Target
cGMP-specific 3',5'-cyclic phosphodiesterase [1-660,682-875]
Ligand
BDBM15338
Substrate
BDBM14391
Meas. Tech.
Enzymatic Assay
pH
7.8±n/a
Temperature
297.15±n/a K
IC50
55000±13000 nM
Km
750000±210000 nM
kcat
2.3±0.6 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 [1-660,682-875]
Synonyms:
PDE5 | PDE5A | PDE5A_HUMAN | Phosphodiesterase Type 5 (PDE5A) H-loop deletion mutant | Phosphodiesterase Type 5 (PDE5A) Mutant (del 661-681)
Type:
Enzyme Catalytic Domain
Mol. Mass.:
97488.04
Organism:
Homo sapiens (Human)
Description:
Mutant was generated from wild-type clone and expressed in E. coli.
Residue:
854
Sequence:
MERAGPSFGQQRQQQQPQQQKQQQRDQDSVEAWLDDHWDFTFSYFVRKATREMVNAWFAERVHTIPVCKEGIRGHTESCSCPLQQSPRADNSAPGTPTRKISASEFDRPLRPIVVKDSEGTVSFLSDSEKKEQMPLTPPRFDHDEGDQCSRLLELVKDISSHLDVTALCHKIFLHIHGLISADRYSLFLVCEDSSNDKFLISRLFDVAEGSTLEEVSNNCIRLEWNKGIVGHVAALGEPLNIKDAYEDPRFNAEVDQITGYKTQSILCMPIKNHREEVVGVAQAINKKSGNGGTFTEKDEKDFAAYLAFCGIVLHNAQLYETSLLENKRNQVLLDLASLIFEEQQSLEVILKKIAATIISFMQVQKCTIFIVDEDCSDSFSSVFHMECEELEKSSDTLTREHDANKINYMYAQYVKNTMEPLNIPDVSKDKRFPWTTENTGNVNQQCIRSLLCTPIKNGKKNKVIGVCQLVNKMEENTGKVKPFNRNDEQFLEAFVIFCGLGIQNTQMYEAVERAMAKQMVTLEVLSYHASAAEEETRELQSLAAAVVPSAQTLKITDFSFSDFELSDLETALCTIRMFTDLNLVQNFQMKHEVLCRWILSVKKNYRKNVAYHNWRHAFNTAQCMFAALKAGKIQNKLTDLEILALLIAALSHDLDHRGVEHHHFDQCLMILNSPGNQILSGLSIEEYKTTLKIIKQAILATDLALYIKRRGEFFELIRKNQFNLEDPHQKELFLAMLMTACDLSAITKPWPIQQRIAELVATEFFDQGDRERKELNIEPTDLMNREKKNKIPSMQVGFIDAICLQLYEALTHVSEDCFPLLDGCRKNRQKWQALAEQQEKMLINGESGQAKRN
  
Inhibitor
Name:
BDBM15338
Synonyms:
5,7-dihydroxy-2-(4-methoxyphenyl)-8-(3-methylbutyl)-3-[(2S,3R,4R,5R,6S)-3,4,5-trihydroxy-6-methyl-oxan-2-yl]oxy-chromen-4-one | 5,7-dihydroxy-2-(4-methoxyphenyl)-8-(3-methylbutyl)-3-{[(2S,3R,4R,5R,6S)-3,4,5-trihydroxy-6-methyloxan-2-yl]oxy}-4H-chromen-4-one | 7CA | Icarisid II
Type:
Small organic molecule
Emp. Form.:
C27H32O10
Mol. Mass.:
516.537
SMILES:
COc1ccc(cc1)-c1oc2c(CCC(C)C)c(O)cc(O)c2c(=O)c1O[C@@H]1O[C@@H](C)[C@H](O)[C@@H](O)[C@H]1O |r|
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: