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Literature summary for 2.4.2.1 extracted from

  • Castilho, M.S.; Postigo, M.P.; Pereira, H.M.; Oliva, G.; Andricopulo, A.D.
    Structural basis for selective inhibition of purine nucleoside phosphorylase from Schistosoma mansoni: kinetic and structural studies (2010), Bioorg. Med. Chem., 18, 1421-1427.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
2-amino-7-(pyridin-2-ylmethyl)-3,5-dihydro-4H-pyrrolo[3,2-d]pyrimidin-4-one
-
Homo sapiens
2-amino-7-(pyridin-2-ylmethyl)-3,5-dihydro-4H-pyrrolo[3,2-d]pyrimidin-4-one
-
Schistosoma mansoni
2-amino-7-[4-(benzyloxy)benzyl]-3,5-dihydro-4H-pyrrolo[3,2-d]pyrimidin-4-one
-
Homo sapiens
2-amino-7-[4-(benzyloxy)benzyl]-3,5-dihydro-4H-pyrrolo[3,2-d]pyrimidin-4-one
-
Schistosoma mansoni
2-amino-7-[4-(propan-2-yl)benzyl]-3,5-dihydro-4H-pyrrolo[3,2-d]pyrimidin-4-one 1.8fold selectivity for Schistosoma enzyme over human enzyme Homo sapiens
2-amino-7-[4-(propan-2-yl)benzyl]-3,5-dihydro-4H-pyrrolo[3,2-d]pyrimidin-4-one 1.8fold selectivity for Schistosoma enzyme over human enzyme Schistosoma mansoni
3-[(2R,5S)-3,4-dihydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl]-3,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one 6.4fold selectivity for Schistosoma enzyme over human enzyme Homo sapiens
3-[(2R,5S)-3,4-dihydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl]-3,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one 6.4fold selectivity for Schistosoma enzyme over human enzyme Schistosoma mansoni

Organism

Organism UniProt Comment Textmining
Homo sapiens P00491
-
-
Schistosoma mansoni
-
-
-

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000023
-
pH 7.4, 25°C Homo sapiens 2-amino-7-(pyridin-2-ylmethyl)-3,5-dihydro-4H-pyrrolo[3,2-d]pyrimidin-4-one
0.00015
-
pH 7.4, 25°C Schistosoma mansoni 2-amino-7-[4-(propan-2-yl)benzyl]-3,5-dihydro-4H-pyrrolo[3,2-d]pyrimidin-4-one
0.00027
-
pH 7.4, 25°C Homo sapiens 2-amino-7-[4-(propan-2-yl)benzyl]-3,5-dihydro-4H-pyrrolo[3,2-d]pyrimidin-4-one
0.0003
-
pH 7.4, 25°C Homo sapiens 2-amino-7-[4-(benzyloxy)benzyl]-3,5-dihydro-4H-pyrrolo[3,2-d]pyrimidin-4-one
0.0005
-
pH 7.4, 25°C Schistosoma mansoni 2-amino-7-[4-(benzyloxy)benzyl]-3,5-dihydro-4H-pyrrolo[3,2-d]pyrimidin-4-one
0.007
-
pH 7.4, 25°C Schistosoma mansoni 2-amino-7-(pyridin-2-ylmethyl)-3,5-dihydro-4H-pyrrolo[3,2-d]pyrimidin-4-one
0.047
-
pH 7.4, 25°C Schistosoma mansoni 3-[(2R,5S)-3,4-dihydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl]-3,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one
0.3
-
pH 7.4, 25°C Homo sapiens 3-[(2R,5S)-3,4-dihydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl]-3,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one