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Compound Detail

CHEMBL221544

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CN(C)[C@@H]1CCN(c2ccc(C(F)(F)F)cc2NC(=O)c2cc(C#Cc3cnc(N)nc3)ccc2F)C1

Basic Information

ChEMBL ID CHEMBL221544
Phase Preclinical
Structure Type MOL
InChI Key CERIBYHZTSTEHD-LJQANCHMSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

512.5
MW (Da)
4.01
ALogP
6
HBA
2
HBD
87.4
PSA (Ų)
0.41
QED
1
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H24F4N6O
MW 512.51
Aromatic Rings 3
Heavy Atoms 37
NP-Likeness -1.82

Activity Summary

IC50 3 meas. best 6.66

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Angiopoietin-1 receptor
CHEMBL4128
IC50 6.66 6.66 220.0 1
Vascular endothelial growth factor receptor 2
CHEMBL279
IC50 6.05 6.05 890.0 1
Tyrosine-protein kinase Lck
CHEMBL258
IC50 5.72 5.72 1920.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Angiopoietin-1 receptor IC50 = 220.0 nM 6.66 Inhibition of TIE2 by HTRF assay 17253679
Vascular endothelial growth factor receptor 2 IC50 = 890.0 nM 6.05 Inhibition of KDR 17253679
Tyrosine-protein kinase Lck IC50 = 1920.0 nM 5.72 Inhibition of LCK 17253679

Literature References

PubMed DOI Target Context # Activities
17253679 10.1021/jm061112p Angiopoietin-1 receptor 2
17253679 10.1021/jm061112p Vascular endothelial growth factor receptor 2 1
17253679 10.1021/jm061112p Tyrosine-protein kinase Lck 1

Data from ChEMBL 36 via Core Engine