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Compound Detail

CHEMBL375617

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COc1ccc(C#Cc2cnc(N)nc2)cc1C(=O)Nc1cc(C(F)(F)F)ccc1N1CCCCC1

Basic Information

ChEMBL ID CHEMBL375617
Phase Preclinical
Structure Type MOL
InChI Key RRZDLEADQGXQKI-UHFFFAOYSA-N
2
Targets
3
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

495.5
MW (Da)
4.73
ALogP
6
HBA
2
HBD
93.4
PSA (Ų)
0.51
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H24F3N5O2
MW 495.51
Aromatic Rings 3
Heavy Atoms 36
NP-Likeness -1.46

Activity Summary

IC50 3 meas. best 7.68

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Angiopoietin-1 receptor
CHEMBL4128
IC50 7.68 6.8 21.0 2
Vascular endothelial growth factor receptor 2
CHEMBL279
IC50 6.41 6.41 390.0 1

Activity Data Samples

Top measurements by pChEMBL value

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