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Compound Detail

CHEMBL1094423

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Brc1cccc(Nc2ncnc3[nH]c(CCc4ccccc4)cc23)c1

Basic Information

ChEMBL ID CHEMBL1094423
Phase Preclinical
Structure Type MOL
InChI Key FDPFCUXBRNWFJA-UHFFFAOYSA-N
2
Targets
4
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

393.3
MW (Da)
5.25
ALogP
3
HBA
2
HBD
53.6
PSA (Ų)
0.49
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 C20H17BrN4
MW 393.29
Aromatic Rings 4
Heavy Atoms 25
NP-Likeness -0.81

Activity Summary

IC50 4 meas. best 5.71

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
A-431
CHEMBL614069
IC50 5.71 5.71 1930.0 1
Platelet-derived growth factor receptor beta
CHEMBL1913
IC50 5.07 5.07 8500.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
A-431 IC50 = 1930.0 nM 5.71 Antiangiogenic activity against human A431 cells 20403693
Platelet-derived growth factor receptor beta IC50 = 8500.0 nM 5.07 Inhibition of PDGFRbeta 20403693

Literature References

PubMed DOI Target Context # Activities
20403693 10.1016/j.bmcl.2010.03.064 A-431 2
20403693 10.1016/j.bmcl.2010.03.064 Epidermal growth factor receptor 1
20403693 10.1016/j.bmcl.2010.03.064 Vascular endothelial growth factor receptor 1 1
20403693 10.1016/j.bmcl.2010.03.064 Vascular endothelial growth factor receptor 2 1
20403693 10.1016/j.bmcl.2010.03.064 Platelet-derived growth factor receptor beta 1

Data from ChEMBL 36 via Core Engine