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Compound Detail

CHEMBL1076721

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COc1ccc(C2=NNC(=O)/C2=N\Nc2cccnc2)cc1

Basic Information

ChEMBL ID CHEMBL1076721
Phase Preclinical
Structure Type MOL
InChI Key IJGDAJQBJGDGGV-UHFFFAOYSA-N
6
Targets
6
Activities
1
Assay Types
0
PK Parameters
14
Publications
0
Known Names

Molecular Properties

295.3
MW (Da)
1.39
ALogP
6
HBA
2
HBD
88.0
PSA (Ų)
0.83
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C15H13N5O2
MW 295.30
Aromatic Rings 2
Heavy Atoms 22
NP-Likeness -1.22

Activity Summary

Ki 6 meas. best 8.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Glycogen synthase kinase-3 beta
CHEMBL262
Ki 8.7 8.7 2.0 1
Cyclin-dependent kinase 2
CHEMBL301
Ki 7.21 7.21 62.0 1
Receptor-type tyrosine-protein kinase FLT3
CHEMBL1974
Ki 6.89 6.89 130.0 1
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform
CHEMBL3267
Ki 6.0 6.0 1000.0 1
Interleukin-1 receptor-associated kinase 4
CHEMBL3778
Ki 5.82 5.82 1500.0 1
Vascular endothelial growth factor receptor 2
CHEMBL279
Ki 5.47 5.47 3400.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
20138514 10.1016/j.bmcl.2010.01.072 Unchecked 14
20138514 10.1016/j.bmcl.2010.01.072 Glycogen synthase kinase-3 beta 1
20138514 10.1016/j.bmcl.2010.01.072 Cyclin-dependent kinase 2 1
20138514 10.1016/j.bmcl.2010.01.072 Receptor-type tyrosine-protein kinase FLT3 1
20138514 10.1016/j.bmcl.2010.01.072 Interleukin-1 receptor-associated kinase 4 1
20138514 10.1016/j.bmcl.2010.01.072 Tyrosine-protein kinase JAK2 1
20138514 10.1016/j.bmcl.2010.01.072 Mitogen-activated protein kinase 10 1
20138514 10.1016/j.bmcl.2010.01.072 Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform 1
20138514 10.1016/j.bmcl.2010.01.072 Vascular endothelial growth factor receptor 2 1
20138514 10.1016/j.bmcl.2010.01.072 Hepatocyte growth factor receptor 1
20138514 10.1016/j.bmcl.2010.01.072 Serine/threonine-protein kinase PLK1 1
20138514 10.1016/j.bmcl.2010.01.072 Rho-associated protein kinase 1 1
20138514 10.1016/j.bmcl.2010.01.072 Proto-oncogene tyrosine-protein kinase Src 1
20138514 10.1016/j.bmcl.2010.01.072 Tyrosine-protein kinase SYK 1

Data from ChEMBL 36 via Core Engine