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Compound Detail

CHEMBL472946

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c1ccc2sc(-c3ccc(Nc4ncnc5ccsc45)cc3)nc2c1

Basic Information

ChEMBL ID CHEMBL472946
Phase Preclinical
Structure Type MOL
InChI Key ZCGDFAQAYLXLJV-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
10
Publications
0
Known Names

Molecular Properties

360.5
MW (Da)
5.71
ALogP
6
HBA
1
HBD
50.7
PSA (Ų)
0.45
QED
1
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C19H12N4S2
MW 360.47
Aromatic Rings 5
Heavy Atoms 25
NP-Likeness -2.25

Activity Summary

IC50 2 meas. best 6.14

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Aurora kinase B
CHEMBL2185
IC50 6.14 6.14 720.0 1
Aurora kinase A
CHEMBL4722
IC50 5.55 5.55 2800.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Aurora kinase B IC50 = 720.0 nM 6.14 Inhibition of Aurora B by virtual HTS assay 19211246
Aurora kinase A IC50 = 2800.0 nM 5.55 Inhibition of Aurora A by virtual HTS assay 19211246

Literature References

PubMed DOI Target Context # Activities
19211246 10.1016/j.bmcl.2009.01.054 Epidermal growth factor receptor 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 Angiopoietin-1 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 Vascular endothelial growth factor receptor 2 1
19211246 10.1016/j.bmcl.2009.01.054 Insulin-like growth factor 1 receptor 1
19211246 10.1016/j.bmcl.2009.01.054 Aurora kinase A 1
19211246 10.1016/j.bmcl.2009.01.054 Aurora kinase B 1

Data from ChEMBL 36 via Core Engine