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Compound Detail

CHEMBL4542797

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Cc1n[nH]cc1-c1cc2nc([C@]3(C)CCCN3)[nH]c(=O)c2s1.Cl.Cl

Basic Information

ChEMBL ID CHEMBL4542797
Phase Preclinical
Structure Type MOL
InChI Key VSIAVHXUYVVNIW-CKUXDGONSA-N
Parent Compound CHEMBL4595787
Active Moiety CHEMBL4595787
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

315.4
MW (Da)
2.28
ALogP
5
HBA
3
HBD
86.5
PSA (Ų)
0.68
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C15H19Cl2N5OS
MW 388.32
Aromatic Rings 3
Heavy Atoms 22
NP-Likeness -0.91

Activity Summary

IC50 3 meas. best 8.01

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
CDC7/DBF4 (Cell division cycle 7-related protein kinase/Activator of S phase kinase)
CHEMBL2111377
IC50 8.01 8.01 9.8 1
Rho-associated protein kinase 1
CHEMBL3231
IC50 6.57 6.57 270.0 1
Cyclin-dependent kinase 2/cyclin E1
CHEMBL1907605
IC50 5.0 5.0 9900.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
31895562 10.1021/acs.jmedchem.9b01427 Unchecked 2
31895562 10.1021/acs.jmedchem.9b01427 CDC7/DBF4 (Cell division cycle 7-related protein kinase/Activator of S phase kinase) 1
31895562 10.1021/acs.jmedchem.9b01427 Cyclin-dependent kinase 2/cyclin E1 1
31895562 10.1021/acs.jmedchem.9b01427 Rho-associated protein kinase 1 1

Data from ChEMBL 36 via Core Engine