Ki Summary

Reaction Details

Report a problem with these data

Target

Retinal rod rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit gamma

Ligand

BDBM14395

Substrate/Competitor

BDBM14391

Meas. Tech.

PDE Enzyme Inhibitor Assays

7.4±n/a

Temperature

303.15±n/a K

IC50

>3000±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:

Type:

Enzyme

Mol. Mass.:

9656.12

Organism:

Canis lupus familiaris (Dog)

Description:

n/a

Residue:

Sequence:

MNLEPPKAEIRSATRVIGGPVTPRKGPPKFKQRQTRQFKSKPPKKGVQGFGDDIPGMEGL
GTDITVICPWEAFNHLELHELAQYGII

BDBM14395

BDBM14391

Name

BDBM14395

Synonyms:

5-[2-Butoxy-5-(1-hydroxyethyl)-3-pyridinyl]-3-ethyl-2-(1-ethyl-3-azetidinyl) -2,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one | 5-[2-butoxy-5-(1-hydroxyethyl)pyridin-3-yl]-3-ethyl-2-(1-ethylazetidin-3-yl)-2H,6H,7H-pyrazolo[4,3-d]pyrimidin-7-one | Sildenafil 5-methyl alcohol analogue 55

Type

Small organic molecule

Emp. Form.

C23H32N6O3

Mol. Mass.

440.5386

SMILES

CCCCOc1ncc(cc1-c1nc2c(CC)n(nc2c(=O)[nH]1)C1CN(CC)C1)C(C)O

Structure