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Compound Detail

CHEMBL381794

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CN(C)C(=O)N1Cc2c(ccc3c2OCC3)C(c2cccc(O)c2)C1

Basic Information

ChEMBL ID CHEMBL381794
Phase Preclinical
Structure Type MOL
InChI Key UCOIZFMGCXDQLI-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

338.4
MW (Da)
2.96
ALogP
3
HBA
1
HBD
53.0
PSA (Ų)
0.87
QED
0
Ro5 Violations
1
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H22N2O3
MW 338.41
Aromatic Rings 2
Heavy Atoms 25
NP-Likeness 0.06

Activity Summary

IC50 2 meas. best 6.63

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
A2780
CHEMBL614004
IC50 6.63 6.63 235.0 1
Kinesin-like protein KIF11
CHEMBL4581
IC50 6.19 6.19 639.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
A2780 IC50 = 235.0 nM 6.63 Antiproliferative activity against human A2780 cells 16458511
Kinesin-like protein KIF11 IC50 = 639.0 nM 6.19 Inhibition of Eg5 by ATPase assay 16458511

Literature References

PubMed DOI Target Context # Activities
16458511 10.1016/j.bmcl.2006.01.056 Kinesin-like protein KIF11 1
16458511 10.1016/j.bmcl.2006.01.056 A2780 1

Data from ChEMBL 36 via Core Engine