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Compound Detail

CHEMBL2417784

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Cc1onc(-c2ccccc2)c1C(=O)NCCCCCNC(=O)[C@@H](C)S

Basic Information

ChEMBL ID CHEMBL2417784
Phase Preclinical
Structure Type MOL
InChI Key IMIDYBQMXWFUIG-CQSZACIVSA-N
3
Targets
4
Activities
1
Assay Types
0
PK Parameters
11
Publications
0
Known Names

Molecular Properties

375.5
MW (Da)
2.98
ALogP
5
HBA
3
HBD
84.2
PSA (Ų)
0.46
QED
0
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C19H25N3O3S
MW 375.49
Aromatic Rings 2
Heavy Atoms 26
NP-Likeness -1.03

Activity Summary

IC50 4 meas. best 6.55

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histone deacetylase 6
CHEMBL1865
IC50 6.55 6.55 280.0 2
Histone deacetylase 3
CHEMBL1829
IC50 4.82 4.82 15000.0 1
Histone deacetylase 3/Nuclear receptor corepressor 2 (HDAC3/NCoR2)
CHEMBL2111363
IC50 4.82 4.82 15000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
23627282 10.1021/jm4001659 Histone deacetylase 4 1
23627282 10.1021/jm4001659 Histone deacetylase 6 1
23627282 10.1021/jm4001659 Histone deacetylase 5 1
23627282 10.1021/jm4001659 Histone deacetylase 3 1
23627282 10.1021/jm4001659 Histone deacetylase 2 1
23627282 10.1021/jm4001659 Histone deacetylase 1 1
33035922 10.1016/j.ejmech.2020.112887 Histone deacetylase 1 1
33035922 10.1016/j.ejmech.2020.112887 Histone deacetylase 2 1
33035922 10.1016/j.ejmech.2020.112887 Histone deacetylase 3/Nuclear receptor corepressor 2 (HDAC3/NCoR2) 1
33035922 10.1016/j.ejmech.2020.112887 Histone deacetylase 6 1
33035922 10.1016/j.ejmech.2020.112887 Unchecked 1

Data from ChEMBL 36 via Core Engine