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Compound Detail

CHEMBL1241849

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CN(C)CCNS(=O)(=O)c1ccc(Nc2cccc(-c3cnc4ccccn34)c2)cc1

Basic Information

ChEMBL ID CHEMBL1241849
Phase Preclinical
Structure Type MOL
InChI Key UTGUSPCINACJKQ-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

435.6
MW (Da)
3.58
ALogP
6
HBA
2
HBD
78.7
PSA (Ų)
0.44
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 C23H25N5O2S
MW 435.55
Aromatic Rings 4
Heavy Atoms 31
NP-Likeness -2.01

Activity Summary

IC50 3 meas. best 8.3

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cyclin-dependent kinase 2
CHEMBL301
IC50 8.3 8.3 5.0 1
Cyclin-dependent kinase 1
CHEMBL308
IC50 7.82 7.82 15.0 1
Cyclin-dependent kinase 4
CHEMBL331
IC50 6.58 6.58 260.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cyclin-dependent kinase 2 IC50 = 5.0 nM 8.3 Inhibition of CDK2 16584130
Cyclin-dependent kinase 1 IC50 = 15.0 nM 7.82 Inhibition of CDK1 16584130
Cyclin-dependent kinase 4 IC50 = 260.0 nM 6.58 Inhibition of CDK4 16584130

Literature References

PubMed DOI Target Context # Activities
16584130 10.1208/aapsj080125 Cyclin-dependent kinase 4 1
16584130 10.1208/aapsj080125 Cyclin-dependent kinase 2 1
16584130 10.1208/aapsj080125 Cyclin-dependent kinase 1 1

Data from ChEMBL 36 via Core Engine