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Literature summary for 3.1.26.13 extracted from

  • Velthuisen, E.J.; Johns, B.A.; Gerondelis, P.; Chen, Y.; Li, M.; Mou, K.; Zhang, W.; Seal, J.W.; Hightower, K.E.; Miranda, S.R.; Brown, K.; Leesnitzer, L.
    Pyridopyrimidinone inhibitors of HIV-1 RNase H (2014), Eur. J. Med. Chem., 83, 609-616.
    View publication on PubMed
Search for more literature for 3.1.26.13

Inhibitors

Inhibitors Comment Organism Structure
1-hydroxy-4-((4-(morpholinomethyl)phenyl)amino)pyrido[2,3-d]pyrimidin-2(1H)-one
-
 Human immunodeficiency virus 1
1-hydroxy-4-((4-(pyridin-4-yl)phenyl)amino)pyrido[2,3-d]pyrimidin-2(1H)-one
-
 Human immunodeficiency virus 1
1-hydroxy-4-([[3-(4-morpholinyl)phenyl]methyl]amino)pyrido[2,3-d]pyrimidin-2(1H)-one
-
 Human immunodeficiency virus 1
1-hydroxy-4-([[3-(4-morpholinylmethyl)phenyl]methyl]amino)pyrido[2,3-d]pyrimidin-2(1H)-one
-
 Human immunodeficiency virus 1
1-hydroxy-4-([[4-(4-morpholinyl)phenyl]methyl]amino)pyrido[2,3-d]pyrimidin-2(1H)-one
-
 Human immunodeficiency virus 1
1-hydroxy-4-([[4-(4-pyridinyl)phenyl]methyl]amino)pyrido[2,3-d]pyrimidin-2(1H)-one
-
 Human immunodeficiency virus 1
1-hydroxy-4-[[4-(4-morpholinyl)phenyl]amino]pyrido[2,3-d]pyrimidin-2(1H)-one
-
 Human immunodeficiency virus 1
1-hydroxypyrido[2,3-d]pyrimidin-2(1H)-one
-
 Human immunodeficiency virus 1
2-hydroxyisoquinoline-1,3(2H,4H)-dione
-
 Human immunodeficiency virus 1
4-((cyclopropylmethyl)amino)-1-hydroxypyrido[2,3-d]pyrimidin-2(1H)-one
-
 Human immunodeficiency virus 1
4-(([1,1'-biphenyl]-4-ylmethyl)amino)-1-hydroxypyrido[2,3-d]pyrimidin-2(1H)-one
-
 Human immunodeficiency virus 1
4-(4,4-difluoropiperidin-1-yl)-1-hydroxypyrido[2,3-d]pyrimidin-2(1H)-one
-
 Human immunodeficiency virus 1
4-([1,1'-biphenyl]-4-ylamino)-1-hydroxypyrido[2,3-d]pyrimidin-2(1H)-one
-
 Human immunodeficiency virus 1
4-[[(4-fluorophenyl)methyl]amino]-1-hydroxypyrido[2,3-d]pyrimidin-2(1H)-one
-
 Human immunodeficiency virus 1
5-(1,1-dioxido-1,2-thiazinan-2-yl)-N-(4-fluorobenzyl)-8-hydroxy-1,6-naphthyridine-7-carboxamide
-
 Human immunodeficiency virus 1
8-hydroxy-1,6-naphthyridine-7-carboxylic acid
-
 Human immunodeficiency virus 1
N-(4-chlorobenzyl)-8-hydroxy-1,6-naphthyridine-7-carboxamide
-
 Human immunodeficiency virus 1

Metals/Ions

Metals/Ions Comment Organism Structure
Mg2+ two Mg2+ ions as essential in formation of the active catalytic complex Human immunodeficiency virus 1

