PF-4181366 |
Inhibitor of PDE9A
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
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Probe Summary
| Targets | Biochemical/Biophysical Potency | Cellular Potency |
|---|---|---|
| PDE9A |
|
Inhibitor
--
Selectivity
In Vitro Selectivity Assessment
PDE1C
Gene ID: Q14123
Organism: Homo sapiens
Family: cyclic nucleotide phosphodiesterase family
Potency: IC50 - 50 nM
Potency Assay Off-Target:
Enzymatic assay using recombinant proteins
Selectivity Assessment Description:
PDE2 >1000 nM;
PDE3A >1000 nM;
PDE4C >1000 nM;
PDE5 349 nM;
PDE6 127 nM;
PDE7B >1000 nM;
PDE8B >1000 ...
Potency Cellular
In Vitro
PDE9A
Mode of Action: Inhibitor
Structure-Activity-Relationship data available? No
DOI Reference: 10.1021/jm9015334
In Vivo Validations
Rat
Dose: 10 mg/kg
Route of delivery:
Subcutaneous
Organ of interest (O):
Brain
Target engagement assay:
PF-4181366 elevated cGMP in the striatum of mice in a dose responsive fashion. A 145% elevation occurred at 3.2 mg/kg, and at 10 mg/kg a 215% elevation was observed.
Reference: --
Chemical Information
| Molecular Formula | C24H27N7O |
| SMILEs | C[C@@H]1CN(Cc2ccc3nccnc3c2)C[C@H]1c1nc2c(cnn2C2CCCC2)c(=O)[nH]1 |
| InChI | InChI=1S/C24H27N7O/c1-15-12-30(13-16-6-7-20-21(10-16)26-9-8-25-20)14-19(15)22-28-23-18(24(32)29-22)11-27-31(23)17-4-2-3-5-17/h6-11,15,17,19H,2-5,12-14H2,1H3,(H,28,29,32)/t15-,19-/m1/s1 |
| Molecular weight | 429.23 Da |
| AlogP | 0.0 |
| HBond acceptors | 8 |
| HBond donors | 1 |
| Atoms | 59 |