Literature summary extracted from

Clinch, K.; Evans, G.B.; Froehlich, R.F.; Furneaux, R.H.; Kelly, P.M.; Legentil, L.; Murkin, A.S.; Li, L.; Schramm, V.L.; Tyler, P.C.; Woolhouse, A.D.
Third-generation immucillins: syntheses and bioactivities of acyclic immucillin inhibitors of human purine nucleoside phosphorylase (2009), J. Med. Chem., 52, 1126-1143.

Inhibitors

EC Number	Inhibitors	Comment	Organism	Structure
2.4.2.1	2-amino-7-([[(2R,3S)-1,3,4-trihydroxybutan-2-yl]amino]methyl)-3,5-dihydro-4Hpyrrolo[3,2-d]pyrimidin-4-one	i.e. DATMe-immucillin-G	Homo sapiens
2.4.2.1	2-amino-7-[[(1,3-dihydroxypropan-2-yl)amino]methyl]-3,5-dihydro-4H-pyrrolo[3,2-d]pyrimidin-4-one	i.e. SerMe-immucillin-G	Homo sapiens
2.4.2.1	7-[[(1,3-dihydroxypropan-2-yl)amino]methyl]-3,5-dihydro-4H-pyrrolo[3,2-d]pyrimidin-4-one	i.e. SerMe-immucillin-H. Kd-value 5.2 pM	Homo sapiens
2.4.2.1	7-[[(1,3-dihydroxypropan-2-yl)amino]methyl]-3,5-dihydro-4H-pyrrolo[3,2-d]pyrimidin-4-one	i.e. SerMe-immucillin-H. Inhibitor is orally available with a long residence time on blood enzyme	Mus musculus
2.4.2.1	immucillin-H	-	Homo sapiens

Organism

EC Number	Organism	UniProt	Comment	Textmining
2.4.2.1	Homo sapiens	-	-	-
2.4.2.1	Mus musculus	-	-	-

Substrates and Products (Substrate)

EC Number	Substrates	Comment Substrates	Organism	Products	Comment (Products)	Rev.	Reac.
2.4.2.1	inosine + phosphate	-	Mus musculus	hypoxanthine + alpha-D-ribose 1-phosphate	-	?
2.4.2.1	inosine + phosphate	-	Homo sapiens	hypoxanthine + alpha-D-ribose 1-phosphate	-	?

Ki Value [mM]

EC Number	Ki Value [mM]	Ki Value maximum [mM]	Inhibitor	Comment	Organism	Structure
2.4.2.1	0.0000000021	-	2-amino-7-[[(1,3-dihydroxypropan-2-yl)amino]methyl]-3,5-dihydro-4H-pyrrolo[3,2-d]pyrimidin-4-one	-	Homo sapiens
2.4.2.1	0.0000000034	-	2-amino-7-([[(2R,3S)-1,3,4-trihydroxybutan-2-yl]amino]methyl)-3,5-dihydro-4Hpyrrolo[3,2-d]pyrimidin-4-one	-	Homo sapiens

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Release 2023.1 (January 2023)