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Compound Detail

CHEMBL589918

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O=C(CCCCC[C@@H]1NC(=O)[C@H]2CCCN2C(=O)[C@@H]2CCCCCCCCCCCC[C@@H](NC1=O)C(=O)N2)NO

Basic Information

ChEMBL ID CHEMBL589918
Phase Preclinical
Structure Type MOL
InChI Key WJKLHHHHJUCBTH-NAVOZUGXSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

563.7
MW (Da)
2.60
ALogP
6
HBA
5
HBD
156.9
PSA (Ų)
0.19
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H49N5O6
MW 563.74
Aromatic Rings 0
Heavy Atoms 40
NP-Likeness 0.55

Activity Summary

IC50 3 meas. best 8.3

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histone deacetylase 4
CHEMBL3524
IC50 8.3 8.3 5.0 1
Histone deacetylase 1
CHEMBL325
IC50 7.89 7.89 13.0 1
Histone deacetylase 6
CHEMBL1865
IC50 6.62 6.62 240.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Histone deacetylase 4 IC50 = 5.0 nM 8.3 Inhibition of HDAC4 20045316
Histone deacetylase 1 IC50 = 13.0 nM 7.89 Inhibition of HDAC1 20045316
Histone deacetylase 6 IC50 = 240.0 nM 6.62 Inhibition of HDAC6 20045316

Literature References

PubMed DOI Target Context # Activities
20045316 10.1016/j.bmcl.2009.12.054 Histone deacetylase 4 2
20045316 10.1016/j.bmcl.2009.12.054 Histone deacetylase 1 1
20045316 10.1016/j.bmcl.2009.12.054 Histone deacetylase 6 1

Data from ChEMBL 36 via Core Engine