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Compound Detail

CHEMBL3290218

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CCOC(=O)c1ccc2c(c1)nc(-c1ccc(N(C)C)cc1)n2-c1ccccc1

Basic Information

ChEMBL ID CHEMBL3290218
Phase Preclinical
Structure Type MOL
InChI Key GMHMLPREGQGSSE-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

385.5
MW (Da)
4.94
ALogP
5
HBA
0
HBD
47.4
PSA (Ų)
0.46
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H23N3O2
MW 385.47
Aromatic Rings 4
Heavy Atoms 29
NP-Likeness -1.35

Activity Summary

IC50 2 meas. best 4.57

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
NAD-dependent protein deacetylase sirtuin-2
CHEMBL4462
IC50 4.57 4.57 26850.0 1
NAD-dependent protein deacetylase sirtuin-1
CHEMBL4506
IC50 4.31 4.31 49120.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
24992072 10.1016/j.ejmech.2014.06.060 NAD-dependent protein deacetylase sirtuin-1 2
24992072 10.1016/j.ejmech.2014.06.060 NAD-dependent protein deacetylase sirtuin-2 2
24992072 10.1016/j.ejmech.2014.06.060 ADMET 1
24992072 10.1016/j.ejmech.2014.06.060 HCT-116 1
24992072 10.1016/j.ejmech.2014.06.060 MDA-MB-468 1
24992072 10.1016/j.ejmech.2014.06.060 CCRF-CEM 1

Data from ChEMBL 36 via Core Engine