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Compound Detail

CHEMBL1940104

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COc1cccc(NC(=O)Cn2cc(Nc3ncnc4cc(OC)c(OC)cc34)cn2)c1

Basic Information

ChEMBL ID CHEMBL1940104
Phase Preclinical
Structure Type MOL
InChI Key FWRUVEHMIVRQGU-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
1
PK Parameters
9
Publications
0
Known Names

Molecular Properties

434.5
MW (Da)
3.23
ALogP
9
HBA
2
HBD
112.4
PSA (Ų)
0.43
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 C22H22N6O4
MW 434.46
Aromatic Rings 4
Heavy Atoms 32
NP-Likeness -1.77

Activity Summary

IC50 2 meas. best 8.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Platelet-derived growth factor receptor beta
CHEMBL1913
IC50 8.0 8.0 10.0 1
Vascular endothelial growth factor receptor 3
CHEMBL1955
IC50 7.6 7.6 25.0 1

Pharmacokinetic Data

Parameter Value Units Species
F 20.0 % Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
22153662 10.1016/j.bmcl.2011.11.019 Aurora kinase B 1
22153662 10.1016/j.bmcl.2011.11.019 Rattus norvegicus 1
22153662 10.1016/j.bmcl.2011.11.019 No relevant target 1
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
- 10.6019/CHEMBL3301361 No relevant target 1

Data from ChEMBL 36 via Core Engine