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Compound Detail

CHEMBL3143935

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O=C1N=C(Nc2ccccc2)N=C2C1N=CN2[C@H]1C[C@H](O)[C@@H](CO)O1

Basic Information

ChEMBL ID CHEMBL3143935
Phase Preclinical
Structure Type MOL
InChI Key NKCIAXNYJIRBFY-VCKSIFHUSA-N
3
Targets
5
Activities
3
Assay Types
3
PK Parameters
5
Publications
0
Known Names

Molecular Properties

343.3
MW (Da)
-0.43
ALogP
8
HBA
3
HBD
119.1
PSA (Ų)
0.69
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 C16H17N5O4
MW 343.34
Aromatic Rings 1
Heavy Atoms 25
NP-Likeness 0.51

Activity Summary

IC50 2 meas. best 6.52
Ki 2 meas. best 6.52
EC50 1 meas. best 6.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Thymidine kinase
CHEMBL1795127
IC50 6.52 6.52 300.0 1
Thymidine kinase
CHEMBL1795127
Ki 6.52 6.52 300.0 1
Thymidine kinase
CHEMBL1820
EC50 6.52 6.52 300.0 1
Thymidine kinase
CHEMBL1820
Ki 6.16 6.16 700.0 1
Thymidine kinase
CHEMBL3415
IC50 5.6 5.6 2500.0 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 0.125 hr Mus musculus
T1/2 1.0 hr Mus musculus
Vd 0.4 L.kg-1 Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
7837239 10.1021/jm00001a010 Mus musculus 5
7837239 10.1021/jm00001a010 Thymidine kinase 2
2153203 10.1021/jm00163a033 Thymidine kinase 2
2840499 10.1021/jm00403a004 Thymidine kinase 1
2840499 10.1021/jm00403a004 Thymidine kinase, cytosolic 1

Data from ChEMBL 36 via Core Engine