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Compound Detail

CHEMBL235411

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COc1ccc(NCc2ccc(C(=O)Nc3ccccc3O)cc2)cc1OC

Basic Information

ChEMBL ID CHEMBL235411
Phase Preclinical
Structure Type MOL
InChI Key BWIHVHAXBCNDLB-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

378.4
MW (Da)
4.27
ALogP
5
HBA
3
HBD
79.8
PSA (Ų)
0.54
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H22N2O4
MW 378.43
Aromatic Rings 3
Heavy Atoms 28
NP-Likeness -1.04

Activity Summary

IC50 2 meas. best 6.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histone deacetylase 2
CHEMBL1937
IC50 6.7 6.7 200.0 1
Histone deacetylase 1
CHEMBL325
IC50 6.52 6.52 300.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Histone deacetylase 2 IC50 = 200.0 nM 6.7 Inhibition of human recombinant HDAC2 17941625
Histone deacetylase 1 IC50 = 300.0 nM 6.52 Inhibition of human recombinant HDAC1 17941625

Literature References

PubMed DOI Target Context # Activities
17941625 10.1021/jm701079h Histone deacetylase 1 2
17941625 10.1021/jm701079h Histone deacetylase 2 2
17941625 10.1021/jm701079h Histone deacetylase 3 1
17941625 10.1021/jm701079h Histone deacetylase 8 1
17941625 10.1021/jm701079h Histone deacetylase 4 1
17941625 10.1021/jm701079h Histone deacetylase 5 1
17941625 10.1021/jm701079h Histone deacetylase 6 1
17941625 10.1021/jm701079h Histone deacetylase 7 1

Data from ChEMBL 36 via Core Engine