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Literature summary for 1.1.1.205 extracted from

  • Dhar, T.G.M.; Shen, Z.; Gu, H.H.; Chen, P.; Norris, D.; Watterson, S.H.; Ballentine, S.K.; Fleener, C.A.; Rouleau, K.A.; Barrish, J.C.; Townsend, R.; Hollenbaugh, D.L.; Iwanowicz, E.J.
    3-Cyanoindole-based inhibitors of inosine monophosphate dehydrogenase: synthesis and initial structureactivity relationships (2003), Bioorg. Med. Chem. Lett., 13, 3557-3560.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
3-cyanoindole-based inhibitors synthesis and initial structure–activity relationships of 3-cyanoindole-based inhibitors with isozyme IMPDH II, IC50: 33-420 nM, comparison to other inhibitor structural classes, overview Homo sapiens
BMS-337197 isozyme IMPDH II IC50: 16 nM Homo sapiens
Mycophenolic acid isozyme IMPDH II IC50: 15 nM Homo sapiens
VX-148 isozyme IMPDH II IC50: 6 nM Homo sapiens
VX-497 isozyme IMPDH II IC50: 11 nM 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
-
ir

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
IMPDH II
-

Source Tissue

Source Tissue Comment Organism Textmining
lymphocyte peripheral blood lymphocytes 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
-
ir
inosine 5'-phosphate + NAD+ + H2O rate-limiting step of the de novo guanine nucleotide biosynthesis Homo sapiens xanthosine 5'-phosphate + NADH
-
ir

Synonyms

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

Cofactor

Cofactor Comment Organism Structure
NAD+
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000006
-
isozyme IMPDH II IC50: 6 nM Homo sapiens VX-148
0.000011
-
isozyme IMPDH II IC50: 11 nM Homo sapiens VX-497
0.000015
-
isozyme IMPDH II IC50: 15 nM Homo sapiens Mycophenolic acid
0.000016
-
isozyme IMPDH II IC50: 16 nM Homo sapiens BMS-337197
0.000033 0.00042 synthesis and initial structure–activity relationships of 3-cyanoindole-based inhibitors with isozyme IMPDH II, IC50: 33-420 nM, comparison to other inhibitor structural classes, overview Homo sapiens 3-cyanoindole-based inhibitors