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Compound Detail

CHEMBL140205

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CNCc1cc(NC(=O)Nc2cccc3c2C2CCCN2C3=O)[nH]n1

Basic Information

ChEMBL ID CHEMBL140205
Phase Preclinical
Structure Type MOL
InChI Key CSEMLDOWPBRBHH-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

340.4
MW (Da)
2.06
ALogP
4
HBA
4
HBD
102.2
PSA (Ų)
0.68
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 C17H20N6O2
MW 340.39
Aromatic Rings 2
Heavy Atoms 25
NP-Likeness -1.09

Activity Summary

IC50 2 meas. best 6.54

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
IC50 6.54 6.54 290.0 1
Cyclin-dependent kinase 2/cyclin A
CHEMBL2094128
IC50 4.85 4.85 14000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked IC50 = 290.0 nM 6.54 Inhibition of human recombinant cyclin D2-CDK4 11741480
Cyclin-dependent kinase 2/cyclin A IC50 = 14000.0 nM 4.85 Inhibition of human recombinant cyclin A-CDK2 11741480

Literature References

PubMed DOI Target Context # Activities
11741480 10.1021/jm010326y Unchecked 1
11741480 10.1021/jm010326y Cyclin-dependent kinase 2/cyclin A 1
11741480 10.1021/jm010326y Cyclin-dependent kinase 2 and 4 (CDK2 and CDK4) 1

Data from ChEMBL 36 via Core Engine