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Compound Detail

CHEMBL271295

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CN(C)CCCOc1ccc(/C=C2\CC/C(=C\c3ccc(OCCCN(C)C)cc3)C2=O)cc1

Basic Information

ChEMBL ID CHEMBL271295
Phase Preclinical
Structure Type MOL
InChI Key AKERQZTUCNLYPR-CDTUYSNOSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

462.6
MW (Da)
5.18
ALogP
5
HBA
0
HBD
42.0
PSA (Ų)
0.32
QED
1
Ro5 Violations
12
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H38N2O3
MW 462.63
Aromatic Rings 2
Heavy Atoms 34
NP-Likeness -0.40

Activity Summary

IC50 4 meas. best 5.62

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
CNE
CHEMBL613824
IC50 5.62 5.62 2400.0 1
HL-60
CHEMBL383
IC50 5.48 5.48 3300.0 1
11-beta-hydroxysteroid dehydrogenase 1
CHEMBL2391
IC50 5.38 5.38 4171.0 1
NCI-H460
CHEMBL396
IC50 5.08 5.08 8310.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
23800686 10.1016/j.bmcl.2013.05.080 11-beta-hydroxysteroid dehydrogenase 1 4
18234497 10.1016/j.bmcl.2007.12.068 J774.A1 2
23800686 10.1016/j.bmcl.2013.05.080 11-beta-hydroxysteroid dehydrogenase type 2 2
19243951 10.1016/j.bmc.2008.10.044 CNE 1
19243951 10.1016/j.bmc.2008.10.044 HL-60 1
19243951 10.1016/j.bmc.2008.10.044 No relevant target 1
21504179 10.1021/jm200017g NCI-H460 1

Data from ChEMBL 36 via Core Engine