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Compound Detail

CHEMBL458420

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O=C(Nc1ccccc1)Nc1c[nH]nc1-c1nc2cc(CN3CCOCC3)ccc2[nH]1

Basic Information

ChEMBL ID CHEMBL458420
Phase Preclinical
Structure Type MOL
InChI Key SOTHNRIRXPUQEZ-UHFFFAOYSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

417.5
MW (Da)
3.43
ALogP
5
HBA
4
HBD
111.0
PSA (Ų)
0.40
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H23N7O2
MW 417.47
Aromatic Rings 4
Heavy Atoms 31
NP-Likeness -2.01

Activity Summary

IC50 4 meas. best 7.92

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Aurora kinase A
CHEMBL4722
IC50 7.92 7.92 12.0 1
Aurora kinase B
CHEMBL2185
IC50 7.27 7.27 54.0 1
Cyclin-dependent kinase 2
CHEMBL301
IC50 5.75 5.75 1800.0 1
Cyclin-dependent kinase 1/cyclin B1
CHEMBL1907602
IC50 5.26 5.26 5500.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Aurora kinase A IC50 = 12.0 nM 7.92 Inhibition of Aurora A 19143567
Aurora kinase B IC50 = 54.0 nM 7.27 Inhibition of Aurora B 19143567
Cyclin-dependent kinase 2 IC50 = 1800.0 nM 5.75 Inhibition of CDK2/Cyclin A 19143567
Cyclin-dependent kinase 1/cyclin B1 IC50 = 5500.0 nM 5.26 Inhibition of CDK1/Cyclin B 19143567

Literature References

PubMed DOI Target Context # Activities
19143567 10.1021/jm800984v Plasma 1
19143567 10.1021/jm800984v Aurora kinase A 1
19143567 10.1021/jm800984v Aurora kinase B 1
19143567 10.1021/jm800984v Cyclin-dependent kinase 1/cyclin B1 1
19143567 10.1021/jm800984v Cyclin-dependent kinase 2 1
19143567 10.1021/jm800984v HCT-116 1

Data from ChEMBL 36 via Core Engine