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Compound Detail

CHEMBL1091931

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O=c1[nH]c(=O)n([C@H]2C[C@H](n3cc(-c4ccccc4)nn3)[C@@H](CO)O2)cc1/C=C/Br

Basic Information

ChEMBL ID CHEMBL1091931
Phase Preclinical
Structure Type MOL
InChI Key DMKMKCDASKTBRN-GBTQTLIESA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

460.3
MW (Da)
1.68
ALogP
8
HBA
2
HBD
115.0
PSA (Ų)
0.60
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C19H18BrN5O4
MW 460.29
Aromatic Rings 3
Heavy Atoms 29
NP-Likeness -0.18

Activity Summary

IC50 4 meas. best 6.6

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Thymidine kinase 2, mitochondrial
CHEMBL4580
IC50 6.6 6.6 250.0 1
Deoxynucleoside kinase
CHEMBL4760
IC50 5.54 5.54 2900.0 1
Unchecked
CHEMBL612545
IC50 5.43 5.43 3700.0 1
Thymidine kinase
CHEMBL1795127
IC50 4.44 4.44 36000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
20218622 10.1021/jm901532h Thymidine kinase, cytosolic 1
20218622 10.1021/jm901532h Thymidine kinase 2, mitochondrial 1
20218622 10.1021/jm901532h Thymidine kinase 1
20218622 10.1021/jm901532h Unchecked 1
20218622 10.1021/jm901532h Deoxynucleoside kinase 1

Data from ChEMBL 36 via Core Engine