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Compound Detail

CHEMBL398079

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Cc1cccc(N2CC(=O)N3[C@H](c4ccc5c(c4)OCO5)c4[nH]c5ccccc5c4C[C@@H]3C2=O)c1

Basic Information

ChEMBL ID CHEMBL398079
Phase Preclinical
Structure Type MOL
InChI Key TXDZREWVVHXUGK-AJTFRIOCSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

465.5
MW (Da)
4.09
ALogP
4
HBA
1
HBD
74.9
PSA (Ų)
0.48
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H23N3O4
MW 465.51
Aromatic Rings 4
Heavy Atoms 35
NP-Likeness -0.52

Activity Summary

IC50 1 meas. best 7.17

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
cGMP-specific 3',5'-cyclic phosphodiesterase
CHEMBL3478
IC50 7.17 7.17 68.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
cGMP-specific 3',5'-cyclic phosphodiesterase IC50 = 68.0 nM 7.17 Inhibition of bovine PDE5 after 24 hrs by HTRF 17107795

Literature References

PubMed DOI Target Context # Activities
17107795 10.1016/j.bmcl.2006.10.069 cGMP-specific 3',5'-cyclic phosphodiesterase 1
21504142 10.1021/jm1014617 Plasmodium falciparum 1
21504142 10.1021/jm1014617 MRC5 1

Data from ChEMBL 36 via Core Engine