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Compound Detail

CHEMBL452602

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C[C@@H]1CNC[C@H](C(=O)Nc2ncc(SCc3ncc(C(C)(C)C)o3)s2)C1

Basic Information

ChEMBL ID CHEMBL452602
Phase Preclinical
Structure Type MOL
InChI Key SSMMYRQDZBSVCY-NWDGAFQWSA-N
6
Targets
6
Activities
1
Assay Types
0
PK Parameters
9
Publications
0
Known Names

Molecular Properties

394.6
MW (Da)
3.91
ALogP
7
HBA
2
HBD
80.0
PSA (Ų)
0.75
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C18H26N4O2S2
MW 394.57
Aromatic Rings 2
Heavy Atoms 26
NP-Likeness -1.29

Activity Summary

IC50 6 meas. best 8.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
CDK9/cyclin T1
CHEMBL2111389
IC50 8.4 8.4 4.0 1
Cyclin-dependent kinase 2
CHEMBL301
IC50 7.7 7.7 20.0 1
Cyclin-dependent kinase 7/ cyclin H
CHEMBL2111288
IC50 6.96 6.96 110.0 1
Cyclin-dependent kinase 1/cyclin B1
CHEMBL1907602
IC50 6.92 6.92 120.0 1
Cyclin-dependent kinase 9
CHEMBL3116
IC50 6.92 6.92 120.0 1
Unchecked
CHEMBL612545
IC50 6.6 6.6 250.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
18926699 10.1016/j.bmcl.2008.09.099 Liver microsomes 2
18926699 10.1016/j.bmcl.2008.09.099 MDCK 2
18926699 10.1016/j.bmcl.2008.09.099 ADMET 2
18926699 10.1016/j.bmcl.2008.09.099 Cyclin-dependent kinase 9 1
18926699 10.1016/j.bmcl.2008.09.099 Cyclin-dependent kinase 2 1
18926699 10.1016/j.bmcl.2008.09.099 Cyclin-dependent kinase 1/cyclin B1 1
18926699 10.1016/j.bmcl.2008.09.099 Unchecked 1
18926699 10.1016/j.bmcl.2008.09.099 Cyclin-dependent kinase 7/ cyclin H 1
18926699 10.1016/j.bmcl.2008.09.099 CDK9/cyclin T1 1

Data from ChEMBL 36 via Core Engine