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Compound Detail

CHEMBL235300

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CC(=O)SCC/C=C/[C@@H]1CC(=O)N[C@H](C)C(=O)N[C@H](C)C(=O)N[C@H](C(C)C)C(=O)NCC(=O)O1

Basic Information

ChEMBL ID CHEMBL235300
Phase Preclinical
Structure Type MOL
InChI Key DSOSPBZVBBLRHS-MGYDIJNBSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

498.6
MW (Da)
-0.21
ALogP
8
HBA
4
HBD
159.8
PSA (Ų)
0.23
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H34N4O7S
MW 498.60
Aromatic Rings 0
Heavy Atoms 34
NP-Likeness 1.89

Activity Summary

IC50 2 meas. best 7.26

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
MCF7
CHEMBL387
IC50 7.26 7.26 55.0 1
Histone deacetylase
CHEMBL2093865
IC50 6.62 6.62 242.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
MCF7 IC50 = 55.0 nM 7.26 Growth inhibition of MCF7 cells 17958342
Histone deacetylase IC50 = 242.0 nM 6.62 Inhibition of HDAC in HeLa nuclear extract in presence of DTT 17958342

Literature References

PubMed DOI Target Context # Activities
17958342 10.1021/jm0703800 MCF7 1
17958342 10.1021/jm0703800 Histone deacetylase 1
17958342 10.1021/jm0703800 Histone deacetylase 1 1
17958342 10.1021/jm0703800 Histone deacetylase 6 1

Data from ChEMBL 36 via Core Engine