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Literature summary for 3.4.23.15 extracted from

  • Sarver, R.W.; Peevers, J.; Cody, W.L.; Ciske, F.L.; Dyer, J.; Emerson, S.D.; Hagadorn, J.C.; Holsworth, D.D.; Jalaie, M.; Kaufman, M.; Mastronardi, M.; McConnell, P.; Powell, N.A.; Quin, J.; Van Huis, C.A.; Zhang, E.; Mochalkin, I.
    Binding thermodynamics of substituted diaminopyrimidine renin inhibitors (2007), Anal. Biochem., 360, 30-40.
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
expression in COS cells Homo sapiens

Crystallization (Commentary)

Crystallization (Comment) Organism
hanging drop vapor diffusion method, recombinant renin. Crystal structure of recombinant renin in complex with 5-[4-[(3,5-difluorobenzyl)amino]phenyl]-6-ethylpyrimidine-2,4-diamine, 6-ethyl-5-[1-(3-methoxypropyl)-2-phenyl-1,2,3,4-tetrahydroquinolin-7-yl]pyrimidine-2,4-diamine, and N-[2-([2-amino-6-ethyl-5-[4-(3-methoxypropyl)-2,2-dimethyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-6-yl]pyrimidin-4-yl]amino)ethyl]naphthalene-2-sulfonamide Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(2R)-6-(2,4-diamino-6-ethylpyrimidin-5-yl)-4-(3-methoxypropyl)-2-methyl-2H-1,4-benzoxazin-3(4H)-one
-
Homo sapiens
4-amino-N-[2-[2-([2-amino-6-ethyl-5-[4-(3-methoxypropyl)-2,2-dimethyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-6-yl]pyrimidin-4-yl]amino)ethyl]phenyl]-3-methoxybenzamide
-
Homo sapiens
5-[4-[(3,5-difluorobenzyl)amino]phenyl]-6-ethylpyrimidine-2,4-diamine
-
Homo sapiens
6-(2,4-diamino-6-ethylpyrimidin-5-yl)-2-(3,5-difluorophenyl)-4-(3-methoxypropyl)-2-methyl-2H-1,4-benzoxazin-3(4H)-one
-
Homo sapiens
6-(2,4-diamino-6-ethylpyrimidin-5-yl)-2-(3,5-difluorophenyl)-4-(3-methoxypropyl)-2H-1,4-benzoxazin-3(4H)-one
-
Homo sapiens
6-ethyl-5-[1-(3-methoxypropyl)-1,2,3,4-tetrahydroquinolin-7-yl]pyrimidine-2,4-diamine
-
Homo sapiens
6-ethyl-5-[1-(3-methoxypropyl)-2-phenyl-1,2,3,4-tetrahydroquinolin-7-yl]pyrimidine-2,4-diamine
-
Homo sapiens
6-ethyl-5-[9-(3-methoxypropyl)-9H-carbazol-2-yl]pyrimidine-2,4-diamine
-
Homo sapiens
N-[2-([2-amino-6-ethyl-5-[4-(3-methoxypropyl)-2,2-dimethyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-6-yl]pyrimidin-4-yl]amino)ethyl]benzamide
-
Homo sapiens
N-[2-([2-amino-6-ethyl-5-[4-(3-methoxypropyl)-2,2-dimethyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-6-yl]pyrimidin-4-yl]amino)ethyl]naphthalene-2-sulfonamide
-
Homo sapiens
N-[2-[6-(2,4-diamino-6-ethylpyrimidin-5-yl)-2,2-dimethyl-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl]ethyl]acetamide
-
Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Purification (Commentary)

Purification (Comment) Organism
recombinant renin Homo sapiens

Source Tissue

Source Tissue Comment Organism Textmining
kidney fetal Homo sapiens
-

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0000071
-
-
Homo sapiens 6-(2,4-diamino-6-ethylpyrimidin-5-yl)-2-(3,5-difluorophenyl)-4-(3-methoxypropyl)-2-methyl-2H-1,4-benzoxazin-3(4H)-one
0.000027
-
-
Homo sapiens N-[2-([2-amino-6-ethyl-5-[4-(3-methoxypropyl)-2,2-dimethyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-6-yl]pyrimidin-4-yl]amino)ethyl]naphthalene-2-sulfonamide
0.000058
-
-
Homo sapiens 6-ethyl-5-[1-(3-methoxypropyl)-2-phenyl-1,2,3,4-tetrahydroquinolin-7-yl]pyrimidine-2,4-diamine
0.000095
-
-
Homo sapiens 6-(2,4-diamino-6-ethylpyrimidin-5-yl)-2-(3,5-difluorophenyl)-4-(3-methoxypropyl)-2H-1,4-benzoxazin-3(4H)-one
0.000132
-
-
Homo sapiens (2R)-6-(2,4-diamino-6-ethylpyrimidin-5-yl)-4-(3-methoxypropyl)-2-methyl-2H-1,4-benzoxazin-3(4H)-one
0.000173
-
-
Homo sapiens 6-ethyl-5-[9-(3-methoxypropyl)-9H-carbazol-2-yl]pyrimidine-2,4-diamine
0.000222
-
-
Homo sapiens N-[2-[6-(2,4-diamino-6-ethylpyrimidin-5-yl)-2,2-dimethyl-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl]ethyl]acetamide
0.000336
-
-
Homo sapiens 4-amino-N-[2-[2-([2-amino-6-ethyl-5-[4-(3-methoxypropyl)-2,2-dimethyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-6-yl]pyrimidin-4-yl]amino)ethyl]phenyl]-3-methoxybenzamide
0.000691
-
-
Homo sapiens 6-ethyl-5-[1-(3-methoxypropyl)-1,2,3,4-tetrahydroquinolin-7-yl]pyrimidine-2,4-diamine
0.00656
-
-
Homo sapiens 5-[4-[(3,5-difluorobenzyl)amino]phenyl]-6-ethylpyrimidine-2,4-diamine