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Compound Detail

CHEMBL1814762

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Nc1ncnc2c1c(-c1ccccc1)cn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O

Basic Information

ChEMBL ID CHEMBL1814762
Phase Preclinical
Structure Type MOL
InChI Key SAFLKKGMJZQGAJ-LSCFUAHRSA-N
4
Targets
4
Activities
2
Assay Types
0
PK Parameters
20
Publications
0
Known Names

Molecular Properties

342.4
MW (Da)
0.29
ALogP
8
HBA
4
HBD
126.7
PSA (Ų)
0.54
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C17H18N4O4
MW 342.36
Aromatic Rings 3
Heavy Atoms 25
NP-Likeness 0.72

Activity Summary

EC50 3 meas. best 5.39
IC50 1 meas. best 5.87

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Mycobacterium tuberculosis
CHEMBL360
IC50 5.87 5.87 1340.0 1
Trypanosoma brucei rhodesiense
CHEMBL612348
EC50 5.39 5.39 4100.0 1
Trypanosoma brucei brucei
CHEMBL612851
EC50 4.49 4.49 32300.0 1
MRC5
CHEMBL614181
EC50 4.25 4.25 56200.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
21711054 10.1021/jm2005173 DU-145 7
25259627 10.1021/jm500497v Mycobacterium tuberculosis 3
30677668 10.1016/j.ejmech.2018.12.050 Unchecked 2
25259627 10.1021/jm500497v Unchecked 2
21711054 10.1021/jm2005173 NON-PROTEIN TARGET 1
27485386 10.1016/j.bmcl.2016.07.041 Histone-lysine N-methyltransferase, H3 lysine-79 specific 1
30677668 10.1016/j.ejmech.2018.12.050 Trypanosoma brucei brucei 1
25259627 10.1021/jm500497v Adenosine kinase 1
25259627 10.1021/jm500497v BJ 1
25259627 10.1021/jm500497v MRC5 1
21711054 10.1021/jm2005173 Adenosine kinase 1
21711054 10.1021/jm2005173 CCRF-CEM 1
21711054 10.1021/jm2005173 A549 1
21711054 10.1021/jm2005173 HL-60 1
21711054 10.1021/jm2005173 MT4 1
21711054 10.1021/jm2005173 BT-549 1
21711054 10.1021/jm2005173 Unchecked 1
21711054 10.1021/jm2005173 HCT-15 1
21711054 10.1021/jm2005173 HCT-116 1
21711054 10.1021/jm2005173 PC-3 1

Data from ChEMBL 36 via Core Engine