CHEMBL4744476

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Nc1ncnn2c([C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)cc(Br)c12

Basic Information

ChEMBL ID CHEMBL4744476
Phase Preclinical
Structure Type MOL
InChI Key SHFJFZGHKDUWTP-QQRDMOCMSA-N
5
Targets
5
Activities
2
Assay Types
0
PK Parameters
9
Publications
0
Known Names

Molecular Properties

345.1
MW (Da)
-0.77
ALogP
8
HBA
4
HBD
126.1
PSA (Ų)
0.56
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 C11H13BrN4O4
MW 345.15
Aromatic Rings 2
Heavy Atoms 20
NP-Likeness 0.66

Activity Summary

IC50 4 meas. best 6.85
EC50 1 meas. best 7.62

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
EC50 7.62 7.62 24.0 1
Trypanosoma brucei rhodesiense
CHEMBL612348
IC50 6.85 6.85 140.0 1
Trypanosoma cruzi
CHEMBL368
IC50 6.11 6.11 780.0 1
Leishmania infantum
CHEMBL612848
IC50 5.95 5.95 1130.0 1
Trypanosoma brucei brucei
CHEMBL612851
IC50 5.77 5.77 1690.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
32294613 10.1016/j.ejmech.2020.112198 Unchecked 3
32294613 10.1016/j.ejmech.2020.112198 RAW264.7 1
32294613 10.1016/j.ejmech.2020.112198 Norovirus 1
33385837 10.1016/j.ejmech.2020.113101 Trypanosoma brucei brucei 1
33385837 10.1016/j.ejmech.2020.113101 Trypanosoma brucei rhodesiense 1
33385837 10.1016/j.ejmech.2020.113101 Trypanosoma cruzi 1
33385837 10.1016/j.ejmech.2020.113101 Leishmania infantum 1
33385837 10.1016/j.ejmech.2020.113101 Unchecked 1
33385837 10.1016/j.ejmech.2020.113101 Macrophage 1

Data from ChEMBL 36 via Core Engine