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Compound Detail

CHEMBL1450796

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Cc1ccc(-c2nc3c(=O)n(C)c(=O)nc-3n(C)n2)cc1

Basic Information

ChEMBL ID CHEMBL1450796
Phase Preclinical
Structure Type MOL
InChI Key ADLBKNFHIOUYGV-UHFFFAOYSA-N
2
Targets
2
Activities
2
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

283.3
MW (Da)
0.35
ALogP
7
HBA
0
HBD
82.7
PSA (Ų)
0.64
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 C14H13N5O2
MW 283.29
Aromatic Rings 1
Heavy Atoms 21
NP-Likeness -1.15

Activity Summary

EC50 1 meas. best 6.54
IC50 1 meas. best 6.96

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
NAD-dependent protein deacetylase sirtuin-1
CHEMBL4506
IC50 6.96 6.96 110.0 1
Tyrosyl-DNA phosphodiesterase 2
CHEMBL2169736
EC50 6.54 6.54 290.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
23859074 10.1021/jm400568p Tyrosyl-DNA phosphodiesterase 2 2
23859074 10.1021/jm400568p Tyrosyl-DNA phosphodiesterase 1 1
23859074 10.1021/jm400568p DNA repair nuclease/redox regulator APEX1 1
27153347 10.1016/j.ejmech.2016.04.063 NAD-dependent protein deacetylase sirtuin-1 1
27153347 10.1016/j.ejmech.2016.04.063 NAD-dependent protein deacetylase sirtuin-2 1

Data from ChEMBL 36 via Core Engine