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Compound Detail

CHEMBL443906

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c1cc(Nc2ncnc3[nH]cnc23)cc(-c2nc3ccccc3s2)c1

Basic Information

ChEMBL ID CHEMBL443906
Phase Preclinical
Structure Type MOL
InChI Key SRCAIQMBBDVLGX-UHFFFAOYSA-N
5
Targets
5
Activities
1
Assay Types
0
PK Parameters
11
Publications
0
Known Names

Molecular Properties

344.4
MW (Da)
4.37
ALogP
6
HBA
2
HBD
79.4
PSA (Ų)
0.51
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C18H12N6S
MW 344.40
Aromatic Rings 5
Heavy Atoms 25
NP-Likeness -1.87

Activity Summary

IC50 5 meas. best 6.08

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Ephrin type-B receptor 4
CHEMBL5147
IC50 6.08 6.08 840.0 1
Vascular endothelial growth factor receptor 2
CHEMBL279
IC50 6.06 6.06 870.0 1
Proto-oncogene tyrosine-protein kinase Src
CHEMBL267
IC50 5.96 5.96 1100.0 1
Insulin-like growth factor 1 receptor
CHEMBL1957
IC50 5.92 5.92 1200.0 1
Epidermal growth factor receptor
CHEMBL203
IC50 5.77 5.77 1700.0 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 Insulin receptor 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 Proto-oncogene tyrosine-protein kinase Src 1
19211246 10.1016/j.bmcl.2009.01.054 Vascular endothelial growth factor receptor 2 1
19211246 10.1016/j.bmcl.2009.01.054 Ephrin type-B receptor 4 1
19211246 10.1016/j.bmcl.2009.01.054 Platelet-derived growth factor receptor beta 1
19211246 10.1016/j.bmcl.2009.01.054 Vascular endothelial growth factor receptor 3 1
19211246 10.1016/j.bmcl.2009.01.054 Angiopoietin-1 receptor 1

Data from ChEMBL 36 via Core Engine