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Compound Detail

CHEMBL2063328

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CN1CCN(c2ccc(C(=O)Nc3cc(-c4ccc(CNC(=O)OCc5cccnc5)cc4)n[nH]3)cc2)CC1

Basic Information

ChEMBL ID CHEMBL2063328
Phase Preclinical
Structure Type MOL
InChI Key UYKQCKLULNMAQI-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
1
PK Parameters
6
Publications
0
Known Names

Molecular Properties

525.6
MW (Da)
3.90
ALogP
7
HBA
3
HBD
115.5
PSA (Ų)
0.32
QED
1
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H31N7O3
MW 525.61
Aromatic Rings 4
Heavy Atoms 39
NP-Likeness -1.67

Activity Summary

IC50 3 meas. best 7.85

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Receptor-type tyrosine-protein kinase FLT3
CHEMBL1974
IC50 7.85 7.85 14.0 1
Vascular endothelial growth factor receptor 2
CHEMBL279
IC50 6.66 6.66 220.0 1
Vascular endothelial growth factor receptor 1
CHEMBL1868
IC50 6.6 6.6 250.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 272.0 ng.hr.mL-1 Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
22726931 10.1016/j.bmcl.2012.05.116 Receptor-type tyrosine-protein kinase FLT3 1
22726931 10.1016/j.bmcl.2012.05.116 Vascular endothelial growth factor receptor 1 1
22726931 10.1016/j.bmcl.2012.05.116 Vascular endothelial growth factor receptor 2 1
22726931 10.1016/j.bmcl.2012.05.116 Aurora kinase A 1
22726931 10.1016/j.bmcl.2012.05.116 MOLM-13 1
22726931 10.1016/j.bmcl.2012.05.116 Rattus norvegicus 1

Data from ChEMBL 36 via Core Engine