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Compound Detail

CHEMBL4159588

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Nc1ncc2ccc(-c3ccc(NC(=O)C4(C(=O)Nc5ccc6c(c5)OCO6)CC4)cc3)cc2n1

Basic Information

ChEMBL ID CHEMBL4159588
Phase Preclinical
Structure Type MOL
InChI Key PZRHVBOBWUZFQZ-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

467.5
MW (Da)
3.97
ALogP
7
HBA
3
HBD
128.5
PSA (Ų)
0.38
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H21N5O4
MW 467.49
Aromatic Rings 4
Heavy Atoms 35
NP-Likeness -0.76

Activity Summary

IC50 2 meas. best 6.36

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Angiopoietin-1 receptor
CHEMBL4128
IC50 6.36 6.36 432.4 1
EA.hy 926
CHEMBL4296410
IC50 4.54 4.54 29200.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
29102175 10.1016/j.ejmech.2017.10.030 Vascular endothelial growth factor receptor 2 1
29102175 10.1016/j.ejmech.2017.10.030 Angiopoietin-1 receptor 1
29102175 10.1016/j.ejmech.2017.10.030 EA.hy 926 1
29102175 10.1016/j.ejmech.2017.10.030 Ephrin type-B receptor 4 1

Data from ChEMBL 36 via Core Engine