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Compound Detail

CHEMBL89483

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Cc1ccc2c(c1)/C(=C/c1[nH]c(C)cc1C)C(=O)N2

Basic Information

ChEMBL ID CHEMBL89483
Phase Preclinical
Structure Type MOL
InChI Key KRYNNRXFWOEDRQ-JYRVWZFOSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

252.3
MW (Da)
3.43
ALogP
1
HBA
2
HBD
44.9
PSA (Ų)
0.75
QED
0
Ro5 Violations
1
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C16H16N2O
MW 252.32
Aromatic Rings 2
Heavy Atoms 19
NP-Likeness -0.41

Activity Summary

IC50 4 meas. best 6.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Vascular endothelial growth factor receptor 2
CHEMBL3337
IC50 6.52 6.52 302.0 1
Vascular endothelial growth factor receptor 1
CHEMBL3516
IC50 6.52 6.52 300.0 1
Proto-oncogene tyrosine-protein kinase receptor Ret
CHEMBL2041
IC50 5.1 5.1 8000.0 1
Platelet-derived growth factor receptor beta
CHEMBL1913
IC50 4.59 4.59 25500.0 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