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Compound Detail

CHEMBL209555

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O=C(NC1CC1)c1ccc(F)c(CCc2cnc(Nc3ccccn3)s2)c1

Basic Information

ChEMBL ID CHEMBL209555
Phase Preclinical
Structure Type MOL
InChI Key CMTFYUMOJRAUPR-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

382.5
MW (Da)
4.10
ALogP
5
HBA
2
HBD
66.9
PSA (Ų)
0.65
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H19FN4OS
MW 382.46
Aromatic Rings 3
Heavy Atoms 27
NP-Likeness -1.94

Activity Summary

IC50 2 meas. best 8.3

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
HUVEC
CHEMBL613979
IC50 8.3 8.3 5.0 1
Vascular endothelial growth factor receptor 2
CHEMBL279
IC50 7.85 7.85 14.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
HUVEC IC50 = 5.0 nM 8.3 Antiproliferative activity against VEGF-stimulated HUVEC 16789733
Vascular endothelial growth factor receptor 2 IC50 = 14.0 nM 7.85 Inhibition of VEGFR2 16789733

Literature References

PubMed DOI Target Context # Activities
16789733 10.1021/jm060347y L2987 1
16789733 10.1021/jm060347y HUVEC 1
16789733 10.1021/jm060347y Vascular endothelial growth factor receptor 2 1

Data from ChEMBL 36 via Core Engine