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Compound Detail

CHEMBL5274737

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COc1cc(/C=C2\N=C(c3ccccc3)N(n3c(SCC(=O)NO)nnc3-c3ccccc3)C2=O)ccc1O

Basic Information

ChEMBL ID CHEMBL5274737
Phase Preclinical
Structure Type MOL
InChI Key VZELXGGTHYOEFP-ZHZULCJRSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

542.6
MW (Da)
3.22
ALogP
10
HBA
3
HBD
142.2
PSA (Ų)
0.13
QED
1
Ro5 Violations
8
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H22N6O5S
MW 542.58
Aromatic Rings 4
Heavy Atoms 39
NP-Likeness -0.90

Activity Summary

IC50 1 meas. best 7.05

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histone deacetylase
CHEMBL2093865
IC50 7.05 7.05 90.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Histone deacetylase IC50 = 90.0 nM 7.05 Inhibition of HDAC (unknown origin) 32791404

Literature References

PubMed DOI Target Context # Activities
32791404 10.1016/j.ejmech.2020.112679 MCF7 1
32791404 10.1016/j.ejmech.2020.112679 Histone deacetylase 1

Data from ChEMBL 36 via Core Engine