Target Information
| Target General Information | Top | |||||
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| Target ID |
T23499
(Former ID: TTDS00198)
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| Target Name |
Endothelin A receptor (EDNRA)
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| Synonyms |
HET-AR; Endothelin-1 receptor; Endothelin receptor type A; Endothelin receptor A; ETRA; ETA-R; ETA receptor; ETA; ET-A
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| Gene Name |
EDNRA
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| Target Type |
Successful target
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[1] | ||||
| Disease | [+] 2 Target-related Diseases | + | ||||
| 1 | Cardiovascular disease [ICD-11: BA00-BE2Z] | |||||
| 2 | Pulmonary hypertension [ICD-11: BB01] | |||||
| Function |
Mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. The rank order of binding affinities for ET-A is: ET1 > ET2 >> ET3. Receptor for endothelin-1.
Click to Show/Hide
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| BioChemical Class |
GPCR rhodopsin
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| UniProt ID | ||||||
| Sequence |
METLCLRASFWLALVGCVISDNPERYSTNLSNHVDDFTTFRGTELSFLVTTHQPTNLVLP
SNGSMHNYCPQQTKITSAFKYINTVISCTIFIVGMVGNATLLRIIYQNKCMRNGPNALIA SLALGDLIYVVIDLPINVFKLLAGRWPFDHNDFGVFLCKLFPFLQKSSVGITVLNLCALS VDRYRAVASWSRVQGIGIPLVTAIEIVSIWILSFILAIPEAIGFVMVPFEYRGEQHKTCM LNATSKFMEFYQDVKDWWLFGFYFCMPLVCTAIFYTLMTCEMLNRRNGSLRIALSEHLKQ RREVAKTVFCLVVIFALCWFPLHLSRILKKTVYNEMDKNRCELLSFLLLMDYIGINLATM NSCINPIALYFVSKKFKNCFQSCLCCCCYQSKSLMTSVPMNGTSIQWKNHDQNNHNTDRS SHKDSMN Click to Show/Hide
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| 3D Structure | Click to Show 3D Structure of This Target | AlphaFold | ||||
| HIT2.0 ID | T34E5V | |||||
| Drugs and Modes of Action | Top | |||||
|---|---|---|---|---|---|---|
| Approved Drug(s) | [+] 4 Approved Drugs | + | ||||
| 1 | Ambrisentan | Drug Info | Approved | Pulmonary arterial hypertension | [2], [3] | |
| 2 | Bosentan | Drug Info | Approved | Pulmonary arterial hypertension | [4], [5] | |
| 3 | LU302146 | Drug Info | Approved | Pulmonary hypertension | [6], [7] | |
| 4 | Macitentan | Drug Info | Approved | Cardiovascular disease | [8], [9], [10] | |
| Clinical Trial Drug(s) | [+] 11 Clinical Trial Drugs | + | ||||
| 1 | Atrasentan | Drug Info | Phase 3 | Diabetic nephropathy | [11] | |
| 2 | Clazosentan | Drug Info | Phase 3 | Cerebral vasospasm | [12], [13] | |
| 3 | Darusentan | Drug Info | Phase 3 | Hypotension | [14], [15] | |
| 4 | PF-1228305 | Drug Info | Phase 3 | Pulmonary hypertension | [16] | |
| 5 | sparsentan | Drug Info | Phase 3 | Focal segmental glomerulosclerosis | [17] | |
| 6 | BQ-123 | Drug Info | Phase 2 | Pulmonary arterial hypertension | [18], [19] | |
| 7 | FR139317 | Drug Info | Phase 2 | Hypertension | [20], [21] | |
| 8 | PD-145065 | Drug Info | Phase 2 | Hypertension | [22] | |
| 9 | TBC-3711 | Drug Info | Phase 2 | Hypotension | [23] | |
| 10 | YM-598 | Drug Info | Phase 2 | Prostate cancer | [24] | |
| 11 | PMZ-2123 | Drug Info | Phase 1 | Cerebral oedema in diabetic ketoacidosis | [11] | |
| Discontinued Drug(s) | [+] 18 Discontinued Drugs | + | ||||
| 1 | Sitaxsentan | Drug Info | Withdrawn from market | Pulmonary arterial hypertension | [25], [3] | |
| 2 | TBC 11251 (TBC) | Drug Info | Withdrawn from market | Pulmonary arterial hypertension | [10], [26] | |
| 3 | Zibotentan | Drug Info | Discontinued in Phase 3 | Prostate cancer | [27], [28] | |
| 4 | 97-139 | Drug Info | Discontinued in Phase 2 | Cerebrovascular disease | [29] | |
| 5 | Avosentan | Drug Info | Discontinued in Phase 2 | Diabetic nephropathy | [30], [31] | |
| 6 | BMS-193884 | Drug Info | Discontinued in Phase 2 | Pulmonary arterial hypertension | [32] | |
| 7 | EDONENTAN HYDRATE | Drug Info | Discontinued in Phase 2 | Pulmonary arterial hypertension | [33] | |
