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Compound Detail

CHEMBL248221

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COc1cc2ncc(C#N)c(N[C@@H]3C[C@H]3c3ccccc3)c2cc1OCCCN1CCOCC1

Basic Information

ChEMBL ID CHEMBL248221
Phase Preclinical
Structure Type MOL
InChI Key YAOFOVYWIFNOKW-XUZZJYLKSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

458.6
MW (Da)
4.18
ALogP
7
HBA
1
HBD
79.6
PSA (Ų)
0.48
QED
0
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H30N4O3
MW 458.56
Aromatic Rings 3
Heavy Atoms 34
NP-Likeness -1.17

Activity Summary

Ki 4 meas. best 7.28

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Epidermal growth factor receptor
CHEMBL203
Ki 7.28 7.28 52.0 1
Vascular endothelial growth factor receptor 2
CHEMBL279
Ki 6.25 6.25 560.0 1
Vascular endothelial growth factor receptor 1
CHEMBL1868
Ki 6.04 6.04 910.0 1
Tyrosine-protein kinase ABL1
CHEMBL1862
Ki 5.75 5.75 1800.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
17827009 10.1016/j.bmcl.2007.07.071 Epidermal growth factor receptor 2
17827009 10.1016/j.bmcl.2007.07.071 Tyrosine-protein kinase SYK 1
17827009 10.1016/j.bmcl.2007.07.071 Proto-oncogene tyrosine-protein kinase Src 1
17827009 10.1016/j.bmcl.2007.07.071 Tyrosine-protein kinase ABL1 1
17827009 10.1016/j.bmcl.2007.07.071 Vascular endothelial growth factor receptor 1 1
17827009 10.1016/j.bmcl.2007.07.071 Vascular endothelial growth factor receptor 2 1

Data from ChEMBL 36 via Core Engine