Reaction Details |
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Target | cGMP-specific 3',5'-cyclic phosphodiesterase |
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Ligand | BDBM50297804 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_584078 (CHEMBL1058319) |
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IC50 | 2.5±n/a nM |
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Citation | Owen, DR; Walker, JK; Jon Jacobsen, E; Freskos, JN; Hughes, RO; Brown, DL; Bell, AS; Brown, DG; Phillips, C; Mischke, BV; Molyneaux, JM; Fobian, YM; Heasley, SE; Moon, JB; Stallings, WC; Joseph Rogier, D; Fox, DN; Palmer, MJ; Ringer, T; Rodriquez-Lens, M; Cubbage, JW; Blevis-Bal, RM; Benson, AG; Acker, BA; Maddux, TM; Tollefson, MB; Bond, BR; Macinnes, A; Yu, Y Identification, synthesis and SAR of amino substituted pyrido[3,2b]pyrazinones as potent and selective PDE5 inhibitors. Bioorg Med Chem Lett19:4088-91 (2009) [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 |
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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BDBM50297804 |
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n/a |
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Name | BDBM50297804 |
Synonyms: | 6-(4-fluorophenyl)-4-(pyridin-3-ylmethyl)-2-((tetrahydro-2H-pyran-4-yl)methylamino)pyrido[2,3-b]pyrazin-3(4H)-one | CHEMBL560545 |
Type | Small organic molecule |
Emp. Form. | C25H24FN5O2 |
Mol. Mass. | 445.4888 |
SMILES | Fc1ccc(cc1)-c1ccc2nc(NCC3CCOCC3)c(=O)n(Cc3cccnc3)c2n1 |
Structure |
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