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Compound Detail

CHEMBL270740

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O=C(CCCCCC(=O)N(CC(=O)Nc1ccccc1)CC(=O)Nc1cccc2cccnc12)NO

Basic Information

ChEMBL ID CHEMBL270740
Phase Preclinical
Structure Type MOL
InChI Key WJVHKXOFLRSFFU-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

491.6
MW (Da)
3.10
ALogP
6
HBA
4
HBD
140.7
PSA (Ų)
0.17
QED
0
Ro5 Violations
12
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H29N5O5
MW 491.55
Aromatic Rings 3
Heavy Atoms 36
NP-Likeness -1.19

Activity Summary

IC50 2 meas. best 7.6

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histone deacetylase 1
CHEMBL325
IC50 7.6 7.6 25.0 1
Unchecked
CHEMBL612545
IC50 4.34 4.34 46000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Histone deacetylase 1 IC50 = 25.0 nM 7.6 Inhibition of human HDAC1 18247554
Unchecked IC50 = 46000.0 nM 4.34 Inhibition of mouse SC9 cells 18247554

Literature References

PubMed DOI Target Context # Activities
18247554 10.1021/jm7011408 Histone deacetylase 1 1
18247554 10.1021/jm7011408 Unchecked 1

Data from ChEMBL 36 via Core Engine