Organism

Organism UniProt Comment Textmining
Human immunodeficiency virus 1
-
-
-

Synonyms

Synonyms Comment Organism
reverse transcriptase bifunctional enzyme with DNA polymerase and ribonuclease H activities Human immunodeficiency virus 1
ribonuclease H
-
 Human immunodeficiency virus 1
RNase H
-
 Human immunodeficiency virus 1

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00001
-
 in 50 mM Tris, pH 8.0, 80 mM KCl, 10 mM MgCl2, at 22°C Human immunodeficiency virus 1 4-(([1,1'-biphenyl]-4-ylmethyl)amino)-1-hydroxypyrido[2,3-d]pyrimidin-2(1H)-one
0.000016
-
 in 50 mM Tris, pH 8.0, 80 mM KCl, 10 mM MgCl2, at 22°C Human immunodeficiency virus 1 1-hydroxy-4-([[4-(4-pyridinyl)phenyl]methyl]amino)pyrido[2,3-d]pyrimidin-2(1H)-one
0.000032
-
 in 50 mM Tris, pH 8.0, 80 mM KCl, 10 mM MgCl2, at 22°C Human immunodeficiency virus 1 4-([1,1'-biphenyl]-4-ylamino)-1-hydroxypyrido[2,3-d]pyrimidin-2(1H)-one
0.00005
-
 in 50 mM Tris, pH 8.0, 80 mM KCl, 10 mM MgCl2, at 22°C Human immunodeficiency virus 1 1-hydroxy-4-[[4-(4-morpholinyl)phenyl]amino]pyrido[2,3-d]pyrimidin-2(1H)-one
0.000079
-
 in 50 mM Tris, pH 8.0, 80 mM KCl, 10 mM MgCl2, at 22°C Human immunodeficiency virus 1 1-hydroxy-4-((4-(pyridin-4-yl)phenyl)amino)pyrido[2,3-d]pyrimidin-2(1H)-one
0.0001
-
 in 50 mM Tris, pH 8.0, 80 mM KCl, 10 mM MgCl2, at 22°C Human immunodeficiency virus 1 1-hydroxy-4-([[4-(4-morpholinyl)phenyl]methyl]amino)pyrido[2,3-d]pyrimidin-2(1H)-one
0.000158
-
 in 50 mM Tris, pH 8.0, 80 mM KCl, 10 mM MgCl2, at 22°C Human immunodeficiency virus 1 4-[[(4-fluorophenyl)methyl]amino]-1-hydroxypyrido[2,3-d]pyrimidin-2(1H)-one
0.0002
-
 in 50 mM Tris, pH 8.0, 80 mM KCl, 10 mM MgCl2, at 22°C Human immunodeficiency virus 1 1-hydroxy-4-((4-(morpholinomethyl)phenyl)amino)pyrido[2,3-d]pyrimidin-2(1H)-one
0.0002
-
 in 50 mM Tris, pH 8.0, 80 mM KCl, 10 mM MgCl2, at 22°C Human immunodeficiency virus 1 1-hydroxy-4-([[3-(4-morpholinyl)phenyl]methyl]amino)pyrido[2,3-d]pyrimidin-2(1H)-one
0.000398
-
 in 50 mM Tris, pH 8.0, 80 mM KCl, 10 mM MgCl2, at 22°C Human immunodeficiency virus 1 4-((cyclopropylmethyl)amino)-1-hydroxypyrido[2,3-d]pyrimidin-2(1H)-one
0.000398
-
 in 50 mM Tris, pH 8.0, 80 mM KCl, 10 mM MgCl2, at 22°C Human immunodeficiency virus 1 1-hydroxy-4-([[3-(4-morpholinylmethyl)phenyl]methyl]amino)pyrido[2,3-d]pyrimidin-2(1H)-one
0.000501
-
 in 50 mM Tris, pH 8.0, 80 mM KCl, 10 mM MgCl2, at 22°C Human immunodeficiency virus 1 4-(4,4-difluoropiperidin-1-yl)-1-hydroxypyrido[2,3-d]pyrimidin-2(1H)-one