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Compound Detail

CHEMBL4786752

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Cc1cc2cc(NS(=O)(=O)Cc3cccc(C(=O)NO)c3)ccc2n(C)c1=O

Basic Information

ChEMBL ID CHEMBL4786752
Phase Preclinical
Structure Type MOL
InChI Key XJZLKGFNNBJERU-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

401.4
MW (Da)
1.91
ALogP
6
HBA
3
HBD
117.5
PSA (Ų)
0.45
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C19H19N3O5S
MW 401.44
Aromatic Rings 3
Heavy Atoms 28
NP-Likeness -1.37

Activity Summary

IC50 1 meas. best 6.33

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histone deacetylase 8
CHEMBL3192
IC50 6.33 6.33 465.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Histone deacetylase 8 IC50 = 465.0 nM 6.33 Inhibition of human recombinant HDAC8 using H2N-Arg-His-Lys(Ac)-Lys(Ac)-AMC as s... 32497960

Literature References

PubMed DOI Target Context # Activities
32497960 10.1016/j.ejmech.2020.112338 THP-1 3
32497960 10.1016/j.ejmech.2020.112338 HL-60 3
32497960 10.1016/j.ejmech.2020.112338 Histone deacetylase 1 2
32497960 10.1016/j.ejmech.2020.112338 Histone deacetylase 6 2
32497960 10.1016/j.ejmech.2020.112338 Histone deacetylase 8 1

Data from ChEMBL 36 via Core Engine