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Compound Detail

CHEMBL207426

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COCCNc1nc(-c2ccc(C(=O)NCCC#N)cc2)nc2c1ncn2C(C)C

Basic Information

ChEMBL ID CHEMBL207426
Phase Preclinical
Structure Type MOL
InChI Key IXMZVTJMZXKFCC-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

407.5
MW (Da)
2.78
ALogP
8
HBA
2
HBD
117.8
PSA (Ų)
0.52
QED
0
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H25N7O2
MW 407.48
Aromatic Rings 3
Heavy Atoms 30
NP-Likeness -1.56

Activity Summary

IC50 2 meas. best 5.47

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cyclin-dependent kinase 5/CDK5 activator 1
CHEMBL1907600
IC50 5.47 5.47 3400.0 1
Cyclin-dependent kinase 1/cyclin B
CHEMBL2094127
IC50 5.38 5.38 4200.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cyclin-dependent kinase 5/CDK5 activator 1 IC50 = 3400.0 nM 5.47 Inhibition of Cdk5/p25 16616489
Cyclin-dependent kinase 1/cyclin B IC50 = 4200.0 nM 5.38 Inhibition of Cdk1/cyclin B 16616489

Literature References

PubMed DOI Target Context # Activities
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
16616489 10.1016/j.bmcl.2006.03.060 Glycogen synthase kinase-3 beta 1

Data from ChEMBL 36 via Core Engine