| 8 | ENRASENTAN | Drug Info | Discontinued in Phase 2 | Pulmonary arterial hypertension | [34] | |
| 9 | J-104132 | Drug Info | Discontinued in Phase 2 | Pulmonary arterial hypertension | [35] | |
| 10 | SB-209670 | Drug Info | Discontinued in Phase 2 | Arrhythmia | [36], [37] | |
| 11 | A-216546 | Drug Info | Discontinued in Phase 1 | Solid tumour/cancer | [38] | |
| 12 | SB-234551 | Drug Info | Discontinued in Phase 1 | Nerve injury | [39], [40] | |
| 13 | ZD-1611 | Drug Info | Discontinued in Phase 1 | Hypotension | [41] | |
| 14 | 50-235 | Drug Info | Terminated | Hypertension | [42] | |
| 15 | BMS-182874 | Drug Info | Terminated | Hypertension | [43] | |
| 16 | BQ-518 | Drug Info | Terminated | Hypertension | [44] | |
| 17 | MX-6120 | Drug Info | Terminated | Heart disease | [45] | |
| 18 | PD-155080 | Drug Info | Terminated | Hypertension | [46] | |
| Mode of Action | [+] 4 Modes of Action | + | ||||
| Antagonist | [+] 31 Antagonist drugs | + | ||||
| 1 | Ambrisentan | Drug Info | [1] | |||
| 2 | LU302146 | Drug Info | [48] | |||
| 3 | Atrasentan | Drug Info | [49] | |||
| 4 | Clazosentan | Drug Info | [50] | |||
| 5 | Darusentan | Drug Info | [51] | |||
| 6 | PF-1228305 | Drug Info | [16] | |||
| 7 | sparsentan | Drug Info | [52], [53] | |||
| 8 | BQ-123 | Drug Info | [54], [55] | |||
| 9 | FR139317 | Drug Info | [56] | |||
| 10 | TBC-3711 | Drug Info | [57] | |||
| 11 | YM-598 | Drug Info | [58] | |||
| 12 | PMZ-2123 | Drug Info | [11] | |||
| 13 | Sitaxsentan | Drug Info | [3] | |||
| 14 | TBC 11251 (TBC) | Drug Info | [59] | |||
| 15 | Zibotentan | Drug Info | [60] | |||
| 16 | 97-139 | Drug Info | [10], [61] | |||
| 17 | Avosentan | Drug Info | [62], [63] | |||
| 18 | EDONENTAN HYDRATE | Drug Info | [10], [65] | |||
| 19 | A-216546 | Drug Info | [10], [70] | |||
| 20 | SB-234551 | Drug Info | [10], [71] | |||
| 21 | ZD-1611 | Drug Info | [72] | |||
| 22 | BQ610 | Drug Info | [77] | |||
| 23 | MX-6120 | Drug Info | [78] | |||
| 24 | PD142893 | Drug Info | [77] | |||
| 25 | PD156707 | Drug Info | [81] | |||
| 26 | HJP-272 | Drug Info | [87] | |||
| 27 | LU302872 | Drug Info | [48] | |||
| 28 | PD164333 | Drug Info | [89] | |||
| 29 | [125I]PD151242 | Drug Info | [92] | |||
| 30 | [3H]BQ123 | Drug Info | [93] | |||
| 31 | [3H]S0139 | Drug Info | [87] | |||
| Modulator | [+] 11 Modulator drugs | + | ||||
| 1 | Bosentan | Drug Info | [47] | |||
| 2 | Macitentan | Drug Info | [9] | |||
| 3 | PD-145065 | Drug Info | [22] | |||
| 4 | BMS-193884 | Drug Info | [64] | |||
| 5 | ENRASENTAN | Drug Info | [66] | |||
| 6 | J-104132 | Drug Info | [67] | |||
| 7 | SB-209670 | Drug Info | [68], [69] | |||
| 8 | 50-235 | Drug Info | [74] | |||
| 9 | BQ-518 | Drug Info | [76] | |||
| 10 | PD-155080 | Drug Info | [79], [80] | |||
| 11 | BMS-187308 | Drug Info | [86] | |||
| Inhibitor | [+] 13 Inhibitor drugs | + | ||||
| 1 | ET-1 | Drug Info | [73] | |||
| 2 | BMS-182874 | Drug Info | [75] | |||
| 3 | 2-HYDROXY-3,5-DIIODOBENZOIC ACID | Drug Info | [82] | |||
| 4 | 4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one | Drug Info | [83] | |||
| 5 | Ac-bhg-F-N-Y-Y-W | Drug Info | [84] | |||
| 6 | Ac-w-F-F-N-Y-Y-W | Drug Info | [84] | |||
| 7 | Asterric acid | Drug Info | [85] | |||
| 8 | Bhg-F-N-Y-Y-W | Drug Info | [84] | |||
| 9 | Endothelin-2 | Drug Info | [73] | |||
| 10 | PD-163140 | Drug Info | [88] | |||
| 11 | Trp-Ile-Ile-Asp-Leu-Hisc(Cys-Ser-Val-Tyr-Phe-Cys) | Drug Info | [91] | |||
| 12 | Trp-Ile-Ile-Asp-Leu-Hisc(Cys-Val-Tyr-Phe-Cys) | Drug Info | [91] | |||
| 13 | W-F-F-N--Y-Y-W | Drug Info | [84] | |||
| Agonist | [+] 1 Agonist drugs | + | ||||
| 1 | sarafotoxin S6b | Drug Info | [90] | |||
| Chemical Structure based Activity Landscape of Target | Top |
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| Drug Property Profile of Target | Top | |
