Reaction Details |
| Report a problem with these data |
Target | Retinal rod rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit gamma |
---|
Ligand | BDBM14394 |
---|
Substrate/Competitor | BDBM14391 |
---|
Meas. Tech. | PDE Enzyme Inhibitor Assays |
---|
pH | 7.4±n/a |
---|
Temperature | 303.15±n/a K |
---|
IC50 | 183±n/a nM |
---|
Comments | cGMP in a 3:1 ratio unlabeled to 3H-labeled at a concentration 1/3Km, such that IC50 = Ki. |
---|
Citation | Allerton, CM; Barber, CG; Beaumont, KC; Brown, DG; Cole, SM; Ellis, D; Lane, CA; Maw, GN; Mount, NM; Rawson, DJ; Robinson, CM; Street, SD; Summerhill, NW A novel series of potent and selective PDE5 inhibitors with potential for high and dose-independent oral bioavailability. J Med Chem49:3581-94 (2006) [PubMed] Article |
---|
More Info.: | Get all data from this article, Solution Info, Assay Method |
---|
|
Retinal rod rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit gamma |
---|
Name: | Retinal rod rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit gamma |
Synonyms: | CNRG_CANLF | GMP-PDE gamma | PDE6G | PDEG | Phosphodiesterase Type 6 (PDE6) | Retinal rod rhodopsin-sensitive cGMP 3 ,5 -cyclic phosphodiesterase subunit gamma |
Type: | Enzyme |
Mol. Mass.: | 9656.12 |
Organism: | Canis lupus familiaris (Dog) |
Description: | n/a |
Residue: | 87 |
Sequence: | MNLEPPKAEIRSATRVIGGPVTPRKGPPKFKQRQTRQFKSKPPKKGVQGFGDDIPGMEGL
GTDITVICPWEAFNHLELHELAQYGII
|
|
|
BDBM14394 |
---|
BDBM14391 |
---|
Name | BDBM14394 |
Synonyms: | 5-(2-butoxy-5-acetylpyridin-3-yl)-3-ethyl-2-(pyridin-2-ylmethyl)-2H,6H,7H-pyrazolo[4,3-d]pyrimidin-7-one | 5-(5-Acetyl-2-butoxy-3-pyridinyl)-3-ethyl-2-(2-pyridinylmethyl)-2,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one | Sildenafil 5-methyl ketone analogue 9 |
Type | Small organic molecule |
Emp. Form. | C24H26N6O3 |
Mol. Mass. | 446.5016 |
SMILES | CCCCOc1ncc(cc1-c1nc2c(CC)n(Cc3ccccn3)nc2c(=O)[nH]1)C(C)=O |
Structure |
|