Target Information
Target General Infomation | |||||
---|---|---|---|---|---|
Target ID |
T23499
|
||||
Former ID |
TTDS00198
|
||||
Target Name |
Endothelin-1 receptor
|
||||
Gene Name |
EDNRA
|
||||
Synonyms |
ET-A; ETA receptor; ETA-R; Endothelin A receptor; Endothelin receptor A; HET-AR; EDNRA
|
||||
Target Type |
Successful
|
||||
Disease | Arrhythmia [ICD9: 427; ICD10: I47-I49] | ||||
Cardiovascular disorder [ICD10: I00-I99] | |||||
Cerebrovascular disorders [ICD10: I60-I69] | |||||
Diabetic nephropathy [ICD9: 250.4; ICD10: E11.21] | |||||
Hormone resistant prostate cancer [ICD9: 185; ICD10: C61] | |||||
Hormone refractory prostate cancer [ICD9: 140-229, 185; ICD10: C61] | |||||
Hypotension [ICD9: 458, 796.3; ICD10: I95] | |||||
Heart disease [ICD9: 390-429; ICD10: I00-I52] | |||||
Hypertension [ICD9: 401; ICD10: I10-I16] | |||||
Myocardial infarction [ICD9: 410; ICD10: I21, I22] | |||||
Nerve injury [ICD10: T14.4] | |||||
Pulmonary arterial hypertension [ICD9: 416; ICD10: I27.0, I27.2] | |||||
Pulmonary hypertension [ICD9: 416; ICD10: I27.0, I27.2] | |||||
Prostate cancer [ICD9: 185; ICD10: C61] | |||||
Premature labour [ICD9: 644, 765; ICD10: O60.1, P07.3] | |||||
Solid tumours [ICD9: 140-199, 210-229; ICD10: C00-D48] | |||||
Vasospasm following subarachnoid hemorrhage [ICD9: 430, 728.85, 852.0, 852.1; ICD10: I60, P10.3, R25.2, S06.6] | |||||
Unspecified [ICD code not available] | |||||
Function |
Receptor for endothelin-1. 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.
|
||||
BioChemical Class |
GPCR rhodopsin
|
||||
Target Validation |
T23499
|
||||
UniProt ID | |||||
Sequence |
METLCLRASFWLALVGCVISDNPERYSTNLSNHVDDFTTFRGTELSFLVTTHQPTNLVLP
SNGSMHNYCPQQTKITSAFKYINTVISCTIFIVGMVGNATLLRIIYQNKCMRNGPNALIA SLALGDLIYVVIDLPINVFKLLAGRWPFDHNDFGVFLCKLFPFLQKSSVGITVLNLCALS VDRYRAVASWSRVQGIGIPLVTAIEIVSIWILSFILAIPEAIGFVMVPFEYRGEQHKTCM LNATSKFMEFYQDVKDWWLFGFYFCMPLVCTAIFYTLMTCEMLNRRNGSLRIALSEHLKQ RREVAKTVFCLVVIFALCWFPLHLSRILKKTVYNEMDKNRCELLSFLLLMDYIGINLATM NSCINPIALYFVSKKFKNCFQSCLCCCCYQSKSLMTSVPMNGTSIQWKNHDQNNHNTDRS SHKDSMN |
||||
Drugs and Mode of Action | |||||
Drug(s) | Ambrisentan | Drug Info | Approved | Pulmonary arterial hypertension | [536294], [540573] |
Bosentan | Drug Info | Approved | Pulmonary arterial hypertension | [537041], [540432] | |
LU302146 | Drug Info | Approved | Pulmonary hypertension | [529282], [530258] | |
Macitentan | Drug Info | Approved | Cardiovascular disorder | [532651], [542373], [551871] | |
Darusentan | Drug Info | Phase 3 | Hypotension | [521903], [540446] | |
PF-1228305 | Drug Info | Phase 3 | Pulmonary hypertension | [549974] | |
BQ-123 | Drug Info | Phase 2 | Pulmonary arterial hypertension | [522196], [543354] | |
FR139317 | Drug Info | Phase 2 | Hypertension | [543355], [549735] | |
PD-145065 | Drug Info | Phase 2 | Hypertension | [533860] | |
PS433540 | Drug Info | Phase 2 | Hypertension | [522259] | |
sparsentan | Drug Info | Phase 2 | Myocardial infarction | [527366] | |
TBC-3711 | Drug Info | Phase 2 | Hypotension | [521781] | |
YM-598 | Drug Info | Phase 2 | Prostate cancer | [521539] | |
ET-1 | Drug Info | Phase 0 | Discovery agent | [524736], [543350] | |
Atrasentan | Drug Info | Withdrawn from market | Hormone refractory prostate cancer | [536957], [540426] | |
Sitaxsentan | Drug Info | Withdrawn from market | Pulmonary arterial hypertension | [536294], [540572] | |
TBC 11251 (TBC) | Drug Info | Withdrawn from market | Pulmonary arterial hypertension | [546296], [551871] | |
Clazosentan | Drug Info | Discontinued in Phase 3 | Vasospasm following subarachnoid hemorrhage | [547565] | |
