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Compound Detail

CHEMBL4789481

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Cc1cc2cc(NS(=O)(=O)c3ccc(C(=O)NO)cc3)ccc2n(C)c1=O

Basic Information

ChEMBL ID CHEMBL4789481
Phase Preclinical
Structure Type MOL
InChI Key AXJXDWNCHLEVAZ-UHFFFAOYSA-N
4
Targets
4
Activities
2
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

387.4
MW (Da)
1.77
ALogP
6
HBA
3
HBD
117.5
PSA (Ų)
0.47
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C18H17N3O5S
MW 387.42
Aromatic Rings 3
Heavy Atoms 27
NP-Likeness -1.26

Activity Summary

IC50 3 meas. best 6.46
Kd 1 meas. best 6.76

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Peregrin
CHEMBL3132741
Kd 6.76 6.76 175.2 1
Histone deacetylase 6
CHEMBL1865
IC50 6.46 6.46 344.0 1
Histone deacetylase 1
CHEMBL325
IC50 6.1 6.1 797.0 1
Histone deacetylase 8
CHEMBL3192
IC50 6.04 6.04 908.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

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

Data from ChEMBL 36 via Core Engine