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Compound Detail

CHEMBL4462898

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Cc1n[nH]cc1-c1cc2nc(C34CCC(CC3)N4)[nH]c(=O)c2s1.Cl

Basic Information

ChEMBL ID CHEMBL4462898
Phase Preclinical
Structure Type MOL
InChI Key KSZVZDFZEKDMHA-UHFFFAOYSA-N
Parent Compound CHEMBL4595540
Active Moiety CHEMBL4595540
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

327.4
MW (Da)
2.42
ALogP
5
HBA
3
HBD
86.5
PSA (Ų)
0.67
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 C16H18ClN5OS
MW 363.87
Aromatic Rings 3
Heavy Atoms 23
NP-Likeness -0.90

Activity Summary

IC50 3 meas. best 9.8

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 9.8 9.8 0.2 1
Rho-associated protein kinase 1
CHEMBL3231
IC50 7.02 7.02 96.0 1
Cyclin-dependent kinase 2/cyclin E1
CHEMBL1907605
IC50 5.82 5.82 1500.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
31895562 10.1021/acs.jmedchem.9b01427 No relevant target 4
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