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Compound Detail

CHEMBL385550

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COC(=O)CCCCC[C@H](NC(=O)Cc1c(C)[nH]c2ccc(OC)cc12)C(=O)NCCc1c(-c2ccccc2)[nH]c2ccccc12

Basic Information

ChEMBL ID CHEMBL385550
Phase Preclinical
Structure Type MOL
InChI Key WBURJDQDBKPXRR-XIFFEERXSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

622.8
MW (Da)
6.14
ALogP
5
HBA
4
HBD
125.3
PSA (Ų)
0.08
QED
2
Ro5 Violations
15
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C37H42N4O5
MW 622.77
Aromatic Rings 5
Heavy Atoms 46
NP-Likeness -0.38

Activity Summary

IC50 2 meas. best 6.82

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histone deacetylase 1
CHEMBL325
IC50 6.82 6.82 150.0 1
HeLa
CHEMBL399
IC50 5.89 5.89 1300.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Histone deacetylase 1 IC50 = 150.0 nM 6.82 Inhibition of HDAC1 (mean IC50) 16987657
HeLa IC50 = 1300.0 nM 5.89 Inhibition of HeLa cell proliferation 16987657

Literature References

PubMed DOI Target Context # Activities
16987657 10.1016/j.bmcl.2006.09.002 Histone deacetylase 1 1
16987657 10.1016/j.bmcl.2006.09.002 HeLa 1

Data from ChEMBL 36 via Core Engine