Zibotentan | Drug Info | Discontinued in Phase 3 | Hormone resistant prostate cancer | [540471], [546670] | |
97-139 | Drug Info | Discontinued in Phase 2 | Cerebrovascular disorders | [546634] | |
Avosentan | Drug Info | Discontinued in Phase 2 | Diabetic nephropathy | [543017], [547349] | |
BMS-193884 | Drug Info | Discontinued in Phase 2 | Pulmonary arterial hypertension | [546390] | |
EDONENTAN HYDRATE | Drug Info | Discontinued in Phase 2 | Pulmonary arterial hypertension | [547387] | |
ENRASENTAN | Drug Info | Discontinued in Phase 2 | Pulmonary arterial hypertension | [545770] | |
J-104132 | Drug Info | Discontinued in Phase 2 | Pulmonary arterial hypertension | [546841] | |
SB-209670 | Drug Info | Discontinued in Phase 2 | Arrhythmia | [540461], [545631] | |
A-216546 | Drug Info | Discontinued in Phase 1 | Solid tumours | [546860] | |
SB-234551 | Drug Info | Discontinued in Phase 1 | Nerve injury | [538610], [546574] | |
ZD-1611 | Drug Info | Discontinued in Phase 1 | Hypotension | [546553] | |
50-235 | Drug Info | Terminated | Hypertension | [545617] | |
BMS-182874 | Drug Info | Terminated | Hypertension | [545806] | |
BQ-518 | Drug Info | Terminated | Hypertension | [546191] | |
BQ610 | Drug Info | Terminated | Discovery agent | [545712] | |
MX-6120 | Drug Info | Terminated | Heart disease | [547652] | |
PD-155080 | Drug Info | Terminated | Hypertension | [545967] | |
PD142893 | Drug Info | Terminated | Discovery agent | [545245] | |
PD156707 | Drug Info | Terminated | Discovery agent | [543356], [545965] | |
Inhibitor | 2-HYDROXY-3,5-DIIODOBENZOIC ACID | Drug Info | [551377] | ||
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one | Drug Info | [531079] | |||
Ac-bhg-F-N-Y-Y-W | Drug Info | [551298] | |||
Ac-w-F-F-N-Y-Y-W | Drug Info | [551298] | |||
Asterric acid | Drug Info | [526255] | |||
Bhg-F-N-Y-Y-W | Drug Info | [551298] | |||
BMS-182874 | Drug Info | [525859] | |||
Endothelin-2 | Drug Info | [530519] | |||
ET-1 | Drug Info | [530519] | |||
PD-163140 | Drug Info | [551335] | |||
Trp-Ile-Ile-Asp-Leu-Hisc(Cys-Ser-Val-Tyr-Phe-Cys) | Drug Info | [551271] | |||
Trp-Ile-Ile-Asp-Leu-Hisc(Cys-Val-Tyr-Phe-Cys) | Drug Info | [551271] | |||
W-F-F-N--Y-Y-W | Drug Info | [551298] | |||
Modulator | 50-235 | Drug Info | [533968] | ||
BMS-187308 | Drug Info | ||||
BMS-193884 | Drug Info | ||||
Bosentan | Drug Info | [556264] | |||
BQ-518 | Drug Info | [533587] | |||
ENRASENTAN | Drug Info | [526546] | |||
J-104132 | Drug Info | [525496] | |||
Macitentan | Drug Info | [532651] | |||
PD-145065 | Drug Info | [533860] | |||
PD-155080 | Drug Info | ||||
PS433540 | Drug Info | ||||
SB-209670 | Drug Info | [534175] | |||
Antagonist | 97-139 | Drug Info | [526406], [551871] | ||
A-216546 | Drug Info | [525441], [551871] | |||
Ambrisentan | Drug Info | [550963] | |||
Atrasentan | Drug Info | [535545] | |||
Avosentan | Drug Info | [536328], [536836] | |||
BQ-123 | Drug Info | [535609], [538019] | |||
BQ610 | Drug Info | [535521] | |||
Clazosentan | Drug Info | [528988] | |||
Darusentan | Drug Info | [528154] | |||
EDONENTAN HYDRATE | Drug Info | [550931], [551871] | |||
FR139317 | Drug Info | [535520] | |||
HJP-272 | Drug Info | [543573] | |||
LU302146 | Drug Info | [535544] | |||
LU302872 | Drug Info | [535544] | |||
MX-6120 | Drug Info | [527075] | |||
PD142893 | Drug Info | [535521] | |||
PD156707 | Drug Info | [538130] | |||
PD164333 | Drug Info | [534570] | |||
PF-1228305 | Drug Info | [549974] | |||
SB-234551 | Drug Info | [526119], [551871] | |||
