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Compound Detail

CHEMBL152543

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O=C(/C=C/c1ccc(CNC(=O)c2ccc(N3CCCC3)cc2)cc1)NO

Basic Information

ChEMBL ID CHEMBL152543
Phase Preclinical
Structure Type MOL
InChI Key JKVNVKOVLBVYHQ-KPKJPENVSA-N
4
Targets
8
Activities
1
Assay Types
0
PK Parameters
17
Publications
0
Known Names

Molecular Properties

365.4
MW (Da)
2.74
ALogP
4
HBA
3
HBD
81.7
PSA (Ų)
0.42
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H23N3O3
MW 365.43
Aromatic Rings 2
Heavy Atoms 27
NP-Likeness -0.96

Activity Summary

IC50 8 meas. best 6.96

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
SK-BR-3
CHEMBL613834
IC50 6.96 6.96 110.0 2
Histone deacetylase
CHEMBL2093865
IC50 6.69 6.69 205.0 2
A549
CHEMBL392
IC50 6.46 6.46 350.0 2
MKN-45
CHEMBL614354
IC50 6.1 6.1 800.0 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
18247554 10.1021/jm7011408 Histone deacetylase 9 1
18247554 10.1021/jm7011408 Histone deacetylase 8 1
18247554 10.1021/jm7011408 Histone deacetylase 7 1
18247554 10.1021/jm7011408 Histone deacetylase 6 1
18247554 10.1021/jm7011408 Histone deacetylase 5 1
18247554 10.1021/jm7011408 Histone deacetylase 4 1
18247554 10.1021/jm7011408 Histone deacetylase 3 1
18247554 10.1021/jm7011408 Histone deacetylase 2 1
18247554 10.1021/jm7011408 Histone deacetylase 1 1
14667227 10.1021/jm030377q A549 1
18247554 10.1021/jm7011408 SK-BR-3 1
18247554 10.1021/jm7011408 Histone deacetylase 1
18247554 10.1021/jm7011408 MKN-45 1
18247554 10.1021/jm7011408 A549 1
14667227 10.1021/jm030377q Histone deacetylase 1
14667227 10.1021/jm030377q MKN-45 1
14667227 10.1021/jm030377q SK-BR-3 1

Data from ChEMBL 36 via Core Engine