Target
cGMP-specific 3',5'-cyclic phosphodiesterase [535-860]
Ligand
BDBM14390
Substrate
BDBM14391
Meas. Tech.
Enzymatic Assay
pH
7.8±n/a
Temperature
297.15±n/a K
IC50
2.4±0.3 nM
Km
5100±1300 nM
kcat
1.3±0.3 1/sec
Citation
 Wang, HLiu, YHuai, QCai, JZoraghi, RFrancis, SHCorbin, JDRobinson, HXin, ZLin, GKe, H Multiple conformations of phosphodiesterase-5: implications for enzyme function and drug development. J Biol Chem 281:21469-79 (2006) [PubMed]  Article 
Target
Name:
cGMP-specific 3',5'-cyclic phosphodiesterase [535-860]
Synonyms:
CGB-PDE | PDE5 | PDE5A | PDE5A_HUMAN | Phosphodiesterase Type 5 (PDE5A) | cGMP-binding cGMP-specific phosphodiesterase | cGMP-specific 3,5-cyclic phosphodiesterase
Type:
Enzyme Catalytic Domain
Mol. Mass.:
37741.15
Organism:
Homo sapiens (Human)
Description:
The coding regions for amino acids 535-860 of PDE5A1 were cloned and expressed in E. coli.
Residue:
326
Sequence:
EETRELQSLAAAVVPSAQTLKITDFSFSDFELSDLETALCTIRMFTDLNLVQNFQMKHEVLCRWILSVKKNYRKNVAYHNWRHAFNTAQCMFAALKAGKIQNKLTDLEILALLIAALSHDLDHRGVNNSYIQRSEHPLAQLYCHSIMEHHHFDQCLMILNSPGNQILSGLSIEEYKTTLKIIKQAILATDLALYIKRRGEFFELIRKNQFNLEDPHQKELFLAMLMTACDLSAITKPWPIQQRIAELVATEFFDQGDRERKELNIEPTDLMNREKKNKIPSMQVGFIDAICLQLYEALTHVSEDCFPLLDGCRKNRQKWQALAEQQ
  
Inhibitor
Name:
BDBM14390
Synonyms:
5-[2-ethoxy-5-(4-methyl-1-piperazinylsulfonyl)phenyl]-1-methyl-3-n-propyl-1,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one | 5-{2-ethoxy-5-[(4-methylpiperazine-1-)sulfonyl]phenyl}-1-methyl-3-propyl-1H,6H,7H-pyrazolo[4,3-d]pyrimidin-7-one | CHEMBL192 | SILDENAFIL CITRATE | Sildenafil | Sildenafil# | US11155558, Compound sildenafil | US11242347, Compound sildenafil | Viagra
Type:
Small organic molecule
Emp. Form.:
C22H30N6O4S
Mol. Mass.:
474.576
SMILES:
CCCc1nn(C)c2c1nc([nH]c2=O)-c1cc(ccc1OCC)S(=O)(=O)N1CCN(C)CC1
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: