Target Information
| Target General Information | Top | |||||
|---|---|---|---|---|---|---|
| Target ID |
T28925
(Former ID: TTDI01771)
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| Target Name |
Inosine-5'-monophosphate dehydrogenase (IMPDH)
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| Gene Name |
NO-GeName
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| Target Type |
Successful target
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[1] | ||||
| Disease | [+] 2 Target-related Diseases | + | ||||
| 1 | Acute myeloid leukaemia [ICD-11: 2A60] | |||||
| 2 | Transplant rejection [ICD-11: NE84] | |||||
| BioChemical Class |
Short-chain dehydrogenases reductase
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| UniProt ID | ||||||
| Drugs and Modes of Action | Top | |||||
|---|---|---|---|---|---|---|
| Approved Drug(s) | [+] 2 Approved Drugs | + | ||||
| 1 | Enteric-coated mycophenolate sodium | Drug Info | Approved | Transplant rejection | [2] | |
| 2 | Thioguanine | Drug Info | Approved | Acute myeloid leukaemia | [3], [4] | |
| Clinical Trial Drug(s) | [+] 1 Clinical Trial Drugs | + | ||||
| 1 | VX-944 | Drug Info | Phase 2 | Solid tumour/cancer | [5] | |
| Discontinued Drug(s) | [+] 2 Discontinued Drugs | + | ||||
| 1 | IMS | Drug Info | Discontinued in Phase 1 | Inflammatory bowel disease | [6] | |
| 2 | R-1518 | Drug Info | Discontinued in Phase 1 | Hepatitis C virus infection | [7] | |
| Mode of Action | [+] 3 Modes of Action | + | ||||
| Inhibitor | [+] 2 Inhibitor drugs | + | ||||
| 1 | Enteric-coated mycophenolate sodium | Drug Info | [1], [2] | |||
| 2 | VX-944 | Drug Info | [9] | |||
| Intercalator | [+] 1 Intercalator drugs | + | ||||
| 1 | Thioguanine | Drug Info | [8] | |||
| Modulator | [+] 3 Modulator drugs | + | ||||
| 1 | IMS | Drug Info | [10] | |||
| 2 | R-1518 | Drug Info | [11] | |||
| 3 | EPB-415 | Drug Info | [12] | |||
| Chemical Structure based Activity Landscape of Target | Top |
|---|---|
| Drug Property Profile of Target | Top | |
|---|---|---|
| (1) Molecular Weight (mw) based Drug Clustering | (2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering | |
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| (3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering | (4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering | |
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| (5) Rotatable Bond Count (rotbonds) based Drug Clustering | (6) Topological Polar Surface Area (polararea) based Drug Clustering | |
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| "RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five | ||
| Co-Targets | Top | |||||
|---|---|---|---|---|---|---|
| Co-Targets | ||||||
| Target Poor or Non Binders | Top | |||||
|---|---|---|---|---|---|---|
| Target Poor or Non Binders | ||||||
| Target Affiliated Biological Pathways | Top | |||||
|---|---|---|---|---|---|---|
| KEGG Pathway | [+] 3 KEGG Pathways | + | ||||
| 1 | Purine metabolism | |||||
| 2 | Drug metabolism - other enzymes | |||||
| 3 | Metabolic pathways | |||||
| Pathwhiz Pathway | [+] 1 Pathwhiz Pathways | + | ||||
| 1 | Purine Metabolism | |||||
| Reactome | [+] 1 Reactome Pathways | + | ||||
| 1 | Purine ribonucleoside monophosphate biosynthesis | |||||
| WikiPathways | [+] 1 WikiPathways | + | ||||
| 1 | Nucleotide Metabolism | |||||
| References | Top | |||||
|---|---|---|---|---|---|---|
| REF 1 | Mycophenolate mofetil, an inhibitor of inosine monophosphate dehydrogenase, causes a paradoxical elevation of GTP in erythrocytes of renal transplant patients. Clin Sci (Lond). 2004 Jul;107(1):63-8. | |||||
| REF 2 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 | |||||
| REF 3 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6845). | |||||
| REF 4 | Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77. | |||||
| REF 5 | ClinicalTrials.gov (NCT00493441) AVN944 in Combination With Gemcitabine for the Treatment of Pancreatic Cancer. U.S. National Institutes of Health. | |||||
| REF 6 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800019853) | |||||
| REF 7 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800018979) | |||||
| REF 8 | Immune effector cells produce lethal DNA damage in cells treated with a thiopurine. Cancer Res. 2009 Mar 15;69(6):2393-9. | |||||
| REF 9 | Novel inosine monophosphate dehydrogenase inhibitor VX-944 induces apoptosis in multiple myeloma cells primarily via caspase-independent AIF/Endo G pathway. Oncogene. 2005 Sep 1;24(38):5888-96. | |||||
| REF 10 | The novel inosine analogue INO-2002 exerts an anti-inflammatory effect in a murine model of acute lung injury. Shock. 2009 Sep;32(3):258-62. | |||||
| REF 11 | US patent application no. 2010,0092,479, Compositions and methods for treatment of viral diseases. | |||||
| REF 12 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 2625). | |||||
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