Therapeutic Targets Database
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Target Validation Information
TTD IDTTDS00063
Target NameInosine-5'-monophosphate dehydrogenase 2    
Type of TargetSuccessful target    
Drug Potency against TargetMycophenolate mofetilIC50 = 0~724 m uMol/L[1]
Mycophenolic acidIC50 = 0~724 m uMol/L[1]
1-methoxy-3-(3-(pyridin-4-yl)-1H-indol-6-yl)ureaIC50 = 1110 nM[2]
3-(pyridin-4-yl)-1H-indoleIC50 = 1150 nM[2]
3-(3-cyano-1H-indol-6-yl)-1-methyl-1-phenylureaIC50 = 15400 nM[2]
N-benzyl-9-oxo-9,10-dihydroacridine-3-carboxamideIC50 = 2200 nM[3]
3-(thiophen-3-yl)-1H-indol-6-amineIC50 = 2320 nM[4]
2-methyl-3-(pyridin-4-yl)-1H-indoleIC50 = 343 nM[4]
6-bromo-3-(pyridin-4-yl)-1H-indoleIC50 = 408 nM[4]
2-methyl-3-(pyridin-4-yl)-1H-indol-6-amineIC50 = 419 nM[4]
mycophenolic hydroxamic acidIC50 = 420 nM[5]
6-phenyl-3-(pyridin-4-yl)-1H-indoleIC50 = 456 nM[2]
6-Methoxy-5-oxazol-5-yl-2-phenyl-1H-indoleIC50 = 500 nM[6]
3-(pyridin-4-yl)-1H-indol-7-amineIC50 = 524 nM[4]
3-(furan-3-yl)-1H-indoleIC50 = 5840 nM[4]
ethyl 3-(pyridin-4-yl)-1H-indole-6-carboxylateIC50 = 586 nM[2]
2-Benzyl-6-methoxy-5-oxazol-5-yl-1H-indoleIC50 = 600 nM[6]
3-(furan-3-yl)-1-methyl-1H-indoleIC50 = 6210 nM[4]
3-(pyridin-4-yl)-1H-indol-6-amineIC50 = 637 nM[4]
1-methyl-1H-indole-3-carbaldehydeIC50 = 6840 nM[4]
1-(3-cyano-1-methyl-1H-indol-6-yl)-3-phenylureaIC50 = 722 nM[2]
1-methyl-1H-indole-3-carbonitrileIC50 = 7660 nM[2]
3-methoxy-4-(oxazol-5-yl)anilineIC50 = 8200 nM[4]
tiazofurin adenine dinucleotideKi = 100 nM[7]
Mycophenolic bis(sulfonamide)Ki = 4000 nM[8]
Action against Disease ModelMycophenolate mofetilIC50 on mitogen-induced h uMan mesangial cell proliferation: 190nM[9]
Mycophenolic acidWe 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[10]
Ref 1Clin Chem. 1995 Jul;41(7):1011-7.Mycophenolic acid binding to human serum albumin: characterization and relation to pharmacodynamics. To Reference
Ref 2Bioorg Med Chem Lett. 2006 May 1;16(9):2539-42. Epub 2006 Feb 17.Novel indole inhibitors of IMPDH from fragments: synthesis and initial structure-activity relationships. To Reference
Ref 3J Med Chem. 2007 Jul 26;50(15):3730-42. Epub 2007 Jun 22.Acridone-based inhibitors of inosine 5'-monophosphate dehydrogenase: discovery and SAR leading to the identification of N-(2-(6-(4-ethylpiperazin-1-yl)pyridin-3-yl)propan-2-yl)-2- fluoro-9-oxo-9,10-dihydroacridine-3-carboxamide (BMS-566419). To Reference
Ref 4Bioorg Med Chem Lett. 2006 May 1;16(9):2535-8. Epub 2006 Feb 17.Low molecular weight indole fragments as IMPDH inhibitors. To Reference
Ref 5Bioorg Med Chem. 2010 Nov 15;18(22):8106-11. Epub 2010 Sep 18.Structure-activity relationships for inhibition of inosine monophosphate dehydrogenase and differentiation induction of K562 cells among the mycophenolic acid derivatives. To Reference
Ref 6Bioorg Med Chem Lett. 2003 Apr 7;13(7):1273-6.Novel indole-based inhibitors of IMPDH: introduction of hydrogen bond acceptors at indole C-3. To Reference
Ref 7J Med Chem. 2007 Dec 27;50(26):6685-91. Epub 2007 Nov 27.Dual inhibitors of inosine monophosphate dehydrogenase and histone deacetylases for cancer treatment. To Reference
Ref 8Bioorg Med Chem. 2008 Aug 1;16(15):7462-9. Epub 2008 Jun 10.Bis(sulfonamide) isosters of mycophenolic adenine dinucleotide analogues: inhibition of inosine monophosphate dehydrogenase. To Reference
Ref 9Nephrol Dial Transplant. 1999 Jan;14(1):58-63.Mycophenolate mofetil inhibits rat and human mesangial cell proliferation by guanosine depletion. To Reference
Ref 10Clin Chem. 2009 May;55(5):986-93. Epub 2009 Mar 19.Effect of mycophenolate acyl-glucuronide on human recombinant type 2 inosine monophosphate dehydrogenase. To Reference



 

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