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Compound Detail

CHEMBL4207409

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CCCc1nn(C)c2c(=O)[nH]c(-c3cc(C4=CCC(C(=O)NO)CC4)ccc3OCC)nc12

Basic Information

ChEMBL ID CHEMBL4207409
Phase Preclinical
Structure Type MOL
InChI Key DRHPBWLHHFRCIG-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

451.5
MW (Da)
3.36
ALogP
7
HBA
3
HBD
122.1
PSA (Ų)
0.37
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H29N5O4
MW 451.53
Aromatic Rings 3
Heavy Atoms 33
NP-Likeness -0.44

Activity Summary

IC50 3 meas. best 7.57

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
cGMP-specific 3',5'-cyclic phosphodiesterase
CHEMBL1827
IC50 7.57 7.57 27.0 1
Histone deacetylase 6
CHEMBL1865
IC50 6.47 6.47 340.0 1
Histone deacetylase 1
CHEMBL325
IC50 5.54 5.54 2880.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
29549837 10.1016/j.ejmech.2018.03.005 Histone deacetylase 1 1
29549837 10.1016/j.ejmech.2018.03.005 Histone deacetylase 2 1
29549837 10.1016/j.ejmech.2018.03.005 Histone deacetylase 6 1
29549837 10.1016/j.ejmech.2018.03.005 cGMP-specific 3',5'-cyclic phosphodiesterase 1

Data from ChEMBL 36 via Core Engine