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Compound Detail

CHEMBL483590

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COCCN(C)S(=O)(=O)c1ccc(Nc2nccc(-c3cnc(C)n3C3CC3)n2)cc1

Basic Information

ChEMBL ID CHEMBL483590
Phase Preclinical
Structure Type MOL
InChI Key CHCQXFQJHTYEHC-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

442.6
MW (Da)
2.99
ALogP
8
HBA
1
HBD
102.2
PSA (Ų)
0.54
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 C21H26N6O3S
MW 442.55
Aromatic Rings 3
Heavy Atoms 31
NP-Likeness -1.80

Activity Summary

IC50 2 meas. best 7.08

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cyclin-dependent kinase 2
CHEMBL301
IC50 7.08 7.08 83.0 1
LoVo
CHEMBL614721
IC50 5.22 5.22 6000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cyclin-dependent kinase 2 IC50 = 83.0 nM 7.08 Inhibition of CDK2 18815031
LoVo IC50 = 6000.0 nM 5.22 Antiproliferative activity against human LoVo cells assessed as BrdU incorporati... 18815031

Literature References

PubMed DOI Target Context # Activities
18815031 10.1016/j.bmcl.2008.09.024 Cyclin-dependent kinase 2 1
18815031 10.1016/j.bmcl.2008.09.024 Cyclin-dependent kinase 4 1
18815031 10.1016/j.bmcl.2008.09.024 LoVo 1

Data from ChEMBL 36 via Core Engine