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Compound Detail

CHEMBL520074

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C=CCc1c(OC)c(NC(=O)CC)cc2c(NCc3ccc(OC)c(Cl)c3)ncnc12

Basic Information

ChEMBL ID CHEMBL520074
Phase Preclinical
Structure Type MOL
InChI Key RZNXAUVMTXWAMP-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

440.9
MW (Da)
4.99
ALogP
6
HBA
2
HBD
85.4
PSA (Ų)
0.46
QED
0
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H25ClN4O3
MW 440.93
Aromatic Rings 3
Heavy Atoms 31
NP-Likeness -0.99

Activity Summary

IC50 3 meas. best 7.75

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
cGMP-specific 3',5'-cyclic phosphodiesterase
CHEMBL3478
IC50 7.75 7.75 18.0 1
Unchecked
CHEMBL612545
IC50 6.1 6.1 790.0 1
Dual 3',5'-cyclic-AMP and -GMP phosphodiesterase 11A
CHEMBL2717
IC50 5.11 5.11 7800.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
18976905 10.1016/j.bmcl.2008.09.108 cGMP-specific 3',5'-cyclic phosphodiesterase 1
18976905 10.1016/j.bmcl.2008.09.108 Unchecked 1
18976905 10.1016/j.bmcl.2008.09.108 Dual 3',5'-cyclic-AMP and -GMP phosphodiesterase 11A 1

Data from ChEMBL 36 via Core Engine