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Compound Detail

CHEMBL3956031

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CCOc1ccc(-c2ccc(C(=O)NO)nc2)cc1-c1nc2c(CC)nn(C)c2c(=O)[nH]1

Basic Information

ChEMBL ID CHEMBL3956031
Phase Preclinical
Structure Type MOL
InChI Key PLORDXSOTXFDIZ-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

434.5
MW (Da)
2.47
ALogP
8
HBA
3
HBD
135.0
PSA (Ų)
0.31
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H22N6O4
MW 434.46
Aromatic Rings 4
Heavy Atoms 32
NP-Likeness -1.02

Activity Summary

IC50 3 meas. best 8.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
cGMP-specific 3',5'-cyclic phosphodiesterase
CHEMBL1827
IC50 8.4 8.4 4.0 1
Histone deacetylase 6
CHEMBL1865
IC50 6.07 6.07 861.0 1
Histone deacetylase 1
CHEMBL325
IC50 5.63 5.63 2360.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
27606546 10.1021/acs.jmedchem.6b00908 NON-PROTEIN TARGET 6
27606546 10.1021/acs.jmedchem.6b00908 Histone deacetylase 6 5
27606546 10.1021/acs.jmedchem.6b00908 cGMP-specific 3',5'-cyclic phosphodiesterase 3
27606546 10.1021/acs.jmedchem.6b00908 Histone deacetylase 1 1
27606546 10.1021/acs.jmedchem.6b00908 Histone deacetylase 2 1
27606546 10.1021/acs.jmedchem.6b00908 Mus musculus 1
27606546 10.1021/acs.jmedchem.6b00908 ADMET 1

Data from ChEMBL 36 via Core Engine