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Compound Detail

CHEMBL3403373

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CCn1c(NC(C)C)nc2c(C3CCN(C(=O)c4ncccc4C)C3)csc2c1=O

Basic Information

ChEMBL ID CHEMBL3403373
Phase Preclinical
Structure Type MOL
InChI Key JUDJZYCORAYMNM-UHFFFAOYSA-N
5
Targets
5
Activities
1
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

425.6
MW (Da)
3.63
ALogP
7
HBA
1
HBD
80.1
PSA (Ų)
0.68
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H27N5O2S
MW 425.56
Aromatic Rings 3
Heavy Atoms 30
NP-Likeness -1.64

Activity Summary

IC50 5 meas. best 8.85

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
High affinity 3',5'-cyclic-AMP phosphodiesterase 7A
CHEMBL3012
IC50 8.85 8.85 1.4 1
3',5'-cyclic-AMP phosphodiesterase 4B
CHEMBL275
IC50 6.85 6.85 140.0 1
Lymphocyte
CHEMBL612599
IC50 6.57 6.57 270.0 1
cGMP-inhibited 3',5'-cyclic phosphodiesterase 3A
CHEMBL241
IC50 5.89 5.89 1300.0 1
cGMP-specific 3',5'-cyclic phosphodiesterase
CHEMBL1827
IC50 5.51 5.51 3100.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
25866242 10.1016/j.bmcl.2015.03.031 Mus musculus 2
25866242 10.1016/j.bmcl.2015.03.031 High affinity 3',5'-cyclic-AMP phosphodiesterase 7A 1
25866242 10.1016/j.bmcl.2015.03.031 3',5'-cyclic-AMP phosphodiesterase 4B 1
25866242 10.1016/j.bmcl.2015.03.031 No relevant target 1
25866242 10.1016/j.bmcl.2015.03.031 cGMP-inhibited 3',5'-cyclic phosphodiesterase 3A 1
25866242 10.1016/j.bmcl.2015.03.031 cGMP-specific 3',5'-cyclic phosphodiesterase 1
25866242 10.1016/j.bmcl.2015.03.031 Lymphocyte 1

Data from ChEMBL 36 via Core Engine