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Compound Detail

CHEMBL3907730

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CCCc1nn(C)c2c(=O)[nH]c(-c3cc(NC4CCN(c5ncc(C(=O)NO)cn5)CC4)ccc3OCC)nc12

Basic Information

ChEMBL ID CHEMBL3907730
Phase Preclinical
Structure Type MOL
InChI Key HHVZIHMMVKGUNH-UHFFFAOYSA-N
5
Targets
5
Activities
1
Assay Types
0
PK Parameters
9
Publications
0
Known Names

Molecular Properties

547.6
MW (Da)
2.66
ALogP
11
HBA
4
HBD
163.2
PSA (Ų)
0.18
QED
2
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H33N9O4
MW 547.62
Aromatic Rings 4
Heavy Atoms 40
NP-Likeness -1.37

Activity Summary

IC50 5 meas. best 8.3

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
cGMP-specific 3',5'-cyclic phosphodiesterase
CHEMBL1827
IC50 8.3 8.3 5.0 1
Histone deacetylase 3/Nuclear receptor corepressor 2 (HDAC3/NCoR2)
CHEMBL2111363
IC50 7.51 7.51 31.0 1
Histone deacetylase 1
CHEMBL325
IC50 7.17 7.17 68.0 1
Histone deacetylase 6
CHEMBL1865
IC50 6.36 6.36 441.0 1
Histone deacetylase 2
CHEMBL1937
IC50 6.31 6.31 490.0 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 Histone deacetylase 3/Nuclear receptor corepressor 2 (HDAC3/NCoR2) 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