Sitaxsentan | Drug Info | [536294] | |||
sparsentan | Drug Info | [527799] | |||
TBC 11251 (TBC) | Drug Info | [538147] | |||
TBC-3711 | Drug Info | [526125] | |||
YM-598 | Drug Info | [544172] | |||
ZD-1611 | Drug Info | [525566] | |||
Zibotentan | Drug Info | [550288] | |||
[125I]PD151242 | Drug Info | [533849] | |||
[125I]PD164333 | Drug Info | [534570] | |||
[3H]BQ123 | Drug Info | [533729] | |||
[3H]S0139 | Drug Info | [543573] | |||
Agonist | sarafotoxin S6b | Drug Info | [533673] | ||
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM) | |||||
TEP | EXP Info | ||||
Pathways | |||||
KEGG Pathway | Calcium signaling pathway | ||||
cGMP-PKG signaling pathway | |||||
cAMP signaling pathway | |||||
Neuroactive ligand-receptor interaction | |||||
Vascular smooth muscle contraction | |||||
Renin secretion | |||||
Pathways in cancer | |||||
NetPath Pathway | IL4 Signaling Pathway | ||||
PANTHER Pathway | Endothelin signaling pathway | ||||
Pathway Interaction Database | Endothelins | ||||
EGFR-dependent Endothelin signaling events | |||||
Reactome | Peptide ligand-binding receptors | ||||
G alpha (q) signalling events | |||||
WikiPathways | Prostaglandin Synthesis and Regulation | ||||
GPCRs, Class A Rhodopsin-like | |||||
Gastrin-CREB signalling pathway via PKC and MAPK | |||||
Peptide GPCRs | |||||
Endothelin Pathways | |||||
GPCR ligand binding | |||||
GPCR downstream signaling | |||||
GPCRs, Other | |||||
References | |||||
Ref 521539 | ClinicalTrials.gov (NCT00050297) YM598 in Patients With Rising PSA After Initial Therapy for Localized Prostate Cancer. U.S. National Institutes of Health. | ||||
Ref 521781 | 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 521903 | 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 522196 | ClinicalTrials.gov (NCT00586820) Role of Endothelin in Microvascular Dysfunction Following PCI for NSTEMI. U.S. National Institutes of Health. | ||||
Ref 522259 | ClinicalTrials.gov (NCT00635232) A Study To Evaluate The Dose-Related Efficacy and Safety of PS433540 in Subjects With Hypertension. U.S. National Institutes of Health. | ||||
Ref 524736 | ClinicalTrials.gov (NCT02124824) Contribution of Endothelin-1 to Exercise Intolerance in Heart Failure. U.S. National Institutes of Health. | ||||
Ref 527366 | Dual angiotensin II and endothelin A receptor antagonists: synthesis of 2'-substituted N-3-isoxazolyl biphenylsulfonamides with improved potency and pharmacokinetics. J Med Chem. 2005 Jan 13;48(1):171-9. | ||||
Ref 530258 | 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 533860 | 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 536294 | Emerging treatments for pulmonary arterial hypertension. Expert Opin Emerg Drugs. 2006 Nov;11(4):609-19. | ||||
Ref 536957 | Current and future treatments of bone metastases. Expert Opin Emerg Drugs. 2008 Dec;13(4):609-27. | ||||
Ref 537041 | Optimizing endothelin receptor antagonist use in the management of pulmonary arterial hypertension. Vasc Health Risk Manag. 2008;4(5):943-52. | ||||
Ref 538610 | (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 540426 | (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: 3487). | ||||
Ref 540432 | (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 540446 | (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 540461 | (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 540471 | (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 540572 | (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 540573 | (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 542373 | (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 543017 | (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 543350 | (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: 989). | ||||
