| Reaction Details |
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 | Report a problem with these data |
| Target | High affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8A |
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| Ligand | BDBM50296256 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_597987 (CHEMBL1045418) |
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| IC50 | >2000±n/a nM |
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| Citation |  Hughes, RO; Walker, JK; Rogier, DJ; Heasley, SE; Blevis-Bal, RM; Benson, AG; Jacobsen, EJ; Cubbage, JW; Fobian, YM; Owen, DR; Freskos, JN; Molyneaux, JM; Brown, DL; Acker, BA; Maddux, TM; Tollefson, MB; Moon, JB; Mischke, BV; Rumsey, JM; Zheng, Y; MacInnes, A; Bond, BR; Yu, Y Optimization of the aminopyridopyrazinones class of PDE5 inhibitors: discovery of 3-[(trans-4-hydroxycyclohexyl)amino]-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2(1H)-one. Bioorg Med Chem Lett19:5209-13 (2009) [PubMed] Article |
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| More Info.: | Get all data from this article, Assay Method |
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| High affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8A |
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| Name: | High affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8A |
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| Synonyms: | High-affinity cAMP-specific and IBMX-insensitive 3 ,5 -cyclic phosphodiesterase 8A | PDE8A | PDE8A_HUMAN | Phosphodiesterase 8 | Phosphodiesterase 8 (PDE8) | Phosphodiesterase 8A (PDE8A) | Phosphodiesterase 8A (PDE8A1) | Phosphodiesterase 8A1 | Phosphodiesterase Type 8 (PDE8A) |
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| Type: | Enzyme Catalytic Domain |
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| Mol. Mass.: | 93295.89 |
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| Organism: | Homo sapiens (Human) |
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| Description: | Recombinant catalytic domain (M1-E829) of human PDE8A. |
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| Residue: | 829 |
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| Sequence: | MGCAPSIHISERLVAEDAPSPAAPPLSSGGPRLPQGQKTAALPRTRGAGLLESELRDGSG
KKVAVADVQFGPMRFHQDQLQVLLVFTKEDNQCNGFCRACEKAGFKCTVTKEAQAVLACF
LDKHHDIIIIDHRNPRQLDAEALCRSIRSSKLSENTVIVGVVRRVDREELSVMPFISAGF
TRRYVENPNIMACYNELLQLEFGEVRSQLKLRACNSVFTALENSEDAIEITSEDRFIQYA
NPAFETTMGYQSGELIGKELGEVPINEKKADLLDTINSCIRIGKEWQGIYYAKKKNGDNI
QQNVKIIPVIGQGGKIRHYVSIIRVCNGNNKAEKISECVQSDTHTDNQTGKHKDRRKGSL
DVKAVASRATEVSSQRRHSSMARIHSMTIEAPITKVINIINAAQESSPMPVTEALDRVLE
ILRTTELYSPQFGAKDDDPHANDLVGGLMSDGLRRLSGNEYVLSTKNTQMVSSNIITPIS
LDDVPPRIARAMENEEYWDFDIFELEAATHNRPLIYLGLKMFARFGICEFLHCSESTLRS
WLQIIEANYHSSNPYHNSTHSADVLHATAYFLSKERIKETLDPIDEVAALIAATIHDVDH
PGRTNSFLCNAGSELAILYNDTAVLESHHAALAFQLTTGDDKCNIFKNMERNDYRTLRQG
IIDMVLATEMTKHFEHVNKFVNSINKPLATLEENGETDKNQEVINTMLRTPENRTLIKRM
LIKCADVSNPCRPLQYCIEWAARISEEYFSQTDEEKQQGLPVVMPVFDRNTCSIPKSQIS
FIDYFITDMFDAWDAFVDLPDLMQHLDNNFKYWKGLDEMKLRNLRPPPE
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| BDBM50296256 |
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| n/a |
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| Name | BDBM50296256 |
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| Synonyms: | 7-(6-methoxypyridin-3-yl)-3-(2-morpholinoethylamino)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2(1H)-one | CHEMBL551052 |
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| Type | Small organic molecule |
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| Emp. Form. | C24H32N6O4 |
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| Mol. Mass. | 468.5487 |
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| SMILES | CCCOCCn1c2cc(ncc2nc(NCCN2CCOCC2)c1=O)-c1ccc(OC)nc1 |
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| Structure | 
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