| Reaction Details |
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 | Report a problem with these data |
| Target | cGMP-specific 3',5'-cyclic phosphodiesterase |
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| Ligand | BDBM14392 |
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| Substrate/Competitor | BDBM14391 |
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| Meas. Tech. | PDE Enzyme Inhibitor Assays |
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| pH | 7.4±n/a |
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| Temperature | 303.15±n/a K |
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| IC50 | 1.3±n/a nM |
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| Comments | cGMP in a 3:1 ratio unlabeled to 3H-labeled at a concentration 1/3Km, such that IC50 = Ki. |
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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 |
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| 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 |
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| Type: | Protein |
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| Mol. Mass.: | 99975.83 |
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| Organism: | Homo sapiens (Human) |
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| Description: | O76074 |
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| Residue: | 875 |
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| Sequence: | MERAGPSFGQQRQQQQPQQQKQQQRDQDSVEAWLDDHWDFTFSYFVRKATREMVNAWFAE
RVHTIPVCKEGIRGHTESCSCPLQQSPRADNSAPGTPTRKISASEFDRPLRPIVVKDSEG
TVSFLSDSEKKEQMPLTPPRFDHDEGDQCSRLLELVKDISSHLDVTALCHKIFLHIHGLI
SADRYSLFLVCEDSSNDKFLISRLFDVAEGSTLEEVSNNCIRLEWNKGIVGHVAALGEPL
NIKDAYEDPRFNAEVDQITGYKTQSILCMPIKNHREEVVGVAQAINKKSGNGGTFTEKDE
KDFAAYLAFCGIVLHNAQLYETSLLENKRNQVLLDLASLIFEEQQSLEVILKKIAATIIS
FMQVQKCTIFIVDEDCSDSFSSVFHMECEELEKSSDTLTREHDANKINYMYAQYVKNTME
PLNIPDVSKDKRFPWTTENTGNVNQQCIRSLLCTPIKNGKKNKVIGVCQLVNKMEENTGK
VKPFNRNDEQFLEAFVIFCGLGIQNTQMYEAVERAMAKQMVTLEVLSYHASAAEEETREL
QSLAAAVVPSAQTLKITDFSFSDFELSDLETALCTIRMFTDLNLVQNFQMKHEVLCRWIL
SVKKNYRKNVAYHNWRHAFNTAQCMFAALKAGKIQNKLTDLEILALLIAALSHDLDHRGV
NNSYIQRSEHPLAQLYCHSIMEHHHFDQCLMILNSPGNQILSGLSIEEYKTTLKIIKQAI
LATDLALYIKRRGEFFELIRKNQFNLEDPHQKELFLAMLMTACDLSAITKPWPIQQRIAE
LVATEFFDQGDRERKELNIEPTDLMNREKKNKIPSMQVGFIDAICLQLYEALTHVSEDCF
PLLDGCRKNRQKWQALAEQQEKMLINGESGQAKRN
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| BDBM14392 |
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| BDBM14391 |
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| Name | BDBM14392 |
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| Synonyms: | 3-ethyl-5-{5-[(4-ethylpiperazine-1-)sulfonyl]-2-(2-methoxyethoxy)pyridin-3-yl}-2-(pyridin-2-ylmethyl)-2H,6H,7H-pyrazolo[4,3-d]pyrimidin-7-one | CHEMBL209157 | Sildenafil Pyridyl Methyl Analogue 1 |
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| Type | Small organic molecule |
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| Emp. Form. | C27H34N8O5S |
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| Mol. Mass. | 582.674 |
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| SMILES | CCN1CCN(CC1)S(=O)(=O)c1cnc(OCCOC)c(c1)-c1nc2c(CC)n(Cc3ccccn3)nc2c(=O)[nH]1 |
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| Structure | 
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