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Compound Detail

CHEMBL466032

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O=C(CCCCc1cc(C(=O)O)no1)Nc1nc(-c2ccccc2)cs1

Basic Information

ChEMBL ID CHEMBL466032
Phase Preclinical
Structure Type MOL
InChI Key DZGAESNTKKTHRY-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
9
Publications
0
Known Names

Molecular Properties

371.4
MW (Da)
3.85
ALogP
6
HBA
2
HBD
105.3
PSA (Ų)
0.58
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C18H17N3O4S
MW 371.42
Aromatic Rings 3
Heavy Atoms 26
NP-Likeness -1.66

Activity Summary

IC50 1 meas. best 4.97

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histone deacetylase 3
CHEMBL1829
IC50 4.97 4.97 10600.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Histone deacetylase 3 IC50 = 10600.0 nM 4.97 Inhibition of human recombinant HDAC3 19419863

Literature References

PubMed DOI Target Context # Activities
19419863 10.1016/j.bmcl.2009.04.058 NON-PROTEIN TARGET 2
19419863 10.1016/j.bmcl.2009.04.058 Histone deacetylase 1 1
19419863 10.1016/j.bmcl.2009.04.058 Histone deacetylase 3 1
19419863 10.1016/j.bmcl.2009.04.058 Histone deacetylase 6 1
19419863 10.1016/j.bmcl.2009.04.058 Histone deacetylase 2 1
19419863 10.1016/j.bmcl.2009.04.058 Polyamine deacetylase HDAC10 1
19419863 10.1016/j.bmcl.2009.04.058 BXPC-3 1
19419863 10.1016/j.bmcl.2009.04.058 HuP-T3 1
19419863 10.1016/j.bmcl.2009.04.058 MIA PaCa-2 1

Data from ChEMBL 36 via Core Engine