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Compound Detail

CHEMBL222067

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Cc1ccc(C(=O)Nc2ccc(C(F)(F)F)cc2)cc1Nc1ncccc1-c1ccncn1

Basic Information

ChEMBL ID CHEMBL222067
Phase Preclinical
Structure Type MOL
InChI Key JQSZIQAUXOKNJP-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

449.4
MW (Da)
5.86
ALogP
5
HBA
2
HBD
79.8
PSA (Ų)
0.40
QED
1
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H18F3N5O
MW 449.44
Aromatic Rings 4
Heavy Atoms 33
NP-Likeness -1.73

Activity Summary

IC50 2 meas. best 6.75

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Vascular endothelial growth factor receptor 2
CHEMBL279
IC50 6.75 6.75 177.0 1
Angiopoietin-1 receptor
CHEMBL4128
IC50 6.3 6.3 504.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Vascular endothelial growth factor receptor 2 IC50 = 177.0 nM 6.75 Inhibition of KDR by HTRF assay 17253678
Angiopoietin-1 receptor IC50 = 504.0 nM 6.3 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
17253678 10.1021/jm061107l No relevant target 1

Data from ChEMBL 36 via Core Engine