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Compound Detail

CHEMBL218431

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CNc1nccc(-c2cc(C)cnc2Oc2cccc(C(=O)Nc3cc(C(F)(F)F)ccc3N3CCCCC3)c2C)n1

Basic Information

ChEMBL ID CHEMBL218431
Phase Preclinical
Structure Type MOL
InChI Key WDEPCTJBPQDCEB-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

576.6
MW (Da)
7.25
ALogP
7
HBA
2
HBD
92.3
PSA (Ų)
0.24
QED
2
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C31H31F3N6O2
MW 576.62
Aromatic Rings 4
Heavy Atoms 42
NP-Likeness -1.48

Activity Summary

IC50 2 meas. best 6.41

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Angiopoietin-1 receptor
CHEMBL4128
IC50 6.41 6.41 388.0 1
Vascular endothelial growth factor receptor 2
CHEMBL279
IC50 5.58 5.58 2600.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Angiopoietin-1 receptor IC50 = 388.0 nM 6.41 Inhibition of Tie2 by HTRF assay 17253678
Vascular endothelial growth factor receptor 2 IC50 = 2600.0 nM 5.58 Inhibition of KDR by HTRF assay 17253678

Literature References

PubMed DOI Target Context # Activities
17253678 10.1021/jm061107l Vascular endothelial growth factor receptor 2 1
17253678 10.1021/jm061107l Angiopoietin-1 receptor 1

Data from ChEMBL 36 via Core Engine