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Compound Detail

CHEMBL4165684

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O=C(NO)c1ccc(CCN2C(=O)c3cccc4c(N5CCOCC5)ccc(c34)C2=O)cc1

Basic Information

ChEMBL ID CHEMBL4165684
Phase Preclinical
Structure Type MOL
InChI Key CVFBZTABCOVCDI-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
13
Publications
0
Known Names

Molecular Properties

445.5
MW (Da)
2.63
ALogP
6
HBA
2
HBD
99.2
PSA (Ų)
0.36
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H23N3O5
MW 445.48
Aromatic Rings 3
Heavy Atoms 33
NP-Likeness -1.06

Activity Summary

IC50 3 meas. best 6.86

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histone deacetylase 6
CHEMBL1865
IC50 6.86 6.86 139.0 1
Polyamine deacetylase HDAC10
CHEMBL5103
IC50 5.73 5.73 1870.0 1
Histone deacetylase 8
CHEMBL3192
IC50 5.52 5.52 3050.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
29102179 10.1016/j.ejmech.2017.10.022 Histone deacetylase 6 5
29102179 10.1016/j.ejmech.2017.10.022 ADMET 2
29102179 10.1016/j.ejmech.2017.10.022 Histone deacetylase 1/2/3 1
29102179 10.1016/j.ejmech.2017.10.022 Histone deacetylase 11 1
29102179 10.1016/j.ejmech.2017.10.022 Polyamine deacetylase HDAC10 1
29102179 10.1016/j.ejmech.2017.10.022 Histone deacetylase 9 1
29102179 10.1016/j.ejmech.2017.10.022 Histone deacetylase 8 1
29102179 10.1016/j.ejmech.2017.10.022 Histone deacetylase 7 1
29102179 10.1016/j.ejmech.2017.10.022 Histone deacetylase 5 1
29102179 10.1016/j.ejmech.2017.10.022 Histone deacetylase 4 1
29102179 10.1016/j.ejmech.2017.10.022 Histone deacetylase 3 1
29102179 10.1016/j.ejmech.2017.10.022 Histone deacetylase 2 1
29102179 10.1016/j.ejmech.2017.10.022 Histone deacetylase 1 1

Data from ChEMBL 36 via Core Engine