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Compound Detail

CHEMBL89040

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Cc1cccc2c1/C(=C/c1ccc(N3CCN(C=O)CC3)cc1)C(=O)N2

Basic Information

ChEMBL ID CHEMBL89040
Phase Preclinical
Structure Type MOL
InChI Key GOJTWENDGDLCOU-AQTBWJFISA-N
5
Targets
5
Activities
1
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

347.4
MW (Da)
2.77
ALogP
3
HBA
1
HBD
52.6
PSA (Ų)
0.69
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H21N3O2
MW 347.42
Aromatic Rings 2
Heavy Atoms 26
NP-Likeness -0.75

Activity Summary

IC50 5 meas. best 5.6

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Vascular endothelial growth factor receptor 2
CHEMBL3337
IC50 5.6 5.6 2511.9 1
Vascular endothelial growth factor receptor 1
CHEMBL3516
IC50 5.6 5.6 2500.0 1
Proto-oncogene tyrosine-protein kinase receptor Ret
CHEMBL2041
IC50 5.43 5.43 3700.0 1
Platelet-derived growth factor receptor beta
CHEMBL1913
IC50 4.61 4.61 24500.0 1
Insulin-like growth factor 1 receptor
CHEMBL1957
IC50 4.17 4.17 67600.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
10956210 10.1021/jm990609e Vascular endothelial growth factor receptor 2 1
9651163 10.1021/jm980123i Platelet-derived growth factor receptor beta 1
9651163 10.1021/jm980123i Vascular endothelial growth factor receptor 1 1
9651163 10.1021/jm980123i Epidermal growth factor receptor 1
9651163 10.1021/jm980123i Receptor tyrosine-protein kinase erbB-2 1
9651163 10.1021/jm980123i Insulin-like growth factor 1 receptor 1
20117004 10.1016/j.bmc.2010.01.011 Proto-oncogene tyrosine-protein kinase receptor Ret 1

Data from ChEMBL 36 via Core Engine