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Compound Detail

CHEMBL130612

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COc1ccc(-c2cnc(N3Cc4c(nc5ccccc5c4O)C3c3ccc(OC)c(OC)c3)nc2)cc1OC

Basic Information

ChEMBL ID CHEMBL130612
Phase Preclinical
Structure Type MOL
InChI Key PFSAOBZGNQDTPJ-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

536.6
MW (Da)
5.54
ALogP
9
HBA
1
HBD
99.1
PSA (Ų)
0.29
QED
2
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C31H28N4O5
MW 536.59
Aromatic Rings 5
Heavy Atoms 40
NP-Likeness -0.24

Activity Summary

Ki 1 meas. best 7.61

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
cGMP-specific 3',5'-cyclic phosphodiesterase
CHEMBL1827
Ki 7.61 7.61 24.7 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
cGMP-specific 3',5'-cyclic phosphodiesterase Ki = 24.7 nM 7.61 Phosphodiesterase 5 activity of human corpus cavernosum 12213052

Literature References

PubMed DOI Target Context # Activities
12213052 10.1021/jm025545d cGMP-specific 3',5'-cyclic phosphodiesterase 1

Data from ChEMBL 36 via Core Engine