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Compound Detail

CHEMBL2332040

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CCNC(=O)c1ccc(C(=O)NCCN2CCN(c3ncnc4cc(C(N)=O)sc34)CC2)s1

Basic Information

ChEMBL ID CHEMBL2332040
Phase Preclinical
Structure Type MOL
InChI Key PHJKODPPONELIT-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

487.6
MW (Da)
1.15
ALogP
9
HBA
3
HBD
133.6
PSA (Ų)
0.43
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H25N7O3S2
MW 487.61
Aromatic Rings 3
Heavy Atoms 33
NP-Likeness -1.76

Activity Summary

IC50 3 meas. best 8.32

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
NAD-dependent protein deacetylase sirtuin-2
CHEMBL4462
IC50 8.32 8.32 4.8 1
NAD-dependent protein deacetylase sirtuin-3, mitochondrial
CHEMBL4461
IC50 7.64 7.64 23.0 1
NAD-dependent protein deacetylase sirtuin-1
CHEMBL4506
IC50 7.51 7.51 31.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
23570514 10.1021/jm400204k No relevant target 2
23570514 10.1021/jm400204k NAD-dependent protein deacetylase sirtuin-3, mitochondrial 1
23570514 10.1021/jm400204k NAD-dependent protein deacetylase sirtuin-2 1
23570514 10.1021/jm400204k NAD-dependent protein deacetylase sirtuin-1 1

Data from ChEMBL 36 via Core Engine