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Compound Detail

CHEMBL4452333

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CCCCCCCC(=O)SCC/C=C/[C@@H]1CC(=O)NCc2nc(cs2)C2=N[C@@](C)(CS2)C(=O)C[C@@H](C(C)C)C(=O)C1

Basic Information

ChEMBL ID CHEMBL4452333
Phase Preclinical
Structure Type MOL
InChI Key NPICYKHOEXQJGW-UNTWLVQOSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

619.9
MW (Da)
6.79
ALogP
9
HBA
1
HBD
105.6
PSA (Ų)
0.21
QED
2
Ro5 Violations
11
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C31H45N3O4S3
MW 619.92
Aromatic Rings 1
Heavy Atoms 41
NP-Likeness 1.00

Activity Summary

IC50 2 meas. best 7.94

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histone deacetylase 1
CHEMBL325
IC50 7.94 7.94 11.4 1
Histone deacetylase 4
CHEMBL3524
IC50 5.52 5.52 3000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Histone deacetylase 1 IC50 = 11.4 nM 7.94 Inhibition of HDAC1 (unknown origin) 30245394
Histone deacetylase 4 IC50 = 3000.0 nM 5.52 Inhibition of HDAC4 (unknown origin) 30245394

Literature References

PubMed DOI Target Context # Activities
30245394 10.1016/j.ejmech.2018.08.073 Histone deacetylase 1 1
30245394 10.1016/j.ejmech.2018.08.073 Histone deacetylase 4 1

Data from ChEMBL 36 via Core Engine