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Compound Detail

CHEMBL270093

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COc1cc2nccc(Oc3ccc4c(c3)OCCN4C(=O)NCc3ccc(C)cc3)c2cc1OC

Basic Information

ChEMBL ID CHEMBL270093
Phase Preclinical
Structure Type MOL
InChI Key RKFUKWHBZZWJNX-UHFFFAOYSA-N
5
Targets
7
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

485.5
MW (Da)
5.46
ALogP
6
HBA
1
HBD
82.2
PSA (Ų)
0.39
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H27N3O5
MW 485.54
Aromatic Rings 4
Heavy Atoms 36
NP-Likeness -1.05

Activity Summary

IC50 7 meas. best 7.59

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Vascular endothelial growth factor receptor 2
CHEMBL279
IC50 7.59 7.585 25.7 2
Tyrosine-protein kinase Lck
CHEMBL258
IC50 6.82 6.82 150.0 1
HUVEC
CHEMBL613979
IC50 6.44 6.2 360.0 2
Hepatocyte growth factor receptor
CHEMBL3717
IC50 6.3 6.3 500.0 1
Angiopoietin-1 receptor
CHEMBL4128
IC50 5.82 5.82 1500.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
18311900 10.1021/jm701129j HUVEC 2
18311900 10.1021/jm701129j Vascular endothelial growth factor receptor 2 1
18311900 10.1021/jm701129j Angiopoietin-1 receptor 1
18311900 10.1021/jm701129j Hepatocyte growth factor receptor 1
18311900 10.1021/jm701129j Tyrosine-protein kinase Lck 1
19081278 10.1016/j.jmgm.2008.10.006 Vascular endothelial growth factor receptor 2 1

Data from ChEMBL 36 via Core Engine