Reaction Details |
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Target | cGMP-specific 3',5'-cyclic phosphodiesterase |
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Ligand | BDBM14408 |
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Substrate/Competitor | BDBM14391 |
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Meas. Tech. | PDE Enzyme Inhibitor Assays |
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IC50 | 0.9±n/a nM |
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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 |
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More Info.: | Get all data from this article, Solution Info, Assay Method |
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cGMP-specific 3',5'-cyclic phosphodiesterase |
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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: | Homo sapiens (Human) |
Description: | O76074 |
Residue: | 875 |
Sequence: | MERAGPSFGQQRQQQQPQQQKQQQRDQDSVEAWLDDHWDFTFSYFVRKATREMVNAWFAE
RVHTIPVCKEGIRGHTESCSCPLQQSPRADNSAPGTPTRKISASEFDRPLRPIVVKDSEG
TVSFLSDSEKKEQMPLTPPRFDHDEGDQCSRLLELVKDISSHLDVTALCHKIFLHIHGLI
SADRYSLFLVCEDSSNDKFLISRLFDVAEGSTLEEVSNNCIRLEWNKGIVGHVAALGEPL
NIKDAYEDPRFNAEVDQITGYKTQSILCMPIKNHREEVVGVAQAINKKSGNGGTFTEKDE
KDFAAYLAFCGIVLHNAQLYETSLLENKRNQVLLDLASLIFEEQQSLEVILKKIAATIIS
FMQVQKCTIFIVDEDCSDSFSSVFHMECEELEKSSDTLTREHDANKINYMYAQYVKNTME
PLNIPDVSKDKRFPWTTENTGNVNQQCIRSLLCTPIKNGKKNKVIGVCQLVNKMEENTGK
VKPFNRNDEQFLEAFVIFCGLGIQNTQMYEAVERAMAKQMVTLEVLSYHASAAEEETREL
QSLAAAVVPSAQTLKITDFSFSDFELSDLETALCTIRMFTDLNLVQNFQMKHEVLCRWIL
SVKKNYRKNVAYHNWRHAFNTAQCMFAALKAGKIQNKLTDLEILALLIAALSHDLDHRGV
NNSYIQRSEHPLAQLYCHSIMEHHHFDQCLMILNSPGNQILSGLSIEEYKTTLKIIKQAI
LATDLALYIKRRGEFFELIRKNQFNLEDPHQKELFLAMLMTACDLSAITKPWPIQQRIAE
LVATEFFDQGDRERKELNIEPTDLMNREKKNKIPSMQVGFIDAICLQLYEALTHVSEDCF
PLLDGCRKNRQKWQALAEQQEKMLINGESGQAKRN
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BDBM14408 |
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BDBM14391 |
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Name | BDBM14408 |
Synonyms: | 5-(2-butoxy-5-acetylpyridin-3-yl)-3-ethyl-2-[(1-methyl-1H-imidazol-2-yl)methyl]-2H,6H,7H-pyrazolo[4,3-d]pyrimidin-7-one | 5-(5-Acetyl-2-butoxy-3-pyridinyl)-3-ethyl-2-[(1-methyl-1H-imidazol-2-yl)methyl]-2,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one | Sildenafil 5-methyl ketone analogue 49 |
Type | Small organic molecule |
Emp. Form. | C23H27N7O3 |
Mol. Mass. | 449.5056 |
SMILES | CCCCOc1ncc(cc1-c1nc2c(CC)n(Cc3nccn3C)nc2c(=O)[nH]1)C(C)=O |
Structure |
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