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Target
cGMP-specific 3',5'-cyclic phosphodiesterase
Ligand
BDBM50140600
Substrate
n/a
Meas. Tech.
ChEBML_155208
IC50
43±n/a nM
Citation
Pissarnitski, DA; Asberom, T; Boyle, CD; Chackalamannil, S; Chintala, M; Clader, JW; Greenlee, WJ; Hu, Y; Kurowski, S; Myers, J; Palamanda, J; Stamford, AW; Vemulapalli, S; Wang, Y; Wang, P; Wu, P; Xu, R SAR development of polycyclic guanine derivatives targeted to the discovery of a selective PDE5 inhibitor for treatment of erectile dysfunction. Bioorg Med Chem Lett 14:1291-4 (2004) [PubMed] Article
More Info.:
Target
Name:
cGMP-specific 3',5'-cyclic phosphodiesterase
Synonyms:
3',5'-cyclic phosphodiesterase | CGB-PDE | PDE5 | PDE5A | PDE5A_HUMAN | Phosphodiesterase 2 and 5 (PDE2 and PDE5) | Phosphodiesterase 5 (PDE5) | Phosphodiesterase 5A | Phosphodiesterase 5A (PDE5A) | cGMP-binding cGMP-specific phosphodiesterase | cGMP-specific 3',5'-cyclic phosphodiesterase
Type:
Protein
Mol. Mass.:
99975.83
Organism:
Human
Description:
O76074
Residue:
875
Sequence:
MERAGPSFGQQRQQQQPQQQKQQQRDQDSVEAWLDDHWDFTFSYFVRKATREMVNAWFAERVHTIPVCKEGIRGHTESCSCPLQQSPRADNSAPGTPTRKISASEFDRPLRPIVVKDSEGTVSFLSDSEKKEQMPLTPPRFDHDEGDQCSRLLELVKDISSHLDVTALCHKIFLHIHGLISADRYSLFLVCEDSSNDKFLISRLFDVAEGSTLEEVSNNCIRLEWNKGIVGHVAALGEPLNIKDAYEDPRFNAEVDQITGYKTQSILCMPIKNHREEVVGVAQAINKKSGNGGTFTEKDEKDFAAYLAFCGIVLHNAQLYETSLLENKRNQVLLDLASLIFEEQQSLEVILKKIAATIISFMQVQKCTIFIVDEDCSDSFSSVFHMECEELEKSSDTLTREHDANKINYMYAQYVKNTMEPLNIPDVSKDKRFPWTTENTGNVNQQCIRSLLCTPIKNGKKNKVIGVCQLVNKMEENTGKVKPFNRNDEQFLEAFVIFCGLGIQNTQMYEAVERAMAKQMVTLEVLSYHASAAEEETRELQSLAAAVVPSAQTLKITDFSFSDFELSDLETALCTIRMFTDLNLVQNFQMKHEVLCRWILSVKKNYRKNVAYHNWRHAFNTAQCMFAALKAGKIQNKLTDLEILALLIAALSHDLDHRGVNNSYIQRSEHPLAQLYCHSIMEHHHFDQCLMILNSPGNQILSGLSIEEYKTTLKIIKQAILATDLALYIKRRGEFFELIRKNQFNLEDPHQKELFLAMLMTACDLSAITKPWPIQQRIAELVATEFFDQGDRERKELNIEPTDLMNREKKNKIPSMQVGFIDAICLQLYEALTHVSEDCFPLLDGCRKNRQKWQALAEQQEKMLINGESGQAKRN
Inhibitor
Name:
BDBM50140600
Synonyms:
(R)-5-((7-benzyl-5-ethyl-2-methoxy-4-oxo-4,5,7,8-tetrahydroimidazo[2,1-e]purin-3-yl)methyl)-2-hydroxybenzonitrile | 5-[7-benzyl-5-ethyl-2-methoxy-4-oxo-(7R)-4,5,7,8-tetrahydro-3H-imidazo[2,1-b]purin-3-ylmethyl]-2-hydroxybenzonitrile | CHEMBL23513
Type:
Small organic molecule
Emp. Form.:
C25H24N6O3
Mol. Mass.:
456.4965
SMILES:
CCN1C2=N[C@H](Cc3ccccc3)CN2c2nc(OC)n(Cc3ccc(O)c(c3)C#N)c2C1=O |r,t:3|