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Compound Detail

CHEMBL4437282

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COc1ccc(CCn2c(=O)c3ccccc3n(Cc3ccc(C(=O)NO)cc3)c2=O)cc1

Basic Information

ChEMBL ID CHEMBL4437282
Phase Preclinical
Structure Type MOL
InChI Key BRPFEMHATQFLIK-UHFFFAOYSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

445.5
MW (Da)
2.58
ALogP
7
HBA
2
HBD
102.6
PSA (Ų)
0.34
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H23N3O5
MW 445.48
Aromatic Rings 4
Heavy Atoms 33
NP-Likeness -1.03

Activity Summary

IC50 4 meas. best 7.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histone deacetylase 6
CHEMBL1865
IC50 7.7 7.7 20.0 1
Histone deacetylase 8
CHEMBL3192
IC50 5.94 5.94 1150.0 1
Histone deacetylase 1
CHEMBL325
IC50 5.13 5.13 7374.0 1
Histone deacetylase 11
CHEMBL3310
IC50 4.86 4.86 13850.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
30525585 10.1021/acs.jmedchem.8b01590 Histone deacetylase 1 1
30525585 10.1021/acs.jmedchem.8b01590 Histone deacetylase 6 1
30525585 10.1021/acs.jmedchem.8b01590 Histone deacetylase 8 1
30525585 10.1021/acs.jmedchem.8b01590 Histone deacetylase 11 1
30525585 10.1021/acs.jmedchem.8b01590 Unchecked 1

Data from ChEMBL 36 via Core Engine