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| (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 Regulators | Top | |||||
|---|---|---|---|---|---|---|
| Target-regulating microRNAs | ||||||
| Target Profiles in Patients | Top | |||||
|---|---|---|---|---|---|---|
| Target Expression Profile (TEP) | ||||||
| Target Affiliated Biological Pathways | Top | |||||
|---|---|---|---|---|---|---|
| KEGG Pathway | [+] 7 KEGG Pathways | + | ||||
| 1 | Calcium signaling pathway | |||||
| 2 | cGMP-PKG signaling pathway | |||||
| 3 | cAMP signaling pathway | |||||
| 4 | Neuroactive ligand-receptor interaction | |||||
| 5 | Vascular smooth muscle contraction | |||||
| 6 | Renin secretion | |||||
| 7 | Pathways in cancer | |||||
| NetPath Pathway | [+] 1 NetPath Pathways | + | ||||
| 1 | IL4 Signaling Pathway | |||||
| Panther Pathway | [+] 1 Panther Pathways | + | ||||
| 1 | Endothelin signaling pathway | |||||
| PID Pathway | [+] 2 PID Pathways | + | ||||
| 1 | Endothelins | |||||
| 2 | EGFR-dependent Endothelin signaling events | |||||
| Reactome | [+] 2 Reactome Pathways | + | ||||
| 1 | Peptide ligand-binding receptors | |||||
| 2 | G alpha (q) signalling events | |||||
| WikiPathways | [+] 8 WikiPathways | + | ||||
| 1 | Prostaglandin Synthesis and Regulation | |||||
| 2 | GPCRs, Class A Rhodopsin-like | |||||
| 3 | Gastrin-CREB signalling pathway via PKC and MAPK | |||||
| 4 | Peptide GPCRs | |||||
| 5 | Endothelin Pathways | |||||
| 6 | GPCR ligand binding | |||||
| 7 | GPCR downstream signaling | |||||
| 8 | GPCRs, Other | |||||
| Target-Related Models and Studies | Top | |||||
|---|---|---|---|---|---|---|
| Target Validation | ||||||
| References | Top | |||||
|---|---|---|---|---|---|---|
| REF 1 | Clinical pipeline report, company report or official report of GlaxoSmithKline (2009). | |||||
| REF 2 | 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: 3951). | |||||
| REF 3 | Emerging treatments for pulmonary arterial hypertension. Expert Opin Emerg Drugs. 2006 Nov;11(4):609-19. | |||||
| REF 4 | 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: 3494). | |||||
| REF 5 | Optimizing endothelin receptor antagonist use in the management of pulmonary arterial hypertension. Vasc Health Risk Manag. 2008;4(5):943-52. | |||||
| REF 6 | 2007 FDA drug approvals: a year of flux. Nat Rev Drug Discov. 2008 Feb;7(2):107-9. | |||||
| REF 7 | Ambrisentan, an endothelin receptor type A-selective endothelin receptor antagonist, for the treatment of pulmonary arterial hypertension. Expert Opin Pharmacother. 2009 Aug;10(11):1847-58. | |||||
| REF 8 | 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: 7352). | |||||
| REF 9 | Radium 223 dichloride for prostate cancer treatment. Drug Des Devel Ther. 2017 Sep 6;11:2643-2651. | |||||
| REF 10 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 | |||||
| REF 11 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
| REF 12 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
| REF 13 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
| REF 14 | 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: 3508). | |||||
| REF 15 | ClinicalTrials.gov (NCT00389779) DORADO-AC - Optimized Doses of Darusentan as Compared to an Active Control in Resistant Hypertension. U.S. National Institutes of Health. | |||||
| REF 16 | Pfizer. Product Development Pipeline. March 31 2009. | |||||
| REF 17 | ClinicalTrials.gov (NCT03493685) Study of Sparsentan in Patients With Primary Focal Segmental Glomerulosclerosis (FSGS) (DUPLEX). U.S. National Institutes of Health. | |||||
| REF 18 | 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: 997). | |||||
| REF 19 | ClinicalTrials.gov (NCT00586820) Role of Endothelin in Microvascular Dysfunction Following PCI for NSTEMI. U.S. National Institutes of Health. | |||||
| REF 20 | 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: 998). | |||||
