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Compound Detail

CHEMBL4084041

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CNc1ncnc2c1ncn2[C@@H]1O[C@H](CN(C)C/C=C\CN)[C@@H](O)[C@H]1O

Basic Information

ChEMBL ID CHEMBL4084041
Phase Preclinical
Structure Type MOL
InChI Key ZDTBJBMINMTIFO-LNNUBQDUSA-N
2
Targets
3
Activities
2
Assay Types
2
PK Parameters
4
Publications
0
Known Names

Molecular Properties

363.4
MW (Da)
-1.07
ALogP
10
HBA
4
HBD
134.6
PSA (Ų)
0.45
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C16H25N7O3
MW 363.42
Aromatic Rings 2
Heavy Atoms 26
NP-Likeness 0.44

Activity Summary

IC50 2 meas. best 6.77
EC50 1 meas. best 6.43

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
IC50 6.77 5.81 170.0 2
Trypanosoma brucei
CHEMBL612849
EC50 6.43 6.43 370.0 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 1.5 hr Homo sapiens
T1/2 1.5 hr Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
28807574 10.1016/j.bmc.2017.07.063 Unchecked 2
28807574 10.1016/j.bmc.2017.07.063 Liver 2
28807574 10.1016/j.bmc.2017.07.063 Trypanosoma brucei 1
28807574 10.1016/j.bmc.2017.07.063 MDCK-MDR1 1

Data from ChEMBL 36 via Core Engine