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Compound Detail

CHEMBL2063334

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CN1CCN(c2ccc(C(=O)Nc3cc(-c4ccc(CNS(=O)(=O)c5ccccc5)cc4)n[nH]3)cc2)CC1

Basic Information

ChEMBL ID CHEMBL2063334
Phase Preclinical
Structure Type MOL
InChI Key WFYFFAMAONWHGA-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

530.6
MW (Da)
3.56
ALogP
6
HBA
3
HBD
110.4
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 C28H30N6O3S
MW 530.65
Aromatic Rings 4
Heavy Atoms 38
NP-Likeness -1.87

Activity Summary

IC50 2 meas. best 6.85

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Receptor-type tyrosine-protein kinase FLT3
CHEMBL1974
IC50 6.85 6.85 140.0 1
Aurora kinase A
CHEMBL4722
IC50 6.0 6.0 1000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Receptor-type tyrosine-protein kinase FLT3 IC50 = 140.0 nM 6.85 Inhibition of wild type FLT3 22726931
Aurora kinase A IC50 = 1000.0 nM 6.0 Inhibition of Aurora A 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

Data from ChEMBL 36 via Core Engine