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Compound Detail

CHEMBL3901988

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CCOc1ccc(C2CC(C(=O)NO)C2)cc1-c1nc2c(CC)nn(C)c2c(=O)[nH]1

Basic Information

ChEMBL ID CHEMBL3901988
Phase Preclinical
Structure Type MOL
InChI Key XHOQZHUIEYFPGU-UHFFFAOYSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

411.5
MW (Da)
2.28
ALogP
7
HBA
3
HBD
122.1
PSA (Ų)
0.42
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 C21H25N5O4
MW 411.46
Aromatic Rings 3
Heavy Atoms 30
NP-Likeness -0.65

Activity Summary

IC50 4 meas. best 7.77

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
cGMP-specific 3',5'-cyclic phosphodiesterase
CHEMBL1827
IC50 7.77 7.77 17.0 1
Histone deacetylase 6
CHEMBL1865
IC50 6.89 6.89 130.0 1
Histone deacetylase 1
CHEMBL325
IC50 6.26 6.26 554.0 1
Histone deacetylase 2
CHEMBL1937
IC50 5.73 5.73 1860.0 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 Unchecked 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