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Compound Detail

CHEMBL245611

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O=C1[C@H]2Cc3c([nH]c4ccccc34)[C@@H](c3ccc4c(c3)OCO4)N2C(=O)CN1c1ccccc1

Basic Information

ChEMBL ID CHEMBL245611
Phase Preclinical
Structure Type MOL
InChI Key SXIATEZTQQHWRD-QFQXNSOFSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

451.5
MW (Da)
3.79
ALogP
4
HBA
1
HBD
74.9
PSA (Ų)
0.50
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 C27H21N3O4
MW 451.48
Aromatic Rings 4
Heavy Atoms 34
NP-Likeness -0.34

Activity Summary

IC50 1 meas. best 7.04

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
cGMP-specific 3',5'-cyclic phosphodiesterase
CHEMBL3478
IC50 7.04 7.04 91.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
cGMP-specific 3',5'-cyclic phosphodiesterase IC50 = 91.0 nM 7.04 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
17107795 10.1016/j.bmcl.2006.10.069 No relevant target 1
21504142 10.1021/jm1014617 Plasmodium falciparum 1
21504142 10.1021/jm1014617 MRC5 1

Data from ChEMBL 36 via Core Engine