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Compound Detail

CHEMBL567255

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CCCOCCn1c(=O)c(NCCO)nc2ncc(-c3ccc(OC)nc3)cc21

Basic Information

ChEMBL ID CHEMBL567255
Phase Preclinical
Structure Type MOL
InChI Key MKUXZEJAFDMNDG-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
2
PK Parameters
4
Publications
0
Known Names

Molecular Properties

399.4
MW (Da)
1.69
ALogP
9
HBA
2
HBD
111.4
PSA (Ų)
0.50
QED
0
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H25N5O4
MW 399.45
Aromatic Rings 3
Heavy Atoms 29
NP-Likeness -1.38

Activity Summary

IC50 2 meas. best 8.93

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
cGMP-specific 3',5'-cyclic phosphodiesterase
CHEMBL1827
IC50 8.93 8.93 1.2 1
Rod cGMP-specific 3',5'-cyclic phosphodiesterase subunit alpha
CHEMBL3878
IC50 6.94 6.94 114.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL - - Rattus norvegicus
F - % Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
19631533 10.1016/j.bmcl.2009.07.019 Rattus norvegicus 3
19631533 10.1016/j.bmcl.2009.07.019 cGMP-specific 3',5'-cyclic phosphodiesterase 1
19631533 10.1016/j.bmcl.2009.07.019 Rod cGMP-specific 3',5'-cyclic phosphodiesterase subunit alpha 1
19631533 10.1016/j.bmcl.2009.07.019 Unchecked 1

Data from ChEMBL 36 via Core Engine