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Compound Detail

CHEMBL475351

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COc1nc(Nc2ccc(-c3nc4ccccc4s3)c(OC)c2)c2cc[nH]c2n1

Basic Information

ChEMBL ID CHEMBL475351
Phase Preclinical
Structure Type MOL
InChI Key AOUMXCXOJGAKLX-UHFFFAOYSA-N
6
Targets
6
Activities
1
Assay Types
0
PK Parameters
10
Publications
0
Known Names

Molecular Properties

403.5
MW (Da)
5.00
ALogP
7
HBA
2
HBD
85.0
PSA (Ų)
0.43
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H17N5O2S
MW 403.47
Aromatic Rings 5
Heavy Atoms 29
NP-Likeness -1.39

Activity Summary

IC50 6 meas. best 6.02

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Vascular endothelial growth factor receptor 2
CHEMBL279
IC50 6.02 6.02 960.0 1
Proto-oncogene tyrosine-protein kinase Src
CHEMBL267
IC50 5.68 5.68 2100.0 1
Angiopoietin-1 receptor
CHEMBL4128
IC50 5.6 5.6 2500.0 1
Insulin-like growth factor 1 receptor
CHEMBL1957
IC50 5.54 5.54 2900.0 1
Epidermal growth factor receptor
CHEMBL203
IC50 5.29 5.29 5100.0 1
Vascular endothelial growth factor receptor 3
CHEMBL1955
IC50 5.11 5.11 7700.0 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 Aurora kinase A 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 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 Insulin-like growth factor 1 receptor 1
19211246 10.1016/j.bmcl.2009.01.054 Angiopoietin-1 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 Vascular endothelial growth factor receptor 2 1

Data from ChEMBL 36 via Core Engine