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Compound Detail

CHEMBL4755821

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N#C[C@@]1(c2cc(Br)c3c(N)ncnn23)O[C@H](CO)[C@@H](O)[C@H]1O

Basic Information

ChEMBL ID CHEMBL4755821
Phase Preclinical
Structure Type MOL
InChI Key SAPYHDLLBVNOKN-CWLXEDRGSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

370.2
MW (Da)
-1.09
ALogP
9
HBA
4
HBD
149.9
PSA (Ų)
0.52
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 C12H12BrN5O4
MW 370.16
Aromatic Rings 2
Heavy Atoms 22
NP-Likeness 0.41

Activity Summary

IC50 4 meas. best 5.8

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Trypanosoma brucei rhodesiense
CHEMBL612348
IC50 5.8 5.8 1580.0 1
Trypanosoma brucei brucei
CHEMBL612851
IC50 4.89 4.89 13000.0 1
Leishmania infantum
CHEMBL612848
IC50 4.49 4.49 32500.0 1
Trypanosoma cruzi
CHEMBL368
IC50 4.41 4.41 39300.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
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