Reaction Details |
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Target | High affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8B |
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Ligand | BDBM50296256 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_597988 (CHEMBL1045419) |
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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 8B |
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Name: | High affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8B |
Synonyms: | PDE8B | PDE8B_HUMAN | Phosphodiesterase 8 | Phosphodiesterase 8B |
Type: | PROTEIN |
Mol. Mass.: | 98984.88 |
Organism: | Homo sapiens (Human) |
Description: | ChEMBL_876321 |
Residue: | 885 |
Sequence: | MGCAPSIHVSQSGVIYCRDSDESSSPRQTTSVSQGPAAPLPGLFVQTDAADAIPPSRASG
PPSVARVRRARTELGSGSSAGSAAPAATTSRGRRRHCCSSAEAETQTCYTSVKQVSSAEV
RIGPMRLTQDPIQVLLIFAKEDSQSDGFWWACDRAGYRCNIARTPESALECFLDKHHEII
VIDHRQTQNFDAEAVCRSIRATNPSEHTVILAVVSRVSDDHEEASVLPLLHAGFNRRFME
NSSIIACYNELIQIEHGEVRSQFKLRACNSVFTALDHCHEAIEITSDDHVIQYVNPAFER
MMGYHKGELLGKELADLPKSDKNRADLLDTINTCIKKGKEWQGVYYARRKSGDSIQQHVK
ITPVIGQGGKIRHFVSLKKLCCTTDNNKQIHKIHRDSGDNSQTEPHSFRYKNRRKESIDV
KSISSRGSDAPSLQNRRYPSMARIHSMTIEAPITKVINIINAAQENSPVTVAEALDRVLE
ILRTTELYSPQLGTKDEDPHTSDLVGGLMTDGLRRLSGNEYVFTKNVHQSHSHLAMPITI
NDVPPCISQLLDNEESWDFNIFELEAITHKRPLVYLGLKVFSRFGVCEFLNCSETTLRAW
FQVIEANYHSSNAYHNSTHAADVLHATAFFLGKERVKGSLDQLDEVAALIAATVHDVDHP
GRTNSFLCNAGSELAVLYNDTAVLESHHTALAFQLTVKDTKCNIFKNIDRNHYRTLRQAI
IDMVLATEMTKHFEHVNKFVNSINKPMAAEIEGSDCECNPAGKNFPENQILIKRMMIKCA
DVANPCRPLDLCIEWAGRISEEYFAQTDEEKRQGLPVVMPVFDRNTCSIPKSQISFIDYF
ITDMFDAWDAFAHLPALMQHLADNYKHWKTLDDLKCKSLRLPSDS
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BDBM50296256 |
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n/a |
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Name | BDBM50296256 |
Synonyms: | 7-(6-methoxypyridin-3-yl)-3-(2-morpholinoethylamino)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2(1H)-one | CHEMBL551052 |
Type | Small organic molecule |
Emp. Form. | C24H32N6O4 |
Mol. Mass. | 468.5487 |
SMILES | CCCOCCn1c2cc(ncc2nc(NCCN2CCOCC2)c1=O)-c1ccc(OC)nc1 |
Structure |
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