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Compound Detail

CHEMBL488645

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COc1cc(C2=C(c3cn(COC(C)C)c4ccccc34)CNC2=O)cc(OC)c1OC

Basic Information

ChEMBL ID CHEMBL488645
Phase Preclinical
Structure Type MOL
InChI Key CPWSAJBBZKPYRF-UHFFFAOYSA-N
7
Targets
7
Activities
1
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

436.5
MW (Da)
4.09
ALogP
6
HBA
1
HBD
71.0
PSA (Ų)
0.58
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H28N2O5
MW 436.51
Aromatic Rings 3
Heavy Atoms 32
NP-Likeness -0.06

Activity Summary

IC50 7 meas. best 5.28

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Vascular endothelial growth factor receptor 3
CHEMBL1955
IC50 5.28 5.28 5300.0 1
Vascular endothelial growth factor receptor 2
CHEMBL279
IC50 5.28 5.28 5200.0 1
Angiopoietin-1 receptor
CHEMBL4128
IC50 4.96 4.96 11000.0 1
Focal adhesion kinase 1
CHEMBL2695
IC50 4.57 4.57 27000.0 1
Proto-oncogene tyrosine-protein kinase Src
CHEMBL267
IC50 4.54 4.54 29000.0 1
Aurora kinase A
CHEMBL4722
IC50 4.48 4.48 33000.0 1
Serine/threonine-protein kinase PLK4
CHEMBL3788
IC50 4.36 4.36 44000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
18529047 10.1021/jm8001185 Aurora kinase A 1
18529047 10.1021/jm8001185 Focal adhesion kinase 1 1
18529047 10.1021/jm8001185 Proto-oncogene tyrosine-protein kinase Src 1
18529047 10.1021/jm8001185 Vascular endothelial growth factor receptor 2 1
18529047 10.1021/jm8001185 Vascular endothelial growth factor receptor 3 1
18529047 10.1021/jm8001185 Serine/threonine-protein kinase PLK4 1
18529047 10.1021/jm8001185 Angiopoietin-1 receptor 1

Data from ChEMBL 36 via Core Engine