Ki Summary

Reaction Details

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Target

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

Ligand

BDBM14392

Substrate/Competitor

BDBM14391

Meas. Tech.

PDE Enzyme Inhibitor Assays

7.4±n/a

Temperature

303.15±n/a K

IC50

386±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

BDBM14392

BDBM14391

Name

BDBM14392

Synonyms:

3-ethyl-5-{5-[(4-ethylpiperazine-1-)sulfonyl]-2-(2-methoxyethoxy)pyridin-3-yl}-2-(pyridin-2-ylmethyl)-2H,6H,7H-pyrazolo[4,3-d]pyrimidin-7-one | CHEMBL209157 | Sildenafil Pyridyl Methyl Analogue 1

Type

Small organic molecule

Emp. Form.

C27H34N8O5S

Mol. Mass.

582.674

SMILES

CCN1CCN(CC1)S(=O)(=O)c1cnc(OCCOC)c(c1)-c1nc2c(CC)n(Cc3ccccn3)nc2c(=O)[nH]1

Structure