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Compound Detail

CHEMBL497167

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CC(=O)Nc1ccccc1-c1cc(Cl)cc(-n2nc(C)c3cnc(N[C@@H](C)c4ccccc4)cc32)c1

Basic Information

ChEMBL ID CHEMBL497167
Phase Preclinical
Structure Type MOL
InChI Key QUYZXRAAIRZUEE-SFHVURJKSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

496.0
MW (Da)
7.18
ALogP
5
HBA
2
HBD
71.8
PSA (Ų)
0.26
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H26ClN5O
MW 496.01
Aromatic Rings 5
Heavy Atoms 36
NP-Likeness -1.50

Activity Summary

IC50 1 meas. best 6.68

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Serine/threonine-protein kinase PLK1
CHEMBL3024
IC50 6.68 6.68 207.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Serine/threonine-protein kinase PLK1 IC50 = 207.0 nM 6.68 Inhibition of Plk1 18793847

Literature References

PubMed DOI Target Context # Activities
18793847 10.1016/j.bmcl.2008.08.095 Serine/threonine-protein kinase PLK1 1
18793847 10.1016/j.bmcl.2008.08.095 HCT-116 1

Data from ChEMBL 36 via Core Engine