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Compound Detail

CHEMBL220052

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Cc1ccc(C(=O)Nc2cc(C(F)(F)F)ccc2N2CCOCC2)cc1Oc1ncccc1-c1ccncn1

Basic Information

ChEMBL ID CHEMBL220052
Phase Preclinical
Structure Type MOL
InChI Key CWCDKJWYUZLNHQ-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

535.5
MW (Da)
5.75
ALogP
7
HBA
1
HBD
89.5
PSA (Ų)
0.34
QED
2
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H24F3N5O3
MW 535.53
Aromatic Rings 4
Heavy Atoms 39
NP-Likeness -1.80

Activity Summary

IC50 1 meas. best 6.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Angiopoietin-1 receptor
CHEMBL4128
IC50 6.4 6.4 399.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Angiopoietin-1 receptor IC50 = 399.0 nM 6.4 Inhibition of Tie2 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