Ref 543354 | (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 543355 | (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 543356 | (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: 999). | ||||
Ref 545245 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002573) | ||||
Ref 545617 | 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 545631 | 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 545712 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004314) | ||||
Ref 545770 | 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 545806 | 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 545965 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005545) | ||||
Ref 545967 | 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 546191 | 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 546296 | 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 546390 | 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 546553 | 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 546574 | 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 546634 | 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 546670 | 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 546841 | 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 546860 | 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 547349 | 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 547387 | 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 547565 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800017374) | ||||
Ref 547652 | 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 525441 | 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 525496 | 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 525566 | Pharmacological profile of ZD1611, a novel, orally active endothelin ETA receptor antagonist. J Pharmacol Exp Ther. 1999 Sep;290(3):1085-91. | ||||
Ref 525859 | J Med Chem. 2000 Aug 10;43(16):3111-7.Biphenylsulfonamide endothelin receptor antagonists. 2. Discovery of 4'-oxazolyl biphenylsulfonamides as a new class of potent, highly selective ET(A) antagonists. | ||||
Ref 526119 | 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 526125 | TBC3711, an ET(A) receptor antagonist, reduces neonatal hypoxia-induced pulmonary hypertension in piglets. Pediatr Res. 2001 Sep;50(3):374-83. | ||||
Ref 526255 | J Nat Prod. 2002 Jan;65(1):7-10.New chlorinated diphenyl ethers from an Aspergillus species. | ||||
Ref 526546 | Enrasentan, an antagonist of endothelin receptors. Cardiovasc Drug Rev. 2003 Spring;21(1):1-16. | ||||
Ref 527075 | Endothelin receptor antagonists in heart failure: current status and future directions. Drugs. 2004;64(10):1029-40. | ||||
Ref 527799 | J Med Chem. 2005 Oct 20;48(21):6523-43.Designed multiple ligands. An emerging drug discovery paradigm. | ||||
Ref 528154 | Endothelin ETA receptor blockade with darusentan increases sodium and potassium excretion in aging rats. J Cardiovasc Pharmacol. 2006 Mar;47(3):456-62. | ||||
Ref 528988 | Effects of the selective endothelin A (ET(A)) receptor antagonist Clazosentan on cerebral perfusion and cerebral oxygenation following severe subarachnoid hemorrhage - preliminary results from a randomized clinical series. Acta Neurochir (Wien). 2007;149(9):911-8; discussion 918. Epub 2007 Aug 13. | ||||
