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Literature summary for 2.4.2.1 extracted from

  • Semeraro, T.; Lossani, A.; Botta, M.; Ghiron, C.; Alvarez, R.; Manetti, F.; Mugnaini, C.; Valensin, S.; Focher, F.; Corelli, F.
    Simplified analogues of immucillin-G retain potent human purine nucleoside phosphorylase inhibitory activity (2006), J. Med. Chem., 49, 6037-6045.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
2-amino-1,5-dihydro-7-[[(2S)-2-(aminomethyl)-1-pyrrolidinyl]-methyl]-4H-pyrrolo[3,2-d]pyrimidin-4-one IC50: 600 nM Homo sapiens
2-amino-1,5-dihydro-7-[[(2S)-2-(hydroxymethyl)-1-pyrrolidinyl]methyl]-4H-pyrrolo[3,2-d]pyrimidin-4-one acetic acid salt, IC50: 4.0 nM Homo sapiens
2-amino-1,5-dihydro-7-[[[2-(hydroxy)ethyl]amino]methyl]-4H-pyrrolo[3,2-d]pyrimidin-4-one IC50: 20 nM Homo sapiens
2-amino-7-[[(2-hydroxyethyl)(methyl)amino]methyl]-3,5-dihydro-4H-pyrrolo[3,2-d]pyrimidin-4-one IC50: 60 nM Homo sapiens
2-amino-7-[[(2R)-2-(hydroxymethyl)pyrrolidin-1-yl]methyl]-3,5-dihydro-4H-pyrrolo[3,2-d]pyrimidin-4-one IC50: 620 nM Homo sapiens
2-amino-7-[[(2S)-2-(methoxymethyl)pyrrolidin-1-yl]methyl]-3,5-dihydro-4H-pyrrolo[3,2-d]pyrimidin-4-one IC50: 600 nM Homo sapiens
2-amino-7-[[(2S,4R)-4-hydroxy-2-(hydroxymethyl)pyrrolidin-1-yl]methyl]-3,5-dihydro-4H-pyrrolo[3,2-d]pyrimidin-4-one IC50: 2 nM Homo sapiens
2-amino-7-[[3-(hydroxymethyl)piperidin-1-yl]methyl]-3,5-dihydro-4H-pyrrolo[3,2-d]pyrimidin-4-one IC50: 0.004 mM Homo sapiens
2-amino-7-[[bis(2-hydroxyethyl)amino]methyl]-3,5-dihydro-4H-pyrrolo[3,2-d]pyrimidin-4-one IC50: 5 nM Homo sapiens
2-amino-7-[[ethyl(2-hydroxyethyl)amino]methyl]-3,5-dihydro-4H-pyrrolo[3,2-d]pyrimidin-4-one IC50: 220 nM Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P00491
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
deoxyguanosine + phosphate
-
Homo sapiens guanine + alpha-D-deoxyribose 1-phosphate
-
?

