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Literature summary for 3.1.4.35 extracted from

  • Hughes, R.O.; Rogier, D.J.; Jacobsen, E.J.; Walker, J.K.; Macinnes, A.; Bond, B.R.; Zhang, L.L.; Yu, Y.; Zheng, Y.; Rumsey, J.M.; Walgren, J.L.; Curtiss, S.W.; Fobian, Y.M.; Heasley, S.E.; Cubbage, J.W.; Moon, J.B.; Brown, D.L.; Acker, B.A.; Maddux, T.M.; Tollefson, M.B.; Mischke, B.V.; Owen, D.R.; Freskos, J.N.; Molyneaux, J.M.; Benson, A.G.; Blevis-Bal, R.M.
    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) (2010), J. Med. Chem., 53, 2656-2660.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
3-(4-ethylpiperazin-1-yl)-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2(1H)-one
-
Rattus norvegicus
3-([2-[(2-hydroxyethyl)amino]ethyl]amino)-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2(1H)-one
-
Rattus norvegicus
3-[(1R,4R)-2,5-diazabicyclo[2.2.1]hept-2-yl]-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2(1H)-one
-
Rattus norvegicus
3-[(2-aminoethyl)amino]-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2(1H)-one
-
Rattus norvegicus
3-[(trans-4-hydroxycyclohexyl)amino]-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2(1H)-one
-
Rattus norvegicus
3-[4-(2,2-dihydroxypropyl)-1,4-diazepan-1-yl]-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2(1H)-one
-
Rattus norvegicus
3-[4-(2-hydroxyethyl)-1,4-diazepan-1-yl]-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2(1H)-one
-
Rattus norvegicus
3-[4-(2-hydroxyethyl)piperazin-1-yl]-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[3,4-b]-pyrazin-2(1H)-one
-
Rattus norvegicus
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 Rattus norvegicus
3-[4-(3-hydroxypropyl)-1,4-diazepan-1-yl]-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2(1H)-one
-
Rattus norvegicus
3-[4-(3-hydroxypropyl)piperazin-1-yl]-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2(1H)-one
-
Rattus norvegicus
3-[4-[(2R)-2-hydroxypropyl]-1,4-diazepan-1-yl]-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2(1H)-one
-
Rattus norvegicus
3-[4-[(2R,3R)-3-hydroxybutan-2-yl]-1,4-diazepan-1-yl]-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2(1H)-one
-
Rattus norvegicus
3-[4-[(2S)-2-hydroxypropyl]-1,4-diazepan-1-yl]-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2(1H)-one
-
Rattus norvegicus
3-[4-[(2S,3R)-3-hydroxybutan-2-yl]-1,4-diazepan-1-yl]-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2(1H)-one
-
Rattus norvegicus
7-(6-methoxypyridin-3-yl)-3-(piperazin-1-yl)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2(1H)-one
-
Rattus norvegicus

Organism

Organism UniProt Comment Textmining
Rattus norvegicus
-
-
-

Synonyms

Synonyms Comment Organism
PDE5
-
Rattus norvegicus
phosphodiesterase 5
-
Rattus norvegicus

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00000018
-
pH and temperature not specified in the publication Rattus norvegicus 3-[4-(3-hydroxypropyl)piperazin-1-yl]-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2(1H)-one
0.0000002
-
pH and temperature not specified in the publication Rattus norvegicus 3-[4-(2-hydroxyethyl)piperazin-1-yl]-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[3,4-b]-pyrazin-2(1H)-one
0.0000002
-
pH and temperature not specified in the publication Rattus norvegicus 3-[4-(2-hydroxyethyl)piperazin-1-yl]-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2(1H)-one
0.00000021
-
pH and temperature not specified in the publication Rattus norvegicus 3-[4-(2,2-dihydroxypropyl)-1,4-diazepan-1-yl]-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2(1H)-one
0.00000022
-
pH and temperature not specified in the publication Rattus norvegicus 3-(4-ethylpiperazin-1-yl)-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2(1H)-one
0.00000023
-
pH and temperature not specified in the publication Rattus norvegicus 3-[4-[(2R)-2-hydroxypropyl]-1,4-diazepan-1-yl]-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2(1H)-one
0.00000025
-
pH and temperature not specified in the publication Rattus norvegicus 3-[(2-aminoethyl)amino]-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2(1H)-one
0.0000003
-
pH and temperature not specified in the publication Rattus norvegicus 3-[4-[(2R,3R)-3-hydroxybutan-2-yl]-1,4-diazepan-1-yl]-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2(1H)-one
0.00000031
-
pH and temperature not specified in the publication Rattus norvegicus 3-[4-[(2S)-2-hydroxypropyl]-1,4-diazepan-1-yl]-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2(1H)-one
0.00000033
-
pH and temperature not specified in the publication Rattus norvegicus 3-[4-[(2S,3R)-3-hydroxybutan-2-yl]-1,4-diazepan-1-yl]-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2(1H)-one
0.00000072
-
pH and temperature not specified in the publication Rattus norvegicus 3-[4-(2-hydroxyethyl)-1,4-diazepan-1-yl]-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2(1H)-one
0.00000108
-
pH and temperature not specified in the publication Rattus norvegicus 3-[4-(3-hydroxypropyl)-1,4-diazepan-1-yl]-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2(1H)-one
0.00000112
-
pH and temperature not specified in the publication Rattus norvegicus 3-([2-[(2-hydroxyethyl)amino]ethyl]amino)-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2(1H)-one
0.00000238
-
pH and temperature not specified in the publication Rattus norvegicus 3-[(1R,4R)-2,5-diazabicyclo[2.2.1]hept-2-yl]-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2(1H)-one
0.00000328
-
pH and temperature not specified in the publication Rattus norvegicus 7-(6-methoxypyridin-3-yl)-3-(piperazin-1-yl)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2(1H)-one