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Compound Detail

CHEMBL179603

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COc1ccc(NC(=O)Nc2ccc(Oc3ncnc4cc(OC)c(OC)cc34)cc2)cc1

Basic Information

ChEMBL ID CHEMBL179603
Phase Preclinical
Structure Type MOL
InChI Key UQLOTEZFDHTNMJ-UHFFFAOYSA-N
2
Targets
5
Activities
1
Assay Types
0
PK Parameters
16
Publications
0
Known Names

Molecular Properties

446.5
MW (Da)
5.09
ALogP
7
HBA
2
HBD
103.8
PSA (Ų)
0.41
QED
1
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H22N4O5
MW 446.46
Aromatic Rings 4
Heavy Atoms 33
NP-Likeness -0.91

Activity Summary

IC50 5 meas. best 8.66

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Vascular endothelial growth factor receptor 2
CHEMBL279
IC50 8.66 7.535 2.2 4
Platelet-derived growth factor receptor alpha
CHEMBL2007
IC50 8.44 8.44 3.6 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
21353546 10.1016/j.bmcl.2011.01.137 Vascular endothelial growth factor receptor 2 2
15743179 10.1021/jm030427r Vascular endothelial growth factor receptor 2 1
15743179 10.1021/jm030427r Platelet-derived growth factor receptor alpha 1
21033670 10.1021/jm1009605 Calf thymus DNA 1
21033670 10.1021/jm1009605 Nucleic Acid 1
21353546 10.1016/j.bmcl.2011.01.137 Epidermal growth factor receptor 1
21353546 10.1016/j.bmcl.2011.01.137 PC-3 1
21353546 10.1016/j.bmcl.2011.01.137 HT-29 1
21353546 10.1016/j.bmcl.2011.01.137 MCF7 1
21353546 10.1016/j.bmcl.2011.01.137 NON-PROTEIN TARGET 1
22229669 10.1021/jm2013453 Epidermal growth factor receptor 1
22229669 10.1021/jm2013453 Vascular endothelial growth factor receptor 2 1
22229669 10.1021/jm2013453 No relevant target 1
22229669 10.1021/jm2013453 PC-3 1
22229669 10.1021/jm2013453 HT-29 1
22229669 10.1021/jm2013453 MCF7 1

Data from ChEMBL 36 via Core Engine