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Compound Detail

CHEMBL428876

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Cn1cc2c(n1)CCc1c-2c2c(c3c1[nH]c1ccc(C(=O)c4cccs4)cc13)CNC2=O

Basic Information

ChEMBL ID CHEMBL428876
Phase Preclinical
Structure Type MOL
InChI Key VOZWUTXGVBZOLP-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

438.5
MW (Da)
4.36
ALogP
5
HBA
2
HBD
79.8
PSA (Ų)
0.40
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H18N4O2S
MW 438.51
Aromatic Rings 5
Heavy Atoms 32
NP-Likeness -0.41

Activity Summary

IC50 2 meas. best 8.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Vascular endothelial growth factor receptor 2
CHEMBL279
IC50 8.7 8.7 2.0 1
Angiopoietin-1 receptor
CHEMBL4128
IC50 6.87 6.87 136.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Vascular endothelial growth factor receptor 2 IC50 = 2.0 nM 8.7 Inhibition of VEGFR2 18343109
Angiopoietin-1 receptor IC50 = 136.0 nM 6.87 Inhibition of TIE2 18343109

Literature References

PubMed DOI Target Context # Activities
18343109 10.1016/j.bmcl.2008.02.069 Angiopoietin-1 receptor 1
18343109 10.1016/j.bmcl.2008.02.069 Vascular endothelial growth factor receptor 2 1

Data from ChEMBL 36 via Core Engine