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Compound Detail

CHEMBL2063329

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O=C(NCc1ccc(-c2cc(NC(=O)c3ccc(OCCN4CCCC4)cc3)[nH]n2)cc1)OCc1cccnc1

Basic Information

ChEMBL ID CHEMBL2063329
Phase Preclinical
Structure Type MOL
InChI Key QSHCYUWYCJJVRK-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
6
Publications
0
Known Names

Molecular Properties

540.6
MW (Da)
4.63
ALogP
7
HBA
3
HBD
121.5
PSA (Ų)
0.25
QED
1
Ro5 Violations
11
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C30H32N6O4
MW 540.62
Aromatic Rings 4
Heavy Atoms 40
NP-Likeness -1.64

Activity Summary

IC50 1 meas. best 7.46

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Receptor-type tyrosine-protein kinase FLT3
CHEMBL1974
IC50 7.46 7.46 35.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 266.0 ng.hr.mL-1 Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Receptor-type tyrosine-protein kinase FLT3 IC50 = 35.0 nM 7.46 Inhibition of wild type FLT3 22726931

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