| REF 21 | Acute Endothelin-Receptor Inhibition Does Not Attenuate Acetylcholine-Induced Coronary Vasoconstriction in Experimental Hypercholesterolemia. Arteriosclerosis, Thrombosis, and Vascular Biology, 1998.18: 108-113. | |||||
| REF 22 | Reversal of established responses to endothelin-1 in vivo and in vitro by the endothelin receptor antagonists, BQ-123 and PD 145065. Br J Pharmacol. 1994 May;112(1):207-13. | |||||
| REF 23 | ClinicalTrials.gov (NCT00272961) A Study Of Different Doses Of TBC3711 In Patients With Uncontrolled High Blood Pressure Already Taking Medications For High Blood Pressure.. U.S. National Institutes of Health. | |||||
| REF 24 | ClinicalTrials.gov (NCT00050297) YM598 in Patients With Rising PSA After Initial Therapy for Localized Prostate Cancer. U.S. National Institutes of Health. | |||||
| REF 25 | 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: 3950). | |||||
| REF 26 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007312) | |||||
| REF 27 | 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: 3539). | |||||
| REF 28 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009560) | |||||
| REF 29 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009311) | |||||
| REF 30 | 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: 8260). | |||||
| REF 31 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800015393) | |||||
| REF 32 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007870) | |||||
| REF 33 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800015788) | |||||
| REF 34 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004637) | |||||
| REF 35 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010566) | |||||
| REF 36 | 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: 3528). | |||||
| REF 37 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003996) | |||||
| REF 38 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010699) | |||||
| REF 39 | 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: 1000). | |||||
| REF 40 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009010) | |||||
| REF 41 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008908) | |||||
| REF 42 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003913) | |||||
| REF 43 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004811) | |||||
| REF 44 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006825) | |||||
| REF 45 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800018158) | |||||
| REF 46 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005553) | |||||
| REF 47 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. | |||||
| REF 48 | Influence of endothelin receptor antagonists on myocardial protein kinase C isoforms in uraemic cardiomyopathy. Clin Sci (Lond). 2002 Aug;103 Suppl 48:276S-279S. | |||||
| REF 49 | Effects of a selective ET(A)-receptor antagonist, atrasentan (ABT-627), in murine models of allergic asthma: demonstration of mouse strain specificity. Clin Sci (Lond). 2002 Aug;103 Suppl 48:367S-370S. | |||||
| REF 50 | Effects of the selective endothelin A (ET(A)) receptor antagonist Clazosentan on cerebral perfusion and cerebral oxygenation following severe subar... Acta Neurochir (Wien). 2007;149(9):911-8; discussion 918. | |||||
| REF 51 | Endothelin ETA receptor blockade with darusentan increases sodium and potassium excretion in aging rats. J Cardiovasc Pharmacol. 2006 Mar;47(3):456-62. | |||||
| REF 52 | Designed multiple ligands. An emerging drug discovery paradigm. J Med Chem. 2005 Oct 20;48(21):6523-43. | |||||
| REF 53 | DOI: 10.1038/hr.2009.135 | |||||
| REF 54 | Endothelin in heart failure: a promising therapeutic target Heart. 1997 Feb;77(2):93-4. | |||||
| REF 55 | The therapeutic potential of endothelin-1 receptor antagonists and endothelin-converting enzyme inhibitors on the cardiovascular system. Expert Opin Investig Drugs. 2002 Nov;11(11):1537-52. | |||||
