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Compound Detail

CHEMBL480442

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CC(C)c1cnn2c(NCc3ccc(Cl)cc3)nc(N[C@@H](CO)C(C)C)nc12

Basic Information

ChEMBL ID CHEMBL480442
Phase Preclinical
Structure Type MOL
InChI Key BOPIEFLHGAQWGB-KRWDZBQOSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

402.9
MW (Da)
3.94
ALogP
7
HBA
3
HBD
87.4
PSA (Ų)
0.53
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H27ClN6O
MW 402.93
Aromatic Rings 3
Heavy Atoms 28
NP-Likeness -1.11

Activity Summary

IC50 3 meas. best 7.22

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cyclin-dependent kinase 5/CDK5 activator 1
CHEMBL1907600
IC50 7.22 7.22 60.0 1
Cyclin-dependent kinase 2
CHEMBL301
IC50 7.22 7.22 60.0 1
Unchecked
CHEMBL612545
IC50 7.1 7.1 80.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
19128055 10.1021/jm801340z Unchecked 1
19128055 10.1021/jm801340z Cyclin-dependent kinase 2 1
19128055 10.1021/jm801340z Cyclin-dependent kinase 5/CDK5 activator 1 1
19128055 10.1021/jm801340z Cyclin-dependent kinase 7/ cyclin H 1
19128055 10.1021/jm801340z CDK9/cyclin T1 1
19128055 10.1021/jm801340z SH-SY5Y 1
19128055 10.1021/jm801340z HEK293 1

Data from ChEMBL 36 via Core Engine