Target Information
| Target General Information | Top | |||||
|---|---|---|---|---|---|---|
| Target ID |
T48940
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| Target Name |
HIF-prolyl hydroxylase (HPH)
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| Gene Name |
NO-GeName
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| Target Type |
Successful target
|
[1] | ||||
| Disease | [+] 1 Target-related Diseases | + | ||||
| 1 | Fungal infection [ICD-11: 1F29-1F2F] | |||||
| UniProt ID | ||||||
| Drugs and Modes of Action | Top | |||||
|---|---|---|---|---|---|---|
| Approved Drug(s) | [+] 1 Approved Drugs | + | ||||
| 1 | Ciclopirox | Drug Info | Approved | Fungal infection | [2] | |
| Clinical Trial Drug(s) | [+] 6 Clinical Trial Drugs | + | ||||
| 1 | AKB-6548 | Drug Info | Phase 3 | Anaemia | [3] | |
| 2 | BAY 853934 | Drug Info | Phase 3 | Anaemia | [4] | |
| 3 | JTZ-951 | Drug Info | Phase 3 | Anaemia | [5] | |
| 4 | FG-2216 | Drug Info | Phase 2 | Kidney disease | [6] | |
| 5 | DS-1093 | Drug Info | Phase 1 | Anemia | [7] | |
| 6 | ZYAN1 | Drug Info | Phase 1 | Anaemia | [8] | |
| Preclinical Drug(s) | [+] 1 Preclinical Drugs | + | ||||
| 1 | JNJ-42905343 | Drug Info | Preclinical | Anaemia | [8] | |
| Mode of Action | [+] 2 Modes of Action | + | ||||
| Modulator | [+] 5 Modulator drugs | + | ||||
| 1 | Ciclopirox | Drug Info | [1] | |||
| 2 | AKB-6548 | Drug Info | [9] | |||
| 3 | JTZ-951 | Drug Info | [11] | |||
| 4 | FG-2216 | Drug Info | [12] | |||
| 5 | DS-1093 | Drug Info | [13] | |||
| Inhibitor | [+] 3 Inhibitor drugs | + | ||||
| 1 | BAY 853934 | Drug Info | [10] | |||
| 2 | ZYAN1 | Drug Info | [14] | |||
| 3 | JNJ-42905343 | Drug Info | [15] | |||
| 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 Profiles in Patients | Top | |||||
|---|---|---|---|---|---|---|
| Target Expression Profile (TEP) | ||||||
| References | Top | |||||
|---|---|---|---|---|---|---|
| REF 1 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. | |||||
| REF 2 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 076435. | |||||
| REF 3 | ClinicalTrials.gov (NCT03242967) Study to Evaluate Three Times Per Week (TIW) Oral Dosing of Vadadustat for Anemia in Subjects With Dialysis-Dependent Chronic Kidney Disease (DD-CKD) (TRILOGY). U.S. National Institutes of Health. | |||||
| REF 4 | ClinicalTrials.gov (NCT03418168) A Study of Molidustat for Treatment of Renal Anemia in Peritoneal Dialysis Subjects (MIYABI PD). U.S. National Institutes of Health. | |||||
| REF 5 | ClinicalTrials.gov (NCT04027517) A Study to Evaluate Efficacy and Safety of JTZ-951 Compared to Darbepoetin Alfa in Korean Renal Anemia Patients Receiving Hemodialysis.. 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 800018242) | |||||
| REF 7 | ClinicalTrials.gov (NCT02299661) Pilot PK/PD Study of DS-1093a in Patients With Chronic Kidney Disease. U.S. National Institutes of Health. | |||||
| REF 8 | Targeting iron metabolism in drug discovery and delivery. Nat Rev Drug Discov. 2017 Jun;16(6):400-423. | |||||
| REF 9 | DOI: 10.1038/nrd4422 | |||||
| REF 10 | Discovery of Molidustat (BAY 85-3934): A Small-Molecule Oral HIF-Prolyl Hydroxylase (HIF-PH) Inhibitor for the Treatment of Renal Anemia. ChemMedChem. 2018 May 23;13(10):988-1003. | |||||
| REF 11 | DOI: 10.1038/nrneph.2015.82 | |||||
| REF 12 | Inhibition of Prolyl Hydroxylases Increases Erythropoietin Production in ESRD | |||||
| REF 13 | Company report (Daiichisankyo) | |||||
| REF 14 | Pharmacological Characterization of ZYAN1, a Novel Prolyl Hydroxylase Inhibitor for the Treatment of Anemia. Drug Res (Stuttg). 2016 Feb;66(2):107-12. | |||||
| REF 15 | Prolyl hydroxylase inhibition corrects functional iron deficiency and inflammation-induced anaemia in rats. Br J Pharmacol. 2015 Aug;172(16):4078-88. | |||||
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