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Compound Detail

CHEMBL214877

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O=C(CCSc1nc(O)cc(CCc2ccccc2)n1)NO

Basic Information

ChEMBL ID CHEMBL214877
Phase Preclinical
Structure Type MOL
InChI Key QRAKIBWWWHOJPB-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

319.4
MW (Da)
1.96
ALogP
6
HBA
3
HBD
95.3
PSA (Ų)
0.31
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C15H17N3O3S
MW 319.39
Aromatic Rings 2
Heavy Atoms 22
NP-Likeness -1.31

Activity Summary

IC50 3 meas. best 7.64

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
IC50 7.64 7.64 23.0 1
Histone deacetylase HD2
CHEMBL4919
IC50 7.43 7.43 37.0 1
Histone deacetylase HD1B
CHEMBL3541
IC50 7.22 7.22 60.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked IC50 = 23.0 nM 7.64 Inhibition of maize HD1A 17004718
Histone deacetylase HD2 IC50 = 37.0 nM 7.43 Inhibition of maize HD2 17004718
Histone deacetylase HD1B IC50 = 60.0 nM 7.22 Inhibition of maize HD1B 17004718

Literature References

PubMed DOI Target Context # Activities
17004718 10.1021/jm0605536 Histone deacetylase HD2 1
17004718 10.1021/jm0605536 Unchecked 1
17004718 10.1021/jm0605536 Histone deacetylase HD1B 1

Data from ChEMBL 36 via Core Engine