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Compound Detail

CHEMBL560516

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CCCOCCn1c(=O)c(NCCN2CCOCC2)nc2ccc(-c3ccc(OC)nc3)cc21

Basic Information

ChEMBL ID CHEMBL560516
Phase Preclinical
Structure Type MOL
InChI Key USFVOQOJWOHVLK-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

467.6
MW (Da)
2.64
ALogP
9
HBA
1
HBD
90.7
PSA (Ų)
0.43
QED
0
Ro5 Violations
11
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H33N5O4
MW 467.57
Aromatic Rings 3
Heavy Atoms 34
NP-Likeness -1.80

Activity Summary

IC50 2 meas. best 9.05

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
cGMP-specific 3',5'-cyclic phosphodiesterase
CHEMBL1827
IC50 9.05 9.05 0.9 1
Unchecked
CHEMBL612545
IC50 6.75 6.75 177.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
cGMP-specific 3',5'-cyclic phosphodiesterase IC50 = 0.9 nM 9.05 Inhibition of PDE5 19539468
Unchecked IC50 = 177.0 nM 6.75 Inhibition of PDE6 19539468

Literature References

PubMed DOI Target Context # Activities
19539468 10.1016/j.bmcl.2009.06.004 Unchecked 2
19539468 10.1016/j.bmcl.2009.06.004 cGMP-specific 3',5'-cyclic phosphodiesterase 1
19539468 10.1016/j.bmcl.2009.06.004 Voltage-gated inwardly rectifying potassium channel KCNH2 1
19539468 10.1016/j.bmcl.2009.06.004 Hepatocyte 1

Data from ChEMBL 36 via Core Engine