Target Validation Information
Target ID T89360
Target Name Inosine-5'-monophosphate dehydrogenase 2
Target Type
Successful
Drug Potency against Target 2-Benzyl-6-methoxy-5-oxazol-5-yl-1H-indole Drug Info IC50 = 600 nM [526581]
3-methoxy-4-(oxazol-5-yl)aniline Drug Info IC50 = 8200 nM [528040]
N-benzyl-9-oxo-9,10-dihydroacridine-3-carboxamide Drug Info IC50 = 2200 nM [528916]
6-bromo-3-(pyridin-4-yl)-1H-indole Drug Info IC50 = 408 nM [528040]
Mycophenolic hydroxamic acid Drug Info IC50 = 420 nM [531203]
Mycophenolic bis(sulfonamide) Drug Info Ki = 4000 nM [529565]
Tiazofurin adenine dinucleotide Drug Info Ki = 100 nM [529172]
Mycophenolate mofetil Drug Info IC50 = 0~724 m uMol/L [553184]
Ethyl 3-(pyridin-4-yl)-1H-indole-6-carboxylate Drug Info IC50 = 586 nM [528041]
1-methoxy-3-(3-(pyridin-4-yl)-1H-indol-6-yl)urea Drug Info IC50 = 1110 nM [528041]
3-(furan-3-yl)-1-methyl-1H-indole Drug Info IC50 = 6210 nM [528040]
3-(thiophen-3-yl)-1H-indol-6-amine Drug Info IC50 = 2320 nM [528040]
3-(pyridin-4-yl)-1H-indol-7-amine Drug Info IC50 = 524 nM [528040]
2-methyl-3-(pyridin-4-yl)-1H-indole Drug Info IC50 = 343 nM [528040]
3-(pyridin-4-yl)-1H-indole Drug Info IC50 = 1150 nM [528041]
1-(3-cyano-1-methyl-1H-indol-6-yl)-3-phenylurea Drug Info IC50 = 722 nM [528041]
2-methyl-3-(pyridin-4-yl)-1H-indol-6-amine Drug Info IC50 = 419 nM [528040]
3-(furan-3-yl)-1H-indole Drug Info IC50 = 5840 nM [528040]
1-methyl-1H-indole-3-carbaldehyde Drug Info IC50 = 6840 nM [528040]
6-phenyl-3-(pyridin-4-yl)-1H-indole Drug Info IC50 = 456 nM [528041]
3-(3-cyano-1H-indol-6-yl)-1-methyl-1-phenylurea Drug Info IC50 = 15400 nM [528041]
1-methyl-1H-indole-3-carbonitrile Drug Info IC50 = 7660 nM [528041]
3-(pyridin-4-yl)-1H-indol-6-amine Drug Info IC50 = 637 nM [528040]
6-Methoxy-5-oxazol-5-yl-2-phenyl-1H-indole Drug Info IC50 = 500 nM [526581]
Action against Disease Model Mycophenolate mofetil IC50 on mitogen-induced h uMan mesangial cell proliferation: 190nM [552177] Drug Info
Mycophenolate mofetil 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 [537158] Drug Info
References
Ref 552177Mycophenolate mofetil inhibits rat and human mesangial cell proliferation by guanosine depletion. Nephrol Dial Transplant. 1999 Jan;14(1):58-63.
Ref 537158Effect of mycophenolate acyl-glucuronide on human recombinant type 2 inosine monophosphate dehydrogenase. Clin Chem. 2009 May;55(5):986-93. Epub 2009 Mar 19.
Ref 526581Bioorg 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.
Ref 528040Bioorg Med Chem Lett. 2006 May 1;16(9):2535-8. Epub 2006 Feb 17.Low molecular weight indole fragments as IMPDH inhibitors.
Ref 528916J 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).
Ref 528040Bioorg Med Chem Lett. 2006 May 1;16(9):2535-8. Epub 2006 Feb 17.Low molecular weight indole fragments as IMPDH inhibitors.
Ref 531203Bioorg 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 amongthe mycophenolic acid derivatives.
Ref 529565Bioorg 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.
Ref 529172J 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.
Ref 553184Mycophenolic acid binding to human serum albumin: characterization and relation to pharmacodynamics. Clin Chem. 1995 Jul;41(7):1011-7.
Ref 528041Bioorg 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.
Ref 528041Bioorg 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.
Ref 528040Bioorg Med Chem Lett. 2006 May 1;16(9):2535-8. Epub 2006 Feb 17.Low molecular weight indole fragments as IMPDH inhibitors.
Ref 528040Bioorg Med Chem Lett. 2006 May 1;16(9):2535-8. Epub 2006 Feb 17.Low molecular weight indole fragments as IMPDH inhibitors.
Ref 528040Bioorg Med Chem Lett. 2006 May 1;16(9):2535-8. Epub 2006 Feb 17.Low molecular weight indole fragments as IMPDH inhibitors.
Ref 528040Bioorg Med Chem Lett. 2006 May 1;16(9):2535-8. Epub 2006 Feb 17.Low molecular weight indole fragments as IMPDH inhibitors.
Ref 528041Bioorg 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.
Ref 528041Bioorg 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.
Ref 528040Bioorg Med Chem Lett. 2006 May 1;16(9):2535-8. Epub 2006 Feb 17.Low molecular weight indole fragments as IMPDH inhibitors.
Ref 528040Bioorg Med Chem Lett. 2006 May 1;16(9):2535-8. Epub 2006 Feb 17.Low molecular weight indole fragments as IMPDH inhibitors.
Ref 528040Bioorg Med Chem Lett. 2006 May 1;16(9):2535-8. Epub 2006 Feb 17.Low molecular weight indole fragments as IMPDH inhibitors.
Ref 528041Bioorg 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.
Ref 528041Bioorg 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.
Ref 528041Bioorg 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.
Ref 528040Bioorg Med Chem Lett. 2006 May 1;16(9):2535-8. Epub 2006 Feb 17.Low molecular weight indole fragments as IMPDH inhibitors.
Ref 526581Bioorg 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.

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