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Compound Detail

CHEMBL233152

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Cc1cc(N2CCCS2(=O)=O)c2oc(-c3ccc(O)c(C#N)c3)c(O)c(=O)c2c1

Basic Information

ChEMBL ID CHEMBL233152
Phase Preclinical
Structure Type MOL
InChI Key WWZIGIHYULFNFK-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

412.4
MW (Da)
2.59
ALogP
7
HBA
2
HBD
131.8
PSA (Ų)
0.66
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H16N2O6S
MW 412.42
Aromatic Rings 3
Heavy Atoms 29
NP-Likeness -0.41

Activity Summary

IC50 2 meas. best 6.8

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cyclin-dependent kinase 1
CHEMBL308
IC50 6.8 6.8 160.0 1
Cyclin-dependent kinase 2
CHEMBL301
IC50 5.85 5.85 1400.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cyclin-dependent kinase 1 IC50 = 160.0 nM 6.8 Inhibition of CDK1 17178224
Cyclin-dependent kinase 2 IC50 = 1400.0 nM 5.85 Inhibition of CDK2 17178224

Literature References

PubMed DOI Target Context # Activities
17178224 10.1016/j.bmcl.2006.12.011 Cyclin-dependent kinase 2 1
17178224 10.1016/j.bmcl.2006.12.011 EJ 1
17178224 10.1016/j.bmcl.2006.12.011 Cyclin-dependent kinase 1 1
17178224 10.1016/j.bmcl.2006.12.011 HCT-116 1
17178224 10.1016/j.bmcl.2006.12.011 SW-620 1
17178224 10.1016/j.bmcl.2006.12.011 MDA-MB-468 1

Data from ChEMBL 36 via Core Engine