Reaction Details |
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Target | Dual specificity calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1C |
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Ligand | BDBM50308557 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_613556 (CHEMBL1074182) |
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IC50 | >2000±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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Dual specificity calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1C |
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Name: | Dual specificity calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1C |
Synonyms: | 3',5'-cyclic-AMP phosphodiesterase | 3',5'-cyclic-GMP phosphodiesterase | Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1C | Cam-PDE 1C | Hcam3 | PDE1C | PDE1C_HUMAN | Phosphodiesterase 1 | Phosphodiesterase 1C | Phosphodiesterase, PDE1/PDE5 |
Type: | Enzyme |
Mol. Mass.: | 80778.58 |
Organism: | Homo sapiens (Human) |
Description: | Q14123 |
Residue: | 709 |
Sequence: | MESPTKEIEEFESNSLKYLQPEQIEKIWLRLRGLRKYKKTSQRLRSLVKQLERGEASVVD
LKKNLEYAATVLESVYIDETRRLLDTEDELSDIQSDAVPSEVRDWLASTFTRQMGMMLRR
SDEKPRFKSIVHAVQAGIFVERMYRRTSNMVGLSYPPAVIEALKDVDKWSFDVFSLNEAS
GDHALKFIFYELLTRYDLISRFKIPISALVSFVEALEVGYSKHKNPYHNLMHAADVTQTV
HYLLYKTGVANWLTELEIFAIIFSAAIHDYEHTGTTNNFHIQTRSDPAILYNDRSVLENH
HLSAAYRLLQDDEEMNILINLSKDDWREFRTLVIEMVMATDMSCHFQQIKAMKTALQQPE
AIEKPKALSLMLHTADISHPAKAWDLHHRWTMSLLEEFFRQGDREAELGLPFSPLCDRKS
TMVAQSQVGFIDFIVEPTFTVLTDMTEKIVSPLIDETSQTGGTGQRRSSLNSISSSDAKR
SGVKTSGSEGSAPINNSVISVDYKSFKATWTEVVHINRERWRAKVPKEEKAKKEAEEKAR
LAAEEQQKEMEAKSQAEEGASGKAEKKTSGETKNQVNGTRANKSDNPRGKNSKAEKSSGE
QQQNGDFKDGKNKTDKKDHSNIGNDSKKTDGTKQRSHGSPAPSTSSTCRLTLPVIKPPLR
HFKRPAYASSSYAPSVSKKTDEHPARYKMLDQRIKMKKIQNISHNWNRK
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BDBM50308557 |
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n/a |
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Name | BDBM50308557 |
Synonyms: | 3-(4-(2-hydroxyethyl)piperazin-1-yl)-1-(2-propoxyethyl)-7-(6-methoxypyridin-3-yl)pyrido[3,4-b]pyrazin-2(1H)-one | CHEMBL591501 |
Type | Small organic molecule |
Emp. Form. | C24H32N6O4 |
Mol. Mass. | 468.5487 |
SMILES | CCCOCCn1c2cc(ncc2nc(N2CCN(CCO)CC2)c1=O)-c1ccc(OC)nc1 |
Structure |
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