Literature summary for 1.1.1.205 extracted from

Beevers, R.E.; Buckley, G.M.; Davies, N.; Fraser, J.L.; Galvin, F.C.; Hannah, D.R.; Haughan, A.F.; Jenkins, K.; Mack, S.R.; Pitt, W.R.; Ratcliffe, A.J.; Richard, M.D.; Sabin, V.; Sharpe, A.; Williams, S.C.
Low molecular weight indole fragments as IMPDH inhibitors (2006), Bioorg. Med. Chem. Lett., 16, 2535-2538.

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Inhibitors

Inhibitors	Comment	Organism	Structure
1-phenylsulfonylindol-3-yl boronic acid	-	Homo sapiens
2-methyl-3-(pyrid-4-yl)indole	IC50: 343 nM	Homo sapiens
3-(pyrid-4-yl)indole	-	Homo sapiens
3-carbamoylindole	-	Homo sapiens
3-cyanoindole	inhibits isozyme IMPDH II at 0.03 mM	Homo sapiens
3-formyl-1-methylindole	-	Homo sapiens
3-formylindole	-	Homo sapiens
3-methoxy-4-(oxazol-5-yl)aniline	-	Homo sapiens
4-pyridylindole	IC50: 0.00115 mM	Homo sapiens
BMS-337197	IC50: 0.0082 mM	Homo sapiens
additional information	optimization of nitrile containing drugs, such as VX-148, by combining them with an oxazole moiety which is very reactive in inhibition, overview	Homo sapiens
Mycophenolic acid	potent, uncompetitive, reversible, inhibits both isozymes, prodrug is mycophenolate mofetil	Homo sapiens
VX-148	-	Homo sapiens
VX-497	-	Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates	Organism	Comment (Nat. Sub.)	Natural Products	Comment (Nat. Pro.)	Rev.	Reac.
inosine 5'-phosphate + NAD+ + H2O	Homo sapiens	rate-limiting step of the de novo guanine nucleotide biosynthesis	xanthosine 5'-phosphate + NADH	-	?

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	-	type I and type II isozymes	-

Source Tissue

Source Tissue	Comment	Organism	Textmining
B-lymphocyte	-	Homo sapiens	-
T-lymphocyte	-	Homo sapiens	-

Substrates and Products (Substrate)

Substrates	Comment Substrates	Organism	Products	Comment (Products)	Rev.	Reac.
inosine 5'-phosphate + NAD+ + H2O	-	Homo sapiens	xanthosine 5'-phosphate + NADH	-	?
inosine 5'-phosphate + NAD+ + H2O	rate-limiting step of the de novo guanine nucleotide biosynthesis	Homo sapiens	xanthosine 5'-phosphate + NADH	-	?

Synonyms

Synonyms	Comment	Organism
IMPDH	-	Homo sapiens
inosine monophosphate dehydrogenase	-	Homo sapiens

Cofactor

Cofactor	Comment	Organism	Structure
NAD+	dependent on	Homo sapiens

IC50 Value

IC50 Value	IC50 Value Maximum	Comment	Organism	Inhibitor	Structure
0.000343	-	IC50: 343 nM	Homo sapiens	2-methyl-3-(pyrid-4-yl)indole
0.00115	-	IC50: 0.00115 mM	Homo sapiens	4-pyridylindole
0.0082	-	IC50: 0.0082 mM	Homo sapiens	BMS-337197

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Release 2023.1 (January 2023)