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Compound Detail

CHEMBL475352

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COc1cc(Nc2ncnc3[nH]cnc23)ccc1-c1nc2ccccc2s1

Basic Information

ChEMBL ID CHEMBL475352
Phase Preclinical
Structure Type MOL
InChI Key DPBAOWACXDVJKP-UHFFFAOYSA-N
5
Targets
5
Activities
1
Assay Types
0
PK Parameters
10
Publications
0
Known Names

Molecular Properties

374.4
MW (Da)
4.38
ALogP
7
HBA
2
HBD
88.6
PSA (Ų)
0.49
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 C19H14N6OS
MW 374.43
Aromatic Rings 5
Heavy Atoms 27
NP-Likeness -1.51

Activity Summary

IC50 5 meas. best 5.89

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Angiopoietin-1 receptor
CHEMBL4128
IC50 5.89 5.89 1300.0 1
Epidermal growth factor receptor
CHEMBL203
IC50 5.58 5.58 2600.0 1
Vascular endothelial growth factor receptor 3
CHEMBL1955
IC50 5.47 5.47 3400.0 1
Aurora kinase A
CHEMBL4722
IC50 5.24 5.24 5800.0 1
Vascular endothelial growth factor receptor 2
CHEMBL279
IC50 5.04 5.04 9200.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
19211246 10.1016/j.bmcl.2009.01.054 Aurora kinase B 1
19211246 10.1016/j.bmcl.2009.01.054 Receptor tyrosine-protein kinase erbB-2 1
19211246 10.1016/j.bmcl.2009.01.054 Insulin receptor 1
19211246 10.1016/j.bmcl.2009.01.054 Proto-oncogene tyrosine-protein kinase Src 1
19211246 10.1016/j.bmcl.2009.01.054 Insulin-like growth factor 1 receptor 1
19211246 10.1016/j.bmcl.2009.01.054 Vascular endothelial growth factor receptor 2 1
19211246 10.1016/j.bmcl.2009.01.054 Aurora kinase A 1
19211246 10.1016/j.bmcl.2009.01.054 Vascular endothelial growth factor receptor 3 1
19211246 10.1016/j.bmcl.2009.01.054 Epidermal growth factor receptor 1
19211246 10.1016/j.bmcl.2009.01.054 Angiopoietin-1 receptor 1

Data from ChEMBL 36 via Core Engine