Ref 530519 | J Nat Prod. 2009 Dec;72(12):2172-6.5-OHKF and NorKA, depsipeptides from a Hawaiian collection of Bryopsis pennata: binding properties for NorKA to the human neuropeptide Y Y1 receptor. | ||||
Ref 531079 | J Med Chem. 2010 Sep 9;53(17):6386-97.Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 receptor agonist with unprecedented selectivity and procognitive potential. | ||||
Ref 533587 | Structure-activity relationships of cyclic pentapeptide endothelin A receptor antagonists. J Med Chem. 1995 Oct 13;38(21):4309-24. | ||||
Ref 533673 | ETA receptor-mediated constrictor responses to endothelin peptides in human blood vessels in vitro. Br J Pharmacol. 1995 May;115(1):191-7. | ||||
Ref 533729 | [3H]BQ-123, a highly specific and reversible radioligand for the endothelin ETA receptor subtype. Eur J Pharmacol. 1995 Feb 14;274(1-3):1-6. | ||||
Ref 533849 | [125I]-PD151242: a selective radioligand for human ETA receptors. Br J Pharmacol. 1994 Jan;111(1):4-6. | ||||
Ref 533860 | 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 533968 | 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 534175 | 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 534570 | Characterization of [125I]-PD164333, an ETA selective non-peptide radiolabelled antagonist, in normal and diseased human tissues. Br J Pharmacol. 1998 Jan;123(2):223-30. | ||||
Ref 535520 | 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 535521 | Human optic nerve head astrocytes as a target for endothelin-1. Invest Ophthalmol Vis Sci. 2002 Aug;43(8):2704-13. | ||||
Ref 535544 | 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 535545 | 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 535609 | 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 536294 | Emerging treatments for pulmonary arterial hypertension. Expert Opin Emerg Drugs. 2006 Nov;11(4):609-19. | ||||
Ref 536328 | 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 536836 | Agents in development for the treatment of diabetic nephropathy. Expert Opin Emerg Drugs. 2008 Sep;13(3):447-63. | ||||
Ref 538130 | Discovery and development of an endothelin A receptor-selective antagonist PD 156707. Pharm Biotechnol. 1998;11:81-112. | ||||
Ref 538147 | Systemic administration of the endothelin-A receptor antagonist TBC 11251 attenuates cerebral vasospasm after experimental subarachnoid hemorrhage: dose study and review of endothelin-based therapiesin the literature on cerebral vasospasm. Neurosurgery. 1998 Dec;43(6):1409-17; discussion 1417-8. | ||||
Ref 543573 | (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: 219). | ||||
Ref 544172 | Role of the endothelin axis and its antagonists in the treatment of cancer. Br J Pharmacol. 2011 May; 163(2): 220-233. | ||||
Ref 550931 | US patent application no. 9,062,094, Dipeptide-based prodrug linkers for aliphatic amine-containing drugs. | ||||
Ref 551271 | Structure-activity relationships in a series of monocyclic endothelin analogues, Bioorg. Med. Chem. Lett. 4(4):567-572 (1994). | ||||
Ref 551298 | Res-701-1, synthesis and a reevaluation of its effects on the endothelin receptors, Bioorg. Med. Chem. Lett. 5(6):621-626 (1995). | ||||
Ref 551335 | gamma-Carbamate butenolide analogues as potent ETA selective endothelin receptor antagonists and prodrugs, Bioorg. Med. Chem. Lett. 7(3):297-302 (1997). | ||||
Ref 551377 | Allosteric inhibition of endothelin <span class="caps">ETA</span> receptors by 3, 5-dibromosalicylic acid. Mol Pharmacol. 2000 Dec;58(6):1461-9. |
If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.