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Compound Detail

CHEMBL247468

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c1ccc(-c2c(-c3ccc(OCCN4CCCC4)cc3)oc3ncnc(NCCN4CCNCC4)c23)cc1

Basic Information

ChEMBL ID CHEMBL247468
Phase Preclinical
Structure Type MOL
InChI Key DMZTWOCJNVKCBW-UHFFFAOYSA-N
9
Targets
10
Activities
1
Assay Types
0
PK Parameters
11
Publications
0
Known Names

Molecular Properties

512.7
MW (Da)
4.35
ALogP
8
HBA
2
HBD
78.7
PSA (Ų)
0.32
QED
1
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C30H36N6O2
MW 512.66
Aromatic Rings 4
Heavy Atoms 38
NP-Likeness -0.94

Activity Summary

IC50 10 meas. best 8.05

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tyrosine-protein kinase Lck
CHEMBL258
IC50 8.05 8.05 9.0 1
Proto-oncogene tyrosine-protein kinase Src
CHEMBL267
IC50 7.35 7.35 45.0 1
Activated CDC42 kinase 1
CHEMBL4599
IC50 7.01 7.01 98.0 1
T-cell
CHEMBL614309
IC50 6.64 6.505 227.0 2
Epidermal growth factor receptor
CHEMBL203
IC50 6.4 6.4 397.0 1
Tyrosine-protein kinase JAK3
CHEMBL2148
IC50 6.02 6.02 960.0 1
Tyrosine-protein kinase ZAP-70
CHEMBL2803
IC50 6.0 6.0 992.0 1
Vascular endothelial growth factor receptor 2
CHEMBL279
IC50 5.51 5.51 3096.0 1
Unchecked
CHEMBL612545
IC50 5.5 5.5 3146.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
17280833 10.1016/j.bmcl.2007.01.057 T-cell 2
17280833 10.1016/j.bmcl.2007.01.057 Activated CDC42 kinase 1 1
17280833 10.1016/j.bmcl.2007.01.057 Tyrosine-protein kinase Lck 1
17280833 10.1016/j.bmcl.2007.01.057 Proto-oncogene tyrosine-protein kinase Src 1
17280833 10.1016/j.bmcl.2007.01.057 Epidermal growth factor receptor 1
17280833 10.1016/j.bmcl.2007.01.057 Tyrosine-protein kinase JAK3 1
17280833 10.1016/j.bmcl.2007.01.057 Tyrosine-protein kinase ZAP-70 1
17280833 10.1016/j.bmcl.2007.01.057 Vascular endothelial growth factor receptor 2 1
17280833 10.1016/j.bmcl.2007.01.057 Unchecked 1
17280833 10.1016/j.bmcl.2007.01.057 Tyrosine-protein kinase JAK2 1
17280833 10.1016/j.bmcl.2007.01.057 Angiopoietin-1 receptor 1

Data from ChEMBL 36 via Core Engine