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Compound Detail

CHEMBL4782188

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CCC(=O)CCCCCC(NC(=O)c1cncs1)c1[nH]c(-c2ccccc2)nc1C(=O)NC

Basic Information

ChEMBL ID CHEMBL4782188
Phase Preclinical
Structure Type MOL
InChI Key PLHIZHDQYPUMEN-UHFFFAOYSA-N
6
Targets
7
Activities
2
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

467.6
MW (Da)
4.29
ALogP
6
HBA
3
HBD
116.8
PSA (Ų)
0.34
QED
0
Ro5 Violations
12
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H29N5O3S
MW 467.60
Aromatic Rings 3
Heavy Atoms 33
NP-Likeness -0.47

Activity Summary

IC50 5 meas. best 8.33
EC50 2 meas. best 6.24

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histone deacetylase 3
CHEMBL1829
IC50 8.33 8.33 4.7 1
Histone deacetylase 1
CHEMBL325
IC50 7.56 7.56 27.6 1
Histone deacetylase 2
CHEMBL1937
IC50 7.04 7.04 91.4 1
Class 1 histone deacetylase
CHEMBL4523988
EC50 6.24 5.99 570.0 2
Histone deacetylase 8
CHEMBL3192
IC50 5.13 5.13 7471.0 1
Histone deacetylase 6
CHEMBL1865
IC50 4.54 4.54 29180.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
32738976 10.1016/j.bmcl.2020.127367 Class 1 histone deacetylase 2
32738976 10.1016/j.bmcl.2020.127367 Histone deacetylase 8 1
32738976 10.1016/j.bmcl.2020.127367 Histone deacetylase 6 1
32738976 10.1016/j.bmcl.2020.127367 Histone deacetylase 2 1
32738976 10.1016/j.bmcl.2020.127367 Histone deacetylase 3 1
32738976 10.1016/j.bmcl.2020.127367 Histone deacetylase 1 1

Data from ChEMBL 36 via Core Engine