| REF 56 | Reduction of bFGF-induced smooth muscle cell proliferation and endothelin receptor mRNA expression by mevastatin and atorvastatin. Biochem Pharmacol. 2002 Aug 1;64(3):497-505. | |||||
| REF 57 | TBC3711, an ET(A) receptor antagonist, reduces neonatal hypoxia-induced pulmonary hypertension in piglets. Pediatr Res. 2001 Sep;50(3):374-83. | |||||
| REF 58 | Role of the endothelin axis and its antagonists in the treatment of cancer. Br J Pharmacol. 2011 May; 163(2): 220-233. | |||||
| REF 59 | Systemic administration of the endothelin-A receptor antagonist TBC 11251 attenuates cerebral vasospasm after experimental subarachnoid hemorrhage:... Neurosurgery. 1998 Dec;43(6):1409-17; discussion 1417-8. | |||||
| REF 60 | Clinical pipeline report, company report or official report of AstraZeneca (2009). | |||||
| REF 61 | S-0139 (Shionogi). Curr Opin Investig Drugs. 2002 Jul;3(7):1051-6. | |||||
| REF 62 | Agents in development for the treatment of diabetic nephropathy. Expert Opin Emerg Drugs. 2008 Sep;13(3):447-63. | |||||
| REF 63 | Influence of avosentan (SPP3OI) on the pharmacokinetics of a second generation oral contraceptive containing ethinylestradiol and levonorgestrel in healthy female volunteers. Int J Clin Pharmacol Ther. 2006 Dec;44(12):668-74. | |||||
| REF 64 | Vasodilator effects of the endothelin ETA receptor selective antagonist BMS-193884 in healthy men | |||||
| REF 65 | US patent application no. 9,062,094, Dipeptide-based prodrug linkers for aliphatic amine-containing drugs. | |||||
| REF 66 | Enrasentan, an antagonist of endothelin receptors. Cardiovasc Drug Rev. 2003 Spring;21(1):1-16. | |||||
| REF 67 | Pharmacological properties of J-104132 (L-753,037), a potent, orally active, mixed ETA/ETB endothelin receptor antagonist. J Pharmacol Exp Ther. 1999 Jun;289(3):1262-70. | |||||
| REF 68 | Effects of the endothelin receptor antagonist, SB 209670, on circulatory failure and organ injury in endotoxic shock in the anaesthetized rat. Br J Pharmacol. 1996 May;118(1):198-204. | |||||
| REF 69 | Nonpeptide endothelin receptor antagonists. III. Effect of SB 209670 and BQ123 on acute renal failure in anesthetized dogs. J Pharmacol Exp Ther. 1994 Nov;271(2):769-75. | |||||
| REF 70 | Pharmacology of A-216546: a highly selective antagonist for endothelin ET(A) receptor. Eur J Pharmacol. 1999 Feb 5;366(2-3):189-201. | |||||
| REF 71 | Effects of the novel selective endothelin ET(A) receptor antagonist, SB 234551, on the cardiovascular responses to endotoxaemia in conscious rats. Br J Pharmacol. 2001 Aug;133(8):1371-7. | |||||
| REF 72 | Pharmacological profile of ZD1611, a novel, orally active endothelin ETA receptor antagonist. J Pharmacol Exp Ther. 1999 Sep;290(3):1085-91. | |||||
| REF 73 | 5-OHKF and NorKA, depsipeptides from a Hawaiian collection of Bryopsis pennata: binding properties for NorKA to the human neuropeptide Y Y1 receptor. J Nat Prod. 2009 Dec;72(12):2172-6. | |||||
| REF 74 | Structure-activity relationships of an endothelin ETA receptor antagonist, 50-235, and its derivatives. Eur J Pharmacol. 1993 Oct 15;247(2):219-21. | |||||
| REF 75 | Biphenylsulfonamide endothelin receptor antagonists. 2. Discovery of 4'-oxazolyl biphenylsulfonamides as a new class of potent, highly selective ET... J Med Chem. 2000 Aug 10;43(16):3111-7. | |||||
| REF 76 | Structure-activity relationships of cyclic pentapeptide endothelin A receptor antagonists. J Med Chem. 1995 Oct 13;38(21):4309-24. | |||||
| REF 77 | Human optic nerve head astrocytes as a target for endothelin-1. Invest Ophthalmol Vis Sci. 2002 Aug;43(8):2704-13. | |||||
| REF 78 | Endothelin receptor antagonists in heart failure: current status and future directions. Drugs. 2004;64(10):1029-40. | |||||
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