enarodustat   Click here for help

GtoPdb Ligand ID: 11828

Synonyms: compound 14 [PMID: 29259755] | Enaroy® | JTZ-951 | JTZ951
Approved drug
enarodustat is an approved drug
Compound class: Synthetic organic
Comment: Enarodustat (JTZ-951) is an orally active inhibitor of hypoxia-inducible factor prolyl hydroxylase (HIF-PH) enzyme activity [3]. Inhibition of prolyl hydroxylation of HIF transcription factors is used as an alternative to erythropoiesis-stimulating agents (epoetin, darbepoetin) for the treatment of anaemia resulting from chronic kidnery disease [1,4].
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2D Structure
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Physico-chemical Properties
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Hydrogen bond acceptors 5
Hydrogen bond donors 3
Rotatable bonds 7
Topological polar surface area 116.56
Molecular weight 340.12
XLogP 2.55
No. Lipinski's rules broken 0
SMILES / InChI / InChIKey
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Canonical SMILES OC(=O)CNC(=O)c1c(=O)cc(n2c1nc[nH]2)CCc1ccccc1
Isomeric SMILES c1ccc(cc1)CCc1cc(=O)c(c2n1[nH]cn2)C(=O)NCC(=O)O
InChI InChI=1S/C17H16N4O4/c22-13-8-12(7-6-11-4-2-1-3-5-11)21-16(19-10-20-21)15(13)17(25)18-9-14(23)24/h1-5,8,10H,6-7,9H2,(H,18,25)(H,19,20)(H,23,24)
InChI Key FJYRBJKWDXVHHO-UHFFFAOYSA-N
References
1. Fukui K, Shinozaki Y, Kobayashi H, Deai K, Yoshiuchi H, Matsui T, Matsuo A, Matsushita M, Tanaka T, Nangaku M. (2019)
JTZ-951 (enarodustat), a hypoxia-inducibe factor prolyl hydroxylase inhibitor, stabilizes HIF-α protein and induces erythropoiesis without effects on the function of vascular endothelial growth factor.
Eur J Pharmacol, 859: 172532. [PMID:31301309]
2. Markham A. (2021)
Enarodustat: First Approval.
Drugs, 81 (1): 169-174. [PMID:33320297]
3. Ogoshi Y, Matsui T, Mitani I, Yokota M, Terashita M, Motoda D, Ueyama K, Hotta T, Ito T, Hase Y et al.. (2017)
Discovery of JTZ-951: A HIF Prolyl Hydroxylase Inhibitor for the Treatment of Renal Anemia.
ACS Med Chem Lett, 8 (12): 1320-1325. [PMID:29259755]
4. (2017)
Erratum Regarding "Hypoxia-Inducible Factor Prolyl Hydroxylase Inhibitors: A Potential New Treatment for Anemia in Patients With CKD" (Am J Kidney Dis. 2017;69[6]:815-826).
Am J Kidney Dis, 69 (6): 869. [PMID:28532635]