Target Validation Information
TTD ID T89360
Target Name Inosine-5'-monophosphate dehydrogenase 2 (IMPDH2)
Type of Target
Successful
Drug Potency against Target Mycophenolate mofetil Drug Info IC50 = 0~724 m uMol/L [10]
1-(3-cyano-1-methyl-1H-indol-6-yl)-3-phenylurea Drug Info IC50 = 722 nM [3]
1-methoxy-3-(3-(pyridin-4-yl)-1H-indol-6-yl)urea Drug Info IC50 = 1110 nM [3]
1-methyl-1H-indole-3-carbaldehyde Drug Info IC50 = 6840 nM [2]
1-methyl-1H-indole-3-carbonitrile Drug Info IC50 = 7660 nM [3]
2-Benzyl-6-methoxy-5-oxazol-5-yl-1H-indole Drug Info IC50 = 600 nM [1]
2-methyl-3-(pyridin-4-yl)-1H-indol-6-amine Drug Info IC50 = 419 nM [2]
2-methyl-3-(pyridin-4-yl)-1H-indole Drug Info IC50 = 343 nM [2]
3-(3-cyano-1H-indol-6-yl)-1-methyl-1-phenylurea Drug Info IC50 = 15400 nM [3]
3-(furan-3-yl)-1-methyl-1H-indole Drug Info IC50 = 6210 nM [2]
3-(furan-3-yl)-1H-indole Drug Info IC50 = 5840 nM [2]
3-(pyridin-4-yl)-1H-indol-6-amine Drug Info IC50 = 637 nM [2]
3-(pyridin-4-yl)-1H-indol-7-amine Drug Info IC50 = 524 nM [2]
3-(thiophen-3-yl)-1H-indol-6-amine Drug Info IC50 = 2320 nM [2]
3-methoxy-4-(oxazol-5-yl)aniline Drug Info IC50 = 8200 nM [2]
6-bromo-3-(pyridin-4-yl)-1H-indole Drug Info IC50 = 408 nM [2]
6-Methoxy-5-oxazol-5-yl-2-phenyl-1H-indole Drug Info IC50 = 500 nM [1]
6-phenyl-3-(pyridin-4-yl)-1H-indole Drug Info IC50 = 456 nM [3]
Ethyl 3-(pyridin-4-yl)-1H-indole-6-carboxylate Drug Info IC50 = 586 nM [3]
Mycophenolic bis(sulfonamide) Drug Info Ki = 4000 nM [6]
Mycophenolic hydroxamic acid Drug Info IC50 = 420 nM [7]
N-benzyl-9-oxo-9,10-dihydroacridine-3-carboxamide Drug Info IC50 = 2200 nM [4]
Rockout Drug Info IC50 = 1150 nM [3]
Tiazofurin adenine dinucleotide Drug Info Ki = 100 nM [5]
Action against Disease Model Mycophenolate mofetil Drug Info IC50 on mitogen-induced h uMan mesangial cell proliferation: 190nM [9]
Mycophenolate mofetil Drug Info We measured intracellular and extracellular concentrations of MPA. After incubation of Jurkat lymphoma cells with each compound separately, using liquid chromatography-tandem mass spectrometry.RESULTS: MPA showed an inhibition of rhIMPDH II (IC(50) 25.6 microg/L [8]
References
REF 1 Novel indole-based inhibitors of IMPDH: introduction of hydrogen bond acceptors at indole C-3. Bioorg Med Chem Lett. 2003 Apr 7;13(7):1273-6.
REF 2 Low molecular weight indole fragments as IMPDH inhibitors. Bioorg Med Chem Lett. 2006 May 1;16(9):2535-8.
REF 3 Novel indole inhibitors of IMPDH from fragments: synthesis and initial structure-activity relationships. Bioorg Med Chem Lett. 2006 May 1;16(9):2539-42.
REF 4 Acridone-based inhibitors of inosine 5'-monophosphate dehydrogenase: discovery and SAR leading to the identification of N-(2-(6-(4-ethylpiperazin-1... J Med Chem. 2007 Jul 26;50(15):3730-42.
REF 5 Dual inhibitors of inosine monophosphate dehydrogenase and histone deacetylases for cancer treatment. J Med Chem. 2007 Dec 27;50(26):6685-91.
REF 6 Bis(sulfonamide) isosters of mycophenolic adenine dinucleotide analogues: inhibition of inosine monophosphate dehydrogenase. Bioorg Med Chem. 2008 Aug 1;16(15):7462-9.
REF 7 Structure-activity relationships for inhibition of inosine monophosphate dehydrogenase and differentiation induction of K562 cells among the mycoph... Bioorg Med Chem. 2010 Nov 15;18(22):8106-11.
REF 8 Effect of mycophenolate acyl-glucuronide on human recombinant type 2 inosine monophosphate dehydrogenase. Clin Chem. 2009 May;55(5):986-93.
REF 9 Mycophenolate mofetil inhibits rat and human mesangial cell proliferation by guanosine depletion. Nephrol Dial Transplant. 1999 Jan;14(1):58-63.
REF 10 Mycophenolic acid binding to human serum albumin: characterization and relation to pharmacodynamics. Clin Chem. 1995 Jul;41(7):1011-7.

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