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Compound Detail

CHEMBL247866

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CC(C)Nc1ncnc2oc(-c3ccc(OCCN4CCCC4)cc3)c(-c3ccccc3)c12

Basic Information

ChEMBL ID CHEMBL247866
Phase Preclinical
Structure Type MOL
InChI Key SSVDSZIWJBBCNN-UHFFFAOYSA-N
10
Targets
11
Activities
1
Assay Types
0
PK Parameters
11
Publications
0
Known Names

Molecular Properties

442.6
MW (Da)
5.85
ALogP
6
HBA
1
HBD
63.4
PSA (Ų)
0.37
QED
1
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H30N4O2
MW 442.56
Aromatic Rings 4
Heavy Atoms 33
NP-Likeness -0.90

Activity Summary

IC50 11 meas. best 7.44

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tyrosine-protein kinase Lck
CHEMBL258
IC50 7.44 7.44 36.0 1
Activated CDC42 kinase 1
CHEMBL4599
IC50 7.11 7.11 78.0 1
T-cell
CHEMBL614309
IC50 6.7 6.485 199.0 2
Vascular endothelial growth factor receptor 2
CHEMBL279
IC50 6.27 6.27 537.0 1
Proto-oncogene tyrosine-protein kinase Src
CHEMBL267
IC50 6.04 6.04 914.0 1
Epidermal growth factor receptor
CHEMBL203
IC50 5.99 5.99 1029.0 1
Tyrosine-protein kinase JAK3
CHEMBL2148
IC50 5.85 5.85 1426.0 1
Unchecked
CHEMBL612545
IC50 5.83 5.83 1493.0 1
Tyrosine-protein kinase ZAP-70
CHEMBL2803
IC50 5.49 5.49 3272.0 1
Tyrosine-protein kinase JAK2
CHEMBL2971
IC50 5.31 5.31 4891.0 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