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Compound Detail

CHEMBL591325

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CN(C)CCOc1ccc2c(c1)CCn1nc(-c3ccc(Oc4ccccc4)cc3)c(C(N)=O)c1N2

Basic Information

ChEMBL ID CHEMBL591325
Phase Preclinical
Structure Type MOL
InChI Key SYWUIAOLWMUYTP-UHFFFAOYSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
12
Publications
0
Known Names

Molecular Properties

483.6
MW (Da)
4.68
ALogP
7
HBA
2
HBD
94.6
PSA (Ų)
0.38
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 C28H29N5O3
MW 483.57
Aromatic Rings 4
Heavy Atoms 36
NP-Likeness -1.03

Activity Summary

IC50 4 meas. best 9.22

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Proto-oncogene tyrosine-protein kinase Src
CHEMBL267
IC50 9.22 9.22 0.6 1
Tyrosine-protein kinase Lck
CHEMBL258
IC50 9.14 9.14 0.7 1
Lymphocyte
CHEMBL612599
IC50 9.13 9.13 0.7 1
Tyrosine-protein kinase CSK
CHEMBL2634
IC50 8.77 8.77 1.7 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
19945867 10.1016/j.bmcl.2009.11.013 Tyrosine-protein kinase Lck 1
19945867 10.1016/j.bmcl.2009.11.013 Lymphocyte 1
19945867 10.1016/j.bmcl.2009.11.013 Proto-oncogene tyrosine-protein kinase Src 1
19945867 10.1016/j.bmcl.2009.11.013 Tyrosine-protein kinase CSK 1
19945867 10.1016/j.bmcl.2009.11.013 Tyrosine-protein kinase ZAP-70 1
19945867 10.1016/j.bmcl.2009.11.013 Dual specificity mitogen-activated protein kinase kinase 1 1
19945867 10.1016/j.bmcl.2009.11.013 Unchecked 1
19945867 10.1016/j.bmcl.2009.11.013 RAC-alpha serine/threonine-protein kinase 1
19945867 10.1016/j.bmcl.2009.11.013 Protein kinase C alpha type 1
19945867 10.1016/j.bmcl.2009.11.013 Cyclin-dependent kinase 1 1
19945867 10.1016/j.bmcl.2009.11.013 Calcium/calmodulin-dependent protein kinase type IV 1
19945867 10.1016/j.bmcl.2009.11.013 Mitogen-activated protein kinase 1 1

Data from ChEMBL 36 via Core Engine