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Compound Detail

CHEMBL4750953

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COc1nc(N)nc2c1c(Br)cn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O

Basic Information

ChEMBL ID CHEMBL4750953
Phase Preclinical
Structure Type MOL
InChI Key UIQAGZKPMBFJDJ-IOSLPCCCSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

375.2
MW (Da)
-0.60
ALogP
9
HBA
4
HBD
135.9
PSA (Ų)
0.56
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C12H15BrN4O5
MW 375.18
Aromatic Rings 2
Heavy Atoms 22
NP-Likeness 0.67

Activity Summary

EC50 3 meas. best 7.11

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Trypanosoma brucei rhodesiense
CHEMBL612348
EC50 7.11 7.11 77.0 1
Trypanosoma brucei brucei
CHEMBL612851
EC50 6.89 6.89 130.0 1
MRC5
CHEMBL614181
EC50 5.49 5.49 3240.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
31931339 10.1016/j.ejmech.2019.112018 Unchecked 2
31931339 10.1016/j.ejmech.2019.112018 Trypanosoma brucei brucei 1
31931339 10.1016/j.ejmech.2019.112018 Trypanosoma brucei rhodesiense 1
31931339 10.1016/j.ejmech.2019.112018 MRC5 1

Data from ChEMBL 36 via Core Engine