| Reaction Details |
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 | Report a problem with these data |
| Target | cGMP-specific 3',5'-cyclic phosphodiesterase |
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| Ligand | BDBM50308561 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_613534 (CHEMBL1073645) |
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| IC50 | 0.300000±n/a nM |
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| Citation |  Hughes, RO; Rogier, DJ; Jacobsen, EJ; Walker, JK; Macinnes, A; Bond, BR; Zhang, LL; Yu, Y; Zheng, Y; Rumsey, JM; Walgren, JL; Curtiss, SW; Fobian, YM; Heasley, SE; Cubbage, JW; Moon, JB; Brown, DL; Acker, BA; Maddux, TM; Tollefson, MB; Mischke, BV; Owen, DR; Freskos, JN; Molyneaux, JM; Benson, AG; Blevis-Bal, RM Design, synthesis, and biological evaluation of 3-[4-(2-hydroxyethyl)piperazin-1-yl]-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2(1H)-one, a potent, orally active, brain penetrant inhibitor of phosphodiesterase 5 (PDE5). J Med Chem53:2656-60 (2010) [PubMed] Article |
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| More Info.: | Get all data from this article, 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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| BDBM50308561 |
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| n/a |
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| Name | BDBM50308561 |
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| Synonyms: | (+/-)-3-(4-((2R,3R)-3-hydroxybutan-2-yl)piperazin-1-yl)-1-(2-propoxyethyl)-7-(6-methoxypyridin-3-yl)pyrido[3,4-b]pyrazin-2(1H)-one | CHEMBL591942 |
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| Type | Small organic molecule |
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| Emp. Form. | C26H36N6O4 |
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| Mol. Mass. | 496.6018 |
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| SMILES | CCCOCCn1c2cc(ncc2nc(N2CCN(CC2)[C@H](C)[C@@H](C)O)c1=O)-c1ccc(OC)nc1 |r| |
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| Structure | 
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