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Compound Detail

CHEMBL403605

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Cc1cccc(CC(=O)Nc2n[nH]c3ccc(N4CCCS4(=O)=O)cc23)c1

Basic Information

ChEMBL ID CHEMBL403605
Phase Preclinical
Structure Type MOL
InChI Key DLFSESWOWKXVMD-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

384.5
MW (Da)
2.59
ALogP
4
HBA
2
HBD
95.2
PSA (Ų)
0.72
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 C19H20N4O3S
MW 384.46
Aromatic Rings 3
Heavy Atoms 27
NP-Likeness -2.16

Activity Summary

IC50 3 meas. best 8.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cyclin-dependent kinase 2
CHEMBL301
IC50 8.0 8.0 10.0 1
Cyclin-dependent kinase 1
CHEMBL308
IC50 7.3 7.3 50.0 1
Cyclin-dependent kinase 4
CHEMBL331
IC50 5.4 5.4 4000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cyclin-dependent kinase 2 IC50 = 10.0 nM 8.0 Inhibition of CDK2 18353638
Cyclin-dependent kinase 1 IC50 = 50.0 nM 7.3 Inhibition of CDK1 18353638
Cyclin-dependent kinase 4 IC50 = 4000.0 nM 5.4 Inhibition of CDK4 18353638

Literature References

PubMed DOI Target Context # Activities
18353638 10.1016/j.bmcl.2008.03.002 Cyclin-dependent kinase 2 1
18353638 10.1016/j.bmcl.2008.03.002 Cyclin-dependent kinase 4 1
18353638 10.1016/j.bmcl.2008.03.002 Cyclin-dependent kinase 1 1
18353638 10.1016/j.bmcl.2008.03.002 Unchecked 1

Data from ChEMBL 36 via Core Engine