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Compound Detail

CHEMBL271861

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Cc1csc(C(=O)c2ccc3c(c2)c2c4c(c5c(c2n3CC(C)C)CCc2nn(C)cc2-5)C(=O)NC4)c1

Basic Information

ChEMBL ID CHEMBL271861
Phase Preclinical
Structure Type MOL
InChI Key NCTPAZULGKKAQA-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

508.6
MW (Da)
5.79
ALogP
6
HBA
1
HBD
68.9
PSA (Ų)
0.31
QED
2
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C30H28N4O2S
MW 508.65
Aromatic Rings 5
Heavy Atoms 37
NP-Likeness -0.55

Activity Summary

IC50 2 meas. best 7.96

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Vascular endothelial growth factor receptor 2
CHEMBL279
IC50 7.96 7.96 11.0 1
Angiopoietin-1 receptor
CHEMBL4128
IC50 7.37 7.37 43.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Vascular endothelial growth factor receptor 2 IC50 = 11.0 nM 7.96 Inhibition of VEGFR2 18343109
Angiopoietin-1 receptor IC50 = 43.0 nM 7.37 Inhibition of TIE2 18343109

Literature References

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

Data from ChEMBL 36 via Core Engine