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Compound Detail

CHEMBL381283

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Nc1c(-c2nc3cc(N4CCOCC4)ccc3[nH]2)c(O)nc2ccncc12

Basic Information

ChEMBL ID CHEMBL381283
Phase Preclinical
Structure Type MOL
InChI Key QXCNZYXAYYZRIY-UHFFFAOYSA-N
5
Targets
5
Activities
2
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

362.4
MW (Da)
2.30
ALogP
7
HBA
3
HBD
113.2
PSA (Ų)
0.50
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C19H18N6O2
MW 362.39
Aromatic Rings 4
Heavy Atoms 27
NP-Likeness -1.24

Activity Summary

IC50 4 meas. best 7.75
EC50 1 meas. best 6.12

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Platelet-derived growth factor receptor beta
CHEMBL2749
IC50 7.75 7.75 18.0 1
Vascular endothelial growth factor receptor 1
CHEMBL1868
IC50 7.43 7.43 37.0 1
Vascular endothelial growth factor receptor 2
CHEMBL3337
IC50 7.24 7.24 57.0 1
Fibroblast growth factor receptor 1
CHEMBL3650
IC50 7.0 7.0 100.0 1
HMEC
CHEMBL614734
EC50 6.12 6.12 768.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
16446087 10.1016/j.bmcl.2006.01.020 Vascular endothelial growth factor receptor 1 1
16446087 10.1016/j.bmcl.2006.01.020 Vascular endothelial growth factor receptor 2 1
16446087 10.1016/j.bmcl.2006.01.020 Platelet-derived growth factor receptor beta 1
16446087 10.1016/j.bmcl.2006.01.020 Fibroblast growth factor receptor 1 1
16446087 10.1016/j.bmcl.2006.01.020 HMEC 1

Data from ChEMBL 36 via Core Engine