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Compound Detail

CHEMBL422759

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CCC(C)(O)C#Cc1nc(NCc2ccc(OC)cc2)c2ncn(C(C)C)c2n1

Basic Information

ChEMBL ID CHEMBL422759
Phase Preclinical
Structure Type MOL
InChI Key ATFBEKGTULYWDD-UHFFFAOYSA-N
3
Targets
4
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

393.5
MW (Da)
3.54
ALogP
7
HBA
2
HBD
85.1
PSA (Ų)
0.62
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H27N5O2
MW 393.49
Aromatic Rings 3
Heavy Atoms 29
NP-Likeness -0.50

Activity Summary

IC50 4 meas. best 6.64

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cyclin-dependent kinase 1/cyclin B
CHEMBL2094127
IC50 6.64 6.64 230.0 2
Cyclin-dependent kinase 1
CHEMBL308
IC50 6.64 6.64 230.0 1
Cyclin-dependent kinase 5
CHEMBL4036
IC50 6.4 6.4 400.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
11063606 10.1021/jm000965t Cyclin-dependent kinase 1 1
11063606 10.1021/jm000965t Cyclin-dependent kinase 5 1
10753466 10.1021/jm9911130 Cyclin-dependent kinase 1/cyclin B 1
16616489 10.1016/j.bmcl.2006.03.060 Glycogen synthase kinase-3 beta 1
16616489 10.1016/j.bmcl.2006.03.060 Cyclin-dependent kinase 1/cyclin B 1
16616489 10.1016/j.bmcl.2006.03.060 Cyclin-dependent kinase 5/CDK5 activator 1 1

Data from ChEMBL 36 via Core Engine