Skip to main content
Free research Free research Free compound review with research home and workspace preview
Quick search ChEMBL 36
Compound Detail

CHEMBL210765

Enter ChEMBL ID:
Free Research Context This compound will appear in recent viewed items on the research home for this browser.
Research home View demo workspace
CN1CCN(CCC(=O)NS(=O)(=O)c2ccc(Nc3nc(N)n(C(=O)c4c(F)cccc4F)n3)cc2)CC1

Basic Information

ChEMBL ID CHEMBL210765
Phase Preclinical
Structure Type MOL
InChI Key YUCANQKNMKNWJA-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
3
PK Parameters
7
Publications
0
Known Names

Molecular Properties

548.6
MW (Da)
1.01
ALogP
11
HBA
3
HBD
155.6
PSA (Ų)
0.37
QED
2
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H26F2N8O4S
MW 548.58
Aromatic Rings 3
Heavy Atoms 38
NP-Likeness -1.63

Activity Summary

IC50 2 meas. best 6.58

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cyclin-dependent kinase 2
CHEMBL301
IC50 6.58 6.58 266.0 1
Cyclin-dependent kinase 1
CHEMBL308
IC50 5.87 5.87 1340.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 12727.06 ng.hr.mL-1 Rattus norvegicus
T1/2 0.16 hr Rattus norvegicus
Tmax 0.08 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cyclin-dependent kinase 2 IC50 = 266.0 nM 6.58 Inhibition of CDK2 16682186
Cyclin-dependent kinase 1 IC50 = 1340.0 nM 5.87 Inhibition of CDK1 16682186

Literature References

PubMed DOI Target Context # Activities
16682186 10.1016/j.bmcl.2006.04.071 Rattus norvegicus 4
16682186 10.1016/j.bmcl.2006.04.071 No relevant target 2
16682186 10.1016/j.bmcl.2006.04.071 A-375 1
16682186 10.1016/j.bmcl.2006.04.071 HCT-116 1
16682186 10.1016/j.bmcl.2006.04.071 HeLa 1
16682186 10.1016/j.bmcl.2006.04.071 Cyclin-dependent kinase 2 1
16682186 10.1016/j.bmcl.2006.04.071 Cyclin-dependent kinase 1 1

Data from ChEMBL 36 via Core Engine