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Compound Detail

CHEMBL270342

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COc1ccc2c(Oc3ccc4c(C(=O)NC5CC5)cccc4c3)ccnc2c1

Basic Information

ChEMBL ID CHEMBL270342
Phase Preclinical
Structure Type MOL
InChI Key VCDOUBNPUAACRA-UHFFFAOYSA-N
5
Targets
6
Activities
1
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

384.4
MW (Da)
5.08
ALogP
4
HBA
1
HBD
60.5
PSA (Ų)
0.52
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 C24H20N2O3
MW 384.44
Aromatic Rings 4
Heavy Atoms 29
NP-Likeness -0.79

Activity Summary

IC50 6 meas. best 9.35

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Vascular endothelial growth factor receptor 2
CHEMBL279
IC50 9.35 9.35 0.4 2
HUVEC
CHEMBL613979
IC50 8.47 8.47 3.4 1
Angiopoietin-1 receptor
CHEMBL4128
IC50 5.08 5.08 8300.0 1
Aurora kinase A
CHEMBL4722
IC50 5.08 5.08 8300.0 1
Hepatocyte growth factor receptor
CHEMBL3717
IC50 4.7 4.7 20000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
18324759 10.1021/jm701098w HUVEC 2
18324759 10.1021/jm701098w Vascular endothelial growth factor receptor 2 1
18324759 10.1021/jm701098w Angiopoietin-1 receptor 1
18324759 10.1021/jm701098w Hepatocyte growth factor receptor 1
18324759 10.1021/jm701098w Aurora kinase A 1
18324759 10.1021/jm701098w Aurora kinase B 1
19081278 10.1016/j.jmgm.2008.10.006 Vascular endothelial growth factor receptor 2 1

Data from ChEMBL 36 via Core Engine