Synonyms

Synonyms Comment Organism
hPNP
-
Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.000001
-
2-amino-7-[[(2S,4R)-4-hydroxy-2-(hydroxymethyl)pyrrolidin-1-yl]methyl]-3,5-dihydro-4H-pyrrolo[3,2-d]pyrimidin-4-one
-
Homo sapiens
0.0000018
-
2-amino-7-[[3-(hydroxymethyl)piperidin-1-yl]methyl]-3,5-dihydro-4H-pyrrolo[3,2-d]pyrimidin-4-one
-
Homo sapiens
0.000002
-
2-amino-1,5-dihydro-7-[[(2S)-2-(hydroxymethyl)-1-pyrrolidinyl]methyl]-4H-pyrrolo[3,2-d]pyrimidin-4-one 37°C, pH 7.0, acetic acid salt Homo sapiens
0.0000025
-
2-amino-7-[[bis(2-hydroxyethyl)amino]methyl]-3,5-dihydro-4H-pyrrolo[3,2-d]pyrimidin-4-one
-
Homo sapiens
0.0000102
-
2-amino-1,5-dihydro-7-[[[2-(hydroxy)ethyl]amino]methyl]-4H-pyrrolo[3,2-d]pyrimidin-4-one 37°C, pH 7.0 Homo sapiens
0.0000306
-
2-amino-7-[[(2-hydroxyethyl)(methyl)amino]methyl]-3,5-dihydro-4H-pyrrolo[3,2-d]pyrimidin-4-one
-
Homo sapiens
0.0001122
-
2-amino-7-[[ethyl(2-hydroxyethyl)amino]methyl]-3,5-dihydro-4H-pyrrolo[3,2-d]pyrimidin-4-one
-
Homo sapiens
0.000306
-
2-amino-1,5-dihydro-7-[[(2S)-2-(aminomethyl)-1-pyrrolidinyl]-methyl]-4H-pyrrolo[3,2-d]pyrimidin-4-one 37°C, pH 7.0 Homo sapiens
0.0003061
-
2-amino-7-[[(2S)-2-(methoxymethyl)pyrrolidin-1-yl]methyl]-3,5-dihydro-4H-pyrrolo[3,2-d]pyrimidin-4-one
-
Homo sapiens
0.0003163
-
2-amino-7-[[(2R)-2-(hydroxymethyl)pyrrolidin-1-yl]methyl]-3,5-dihydro-4H-pyrrolo[3,2-d]pyrimidin-4-one
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000002
-
IC50: 2 nM Homo sapiens 2-amino-7-[[(2S,4R)-4-hydroxy-2-(hydroxymethyl)pyrrolidin-1-yl]methyl]-3,5-dihydro-4H-pyrrolo[3,2-d]pyrimidin-4-one
0.000004
-
acetic acid salt, IC50: 4.0 nM Homo sapiens 2-amino-1,5-dihydro-7-[[(2S)-2-(hydroxymethyl)-1-pyrrolidinyl]methyl]-4H-pyrrolo[3,2-d]pyrimidin-4-one
0.000005
-
IC50: 5 nM Homo sapiens 2-amino-7-[[bis(2-hydroxyethyl)amino]methyl]-3,5-dihydro-4H-pyrrolo[3,2-d]pyrimidin-4-one
0.00002
-
IC50: 20 nM Homo sapiens 2-amino-1,5-dihydro-7-[[[2-(hydroxy)ethyl]amino]methyl]-4H-pyrrolo[3,2-d]pyrimidin-4-one
0.00006
-
IC50: 60 nM Homo sapiens 2-amino-7-[[(2-hydroxyethyl)(methyl)amino]methyl]-3,5-dihydro-4H-pyrrolo[3,2-d]pyrimidin-4-one
0.00022
-
IC50: 220 nM Homo sapiens 2-amino-7-[[ethyl(2-hydroxyethyl)amino]methyl]-3,5-dihydro-4H-pyrrolo[3,2-d]pyrimidin-4-one
0.0006
-
IC50: 600 nM Homo sapiens 2-amino-1,5-dihydro-7-[[(2S)-2-(aminomethyl)-1-pyrrolidinyl]-methyl]-4H-pyrrolo[3,2-d]pyrimidin-4-one
0.0006
-
IC50: 600 nM Homo sapiens 2-amino-7-[[(2S)-2-(methoxymethyl)pyrrolidin-1-yl]methyl]-3,5-dihydro-4H-pyrrolo[3,2-d]pyrimidin-4-one
0.00062
-
IC50: 620 nM Homo sapiens 2-amino-7-[[(2R)-2-(hydroxymethyl)pyrrolidin-1-yl]methyl]-3,5-dihydro-4H-pyrrolo[3,2-d]pyrimidin-4-one
0.004
-
IC50: 0.004 mM Homo sapiens 2-amino-7-[[3-(hydroxymethyl)piperidin-1-yl]methyl]-3,5-dihydro-4H-pyrrolo[3,2-d]pyrimidin-4-one