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Compound Detail

CHEMBL127351

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O=C(CCCCCCOc1cccc(-c2ccccc2)c1)c1ncco1

Basic Information

ChEMBL ID CHEMBL127351
Phase Preclinical
Structure Type MOL
InChI Key HWZHDGRMABBYOV-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
1
PK Parameters
3
Publications
0
Known Names

Molecular Properties

349.4
MW (Da)
5.55
ALogP
4
HBA
0
HBD
52.3
PSA (Ų)
0.36
QED
1
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H23NO3
MW 349.43
Aromatic Rings 3
Heavy Atoms 26
NP-Likeness -0.43

Activity Summary

IC50 2 meas. best 6.21

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histone deacetylase
CHEMBL2093865
IC50 6.21 6.21 620.0 1
Unchecked
CHEMBL612545
IC50 6.21 6.21 620.0 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 0.21 hr -

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Histone deacetylase IC50 = 620.0 nM 6.21 In vitro inhibition of Histone deacetylase in K 562 erythroleukemia cells. 14592473
Unchecked IC50 = 620.0 nM 6.21 Inhibition of HDAC 18053726

Literature References

PubMed DOI Target Context # Activities
14592473 10.1016/j.bmcl.2003.09.007 Histone deacetylase 1
14592473 10.1016/j.bmcl.2003.09.007 ADMET 1
18053726 10.1016/j.bmc.2007.11.015 Unchecked 1

Data from ChEMBL 36 via Core Engine