Target
Retinal rod rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit gamma
Ligand
BDBM14395
Substrate
BDBM14391
Meas. Tech.
PDE Enzyme Inhibitor Assays
pH
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, CMBarber, CGBeaumont, KCBrown, DGCole, SMEllis, DLane, CAMaw, GNMount, NMRawson, DJRobinson, CMStreet, SDSummerhill, NW A novel series of potent and selective PDE5 inhibitors with potential for high and dose-independent oral bioavailability. J Med Chem 49:3581-94 (2006) [PubMed]  Article 
Target
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:
MNLEPPKAEIRSATRVIGGPVTPRKGPPKFKQRQTRQFKSKPPKKGVQGFGDDIPGMEGLGTDITVICPWEAFNHLELHELAQYGII
  
Inhibitor
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:
Search PDB for entries with ligand similarity:
Substrate
Name:
BDBM14391
Synonyms:
2-amino-9-[(4aR,6R,7R,7aS)-2,7-dihydroxy-2-oxidotetrahydro-4H-furo[3,2-d][1,3,2]dioxaphosphinin-6-yl]-1,9-dihydro-6H-purin-6-one | 9-[(4aR,6R,7R,7aS)-2,7-dihydroxy-2-oxo-hexahydro-1,3,5,2-furo[3,2-d][1,3,2]dioxaphosphinin-6-yl]-2-amino-6,9-dihydro-1H-purin-6-one | GUANOSINE-3 ,5 -MONOPHOSPHATE | US11701371, Compound cGMP | cGMP
Type:
Nucleoside or nucleotide
Emp. Form.:
C10H12N5O7P
Mol. Mass.:
345.2053
SMILES:
Nc1nc2n(cnc2c(=O)[nH]1)[C@@H]1O[C@@H]2COP(O)(=O)O[C@H]2[C@H]1O
Structure:
Search PDB for entries with ligand similarity: