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Compound Detail

CHEMBL1940275

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COc1cc2ncnc(Nc3ccc(CC(=O)Nc4cnn(C(C)C)c4)cc3)c2cc1OC

Basic Information

ChEMBL ID CHEMBL1940275
Phase Preclinical
Structure Type MOL
InChI Key FQGHYVHLTQUXGX-UHFFFAOYSA-N
4
Targets
6
Activities
1
Assay Types
0
PK Parameters
12
Publications
0
Known Names

Molecular Properties

446.5
MW (Da)
4.35
ALogP
8
HBA
2
HBD
103.2
PSA (Ų)
0.41
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H26N6O3
MW 446.51
Aromatic Rings 4
Heavy Atoms 33
NP-Likeness -1.52

Activity Summary

IC50 6 meas. best 7.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Platelet-derived growth factor receptor beta
CHEMBL1913
IC50 7.7 7.7 20.0 2
Receptor-type tyrosine-protein kinase FLT3
CHEMBL1974
IC50 7.7 7.7 20.0 2
Vascular endothelial growth factor receptor 3
CHEMBL1955
IC50 6.31 6.31 485.0 1
Vascular endothelial growth factor receptor 2
CHEMBL279
IC50 6.31 6.31 485.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
30204441 10.1021/acs.jmedchem.8b00938 Mast/stem cell growth factor receptor Kit 3
22153662 10.1016/j.bmcl.2011.11.019 Platelet-derived growth factor receptor beta 1
22153662 10.1016/j.bmcl.2011.11.019 Vascular endothelial growth factor receptor 3 1
22153662 10.1016/j.bmcl.2011.11.019 Macrophage colony-stimulating factor 1 receptor 1
22153662 10.1016/j.bmcl.2011.11.019 Receptor-type tyrosine-protein kinase FLT3 1
22153662 10.1016/j.bmcl.2011.11.019 Platelet-derived growth factor receptor alpha 1
22497760 10.1016/j.bmcl.2012.03.074 Platelet-derived growth factor receptor beta 1
22497760 10.1016/j.bmcl.2012.03.074 Receptor-type tyrosine-protein kinase FLT3 1
22497760 10.1016/j.bmcl.2012.03.074 Vascular endothelial growth factor receptor 2 1
22497760 10.1016/j.bmcl.2012.03.074 Macrophage colony-stimulating factor 1 receptor 1
30204441 10.1021/acs.jmedchem.8b00938 BaF3 1
30204441 10.1021/acs.jmedchem.8b00938 Vascular endothelial growth factor receptor 2 1

Data from ChEMBL 36 via Core Engine