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Compound Detail

CHEMBL233153

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

Basic Information

ChEMBL ID CHEMBL233153
Phase Preclinical
Structure Type MOL
InChI Key JMPLGCVMPMVPMF-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

455.4
MW (Da)
3.74
ALogP
6
HBA
2
HBD
108.0
PSA (Ų)
0.61
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 C20H16F3NO6S
MW 455.41
Aromatic Rings 3
Heavy Atoms 31
NP-Likeness -0.31

Activity Summary

IC50 2 meas. best 7.2

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cyclin-dependent kinase 1
CHEMBL308
IC50 7.2 7.2 63.0 1
Cyclin-dependent kinase 2
CHEMBL301
IC50 5.77 5.77 1700.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cyclin-dependent kinase 1 IC50 = 63.0 nM 7.2 Inhibition of CDK1 17178224
Cyclin-dependent kinase 2 IC50 = 1700.0 nM 5.77 Inhibition of CDK2 17178224

Literature References

PubMed DOI Target Context # Activities
17178224 10.1016/j.bmcl.2006.12.011 EJ 1
17178224 10.1016/j.bmcl.2006.12.011 Cyclin-dependent kinase 2 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