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Compound Detail

CHEMBL3828225

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CC(C)=CCC/C(C)=C/C[C@@H]1C[C@]2(CC=C(C)C)C(=O)[C@@](CC=C(C)C)(C(=O)C(Cc3ccc(O)c(O)c3)=C2O)[C@@]1(C)CCC=C(C)C

Basic Information

ChEMBL ID CHEMBL3828225
Phase Preclinical
Structure Type MOL
InChI Key DTKZLRNMMJFGPD-NSKWMCEGSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
9
Publications
0
Known Names

Molecular Properties

657.0
MW (Da)
11.14
ALogP
5
HBA
3
HBD
94.8
PSA (Ų)
0.11
QED
2
Ro5 Violations
14
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C43H60O5
MW 656.95
Aromatic Rings 1
Heavy Atoms 48
NP-Likeness 2.20

Activity Summary

IC50 2 meas. best 5.05

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
NAD-dependent protein deacetylase sirtuin-1
CHEMBL4506
IC50 5.05 5.05 9000.0 1
NAD-dependent protein deacetylase sirtuin-2
CHEMBL4462
IC50 4.66 4.66 22000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
27396929 10.1016/j.bmc.2016.06.054 Hepatocyte growth factor receptor 2
27396929 10.1016/j.bmc.2016.06.054 NON-PROTEIN TARGET 2
27396929 10.1016/j.bmc.2016.06.054 HepG2 1
27396929 10.1016/j.bmc.2016.06.054 AGS 1
27396929 10.1016/j.bmc.2016.06.054 A549 1
27396929 10.1016/j.bmc.2016.06.054 HeLa 1
27396929 10.1016/j.bmc.2016.06.054 HT-29 1
27153347 10.1016/j.ejmech.2016.04.063 NAD-dependent protein deacetylase sirtuin-2 1
27153347 10.1016/j.ejmech.2016.04.063 NAD-dependent protein deacetylase sirtuin-1 1

Data from ChEMBL 36 via Core Engine