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Compound Detail

CHEMBL3143491

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Nc1cn([C@H]2C[C@H](O)[C@@H](CO)O2)c(=O)[nH]c1=O

Basic Information

ChEMBL ID CHEMBL3143491
Phase Preclinical
Structure Type MOL
InChI Key OZMVAFPILSPXRM-RRKCRQDMSA-N
1
Targets
4
Activities
2
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

243.2
MW (Da)
-2.24
ALogP
7
HBA
4
HBD
130.6
PSA (Ų)
0.46
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C9H13N3O5
MW 243.22
Aromatic Rings 1
Heavy Atoms 17
NP-Likeness 1.03

Activity Summary

Ki 3 meas. best 4.14
IC50 1 meas.

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Thymidine kinase 2
CHEMBL5489
Ki 4.14 4.14 72000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Thymidine kinase 2 Ki = 72000.0 nM 4.14 Competitive inhibition against rat mitochondrial thymidine kinase 7097717

Literature References

PubMed DOI Target Context # Activities
7097717 10.1021/jm00348a007 Thymidine kinase 2 2
7097717 10.1021/jm00348a007 Thymidine kinase, cytosolic 2
7097717 10.1021/jm00348a007 Unchecked 1
458818 10.1021/jm00192a005 Thymidine kinase, cytosolic 1
395303 10.1021/jm00198a017 Unchecked 1

Data from ChEMBL 36 via Core Engine