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Compound Detail

CHEMBL3628796

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COc1cc2ncnc(Nc3ccc(NC(=O)Nc4cccc(Br)c4)cc3)c2cc1OC

Basic Information

ChEMBL ID CHEMBL3628796
Phase Preclinical
Structure Type MOL
InChI Key VCLVPTJGTKXMSP-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
9
Publications
0
Known Names

Molecular Properties

494.4
MW (Da)
5.80
ALogP
6
HBA
3
HBD
97.4
PSA (Ų)
0.31
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H20BrN5O3
MW 494.35
Aromatic Rings 4
Heavy Atoms 32
NP-Likeness -1.18

Activity Summary

IC50 3 meas. best 8.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Mast/stem cell growth factor receptor Kit
CHEMBL1936
IC50 8.52 8.52 3.0 1
Vascular endothelial growth factor receptor 2
CHEMBL279
IC50 7.92 7.92 12.0 1
Epidermal growth factor receptor
CHEMBL203
IC50 5.11 5.11 7710.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
26526740 10.1016/j.bmc.2015.10.035 Epidermal growth factor receptor 1
26526740 10.1016/j.bmc.2015.10.035 Proto-oncogene tyrosine-protein kinase Src 1
26526740 10.1016/j.bmc.2015.10.035 RAF proto-oncogene serine/threonine-protein kinase 1
26526740 10.1016/j.bmc.2015.10.035 Hepatocyte growth factor receptor 1
26526740 10.1016/j.bmc.2015.10.035 Vascular endothelial growth factor receptor 2 1
26526740 10.1016/j.bmc.2015.10.035 Vascular endothelial growth factor receptor 1 1
26526740 10.1016/j.bmc.2015.10.035 Vascular endothelial growth factor receptor 3 1
26526740 10.1016/j.bmc.2015.10.035 Platelet-derived growth factor receptor beta 1
26526740 10.1016/j.bmc.2015.10.035 Mast/stem cell growth factor receptor Kit 1

Data from ChEMBL 36 via Core Engine