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Compound Detail

CHEMBL287727

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Oc1[nH]c(Nc2ccccc2)nc2ncnc1-2

Basic Information

ChEMBL ID CHEMBL287727
Phase Preclinical
Structure Type MOL
InChI Key JDCULXHGRMPCAM-UHFFFAOYSA-N
3
Targets
7
Activities
2
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

227.2
MW (Da)
1.75
ALogP
5
HBA
3
HBD
86.7
PSA (Ų)
0.62
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 C11H9N5O
MW 227.23
Aromatic Rings 1
Heavy Atoms 17
NP-Likeness -0.92

Activity Summary

IC50 6 meas. best 5.8
EC50 1 meas. best 5.1

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Thymidine kinase
CHEMBL1820
IC50 5.8 5.45 1600.0 2
Thymidine kinase
CHEMBL3415
IC50 5.8 5.8 1584.9 2
Thymidine kinase
CHEMBL1795127
IC50 5.1 5.1 8000.0 2
Thymidine kinase
CHEMBL1820
EC50 5.1 5.1 8000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
1323680 10.1021/jm00094a007 Thymidine kinase 2
7837239 10.1021/jm00001a010 Thymidine kinase 2
2153203 10.1021/jm00163a033 Thymidine kinase 2
7752206 10.1021/jm00010a027 DNA helicase/primase complex protein 1
2840499 10.1021/jm00403a004 Thymidine kinase 1
28005359 10.1021/acs.jmedchem.6b01254 CDK2/Bovine cyclin A 1

Data from ChEMBL 36 via Core Engine