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Compound Detail

CHEMBL473557

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Fc1cc(-c2nc3ccccc3s2)ccc1Nc1ncnc2cc(Cl)ccc12

Basic Information

ChEMBL ID CHEMBL473557
Phase Preclinical
Structure Type MOL
InChI Key RKGNVOKYSGKVQZ-UHFFFAOYSA-N
6
Targets
6
Activities
1
Assay Types
0
PK Parameters
9
Publications
0
Known Names

Molecular Properties

406.9
MW (Da)
6.44
ALogP
5
HBA
1
HBD
50.7
PSA (Ų)
0.37
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 C21H12ClFN4S
MW 406.87
Aromatic Rings 5
Heavy Atoms 28
NP-Likeness -2.29

Activity Summary

IC50 6 meas. best 6.29

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Aurora kinase B
CHEMBL2185
IC50 6.29 6.29 510.0 1
Proto-oncogene tyrosine-protein kinase Src
CHEMBL267
IC50 6.16 6.16 700.0 1
Vascular endothelial growth factor receptor 2
CHEMBL279
IC50 6.1 6.1 800.0 1
Angiopoietin-1 receptor
CHEMBL4128
IC50 6.0 6.0 1000.0 1
Ephrin type-B receptor 4
CHEMBL5147
IC50 6.0 6.0 1000.0 1
Insulin-like growth factor 1 receptor
CHEMBL1957
IC50 5.96 5.96 1100.0 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 A 1
19211246 10.1016/j.bmcl.2009.01.054 Epidermal growth factor receptor 1
19211246 10.1016/j.bmcl.2009.01.054 Insulin 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 Ephrin type-B receptor 4 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 2 1
19211246 10.1016/j.bmcl.2009.01.054 Proto-oncogene tyrosine-protein kinase Src 1
19211246 10.1016/j.bmcl.2009.01.054 Aurora kinase B 1

Data from ChEMBL 36 via Core Engine