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Compound Detail

CHEMBL563150

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Cn1nc(C(=O)Nc2ccccc2)c2c1-c1nc(Nc3ccccc3)ncc1CC2

Basic Information

ChEMBL ID CHEMBL563150
Phase Preclinical
Structure Type MOL
InChI Key VRZQAXBLQMWLAF-UHFFFAOYSA-N
2
Targets
3
Activities
1
Assay Types
0
PK Parameters
12
Publications
0
Known Names

Molecular Properties

396.4
MW (Da)
3.97
ALogP
6
HBA
2
HBD
84.7
PSA (Ų)
0.55
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H20N6O
MW 396.45
Aromatic Rings 4
Heavy Atoms 30
NP-Likeness -1.24

Activity Summary

IC50 3 meas. best 6.24

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cyclin-dependent kinase 2/cyclin A
CHEMBL2094128
IC50 6.24 6.24 574.0 2
Cyclin-dependent kinase 2
CHEMBL301
IC50 6.24 6.24 574.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
19603809 10.1021/jm9006559 Cyclin-dependent kinase 2 1
19603809 10.1021/jm9006559 Aurora kinase A 1
19603809 10.1021/jm9006559 A2780 1
19603809 10.1021/jm9006559 No relevant target 1
20397705 10.1021/jm901713n Cyclin-dependent kinase 2/cyclin A 1
20397705 10.1021/jm901713n Serine/threonine-protein kinase PLK1 1
20397705 10.1021/jm901713n Aurora kinase A 1
20397705 10.1021/jm901713n A2780 1
21723120 10.1016/j.bmcl.2011.05.122 Dual specificity protein kinase TTK 1
21723120 10.1016/j.bmcl.2011.05.122 Aurora kinase A 1
21723120 10.1016/j.bmcl.2011.05.122 Serine/threonine-protein kinase PLK1 1
21723120 10.1016/j.bmcl.2011.05.122 Cyclin-dependent kinase 2/cyclin A 1

Data from ChEMBL 36 via Core Engine