Target Validation Information
Target ID T23499
Target Name Endothelin-1 receptor
Target Type
Successful
Drug Potency against Target Sitaxsentan Drug Info IC50 = 1.4 nM [552745]
Bhg-F-N-Y-Y-W Drug Info IC50 = 9500 nM
Zibotentan Drug Info EC50 = 23 nM [552593]
Asterric acid Drug Info IC50 = 10000 nM [526255]
BMS-182874 Drug Info Ki = 55 nM [525859]
PS433540 Drug Info Ki = 1.9 nM [527799]
Ambrisentan Drug Info IC50 = 21.7 nM
Trp-Ile-Ile-Asp-Leu-Hisc(Cys-Val-Tyr-Phe-Cys) Drug Info IC50 = 6500 nM
W-F-F-N--Y-Y-W Drug Info IC50 = 2400 nM
Ac-bhg-F-N-Y-Y-W Drug Info IC50 = 1900 nM
BMS-193884 Drug Info Ki = 1.4 nM [525859]
Endothelin-2 Drug Info IC50 = 0.288 nM [530519]
PD-155080 Drug Info IC50 = 7.4 nM
PD-163140 Drug Info IC50 = 0.35 nM
Bosentan Drug Info IC50 = 4.1~4.7 nM [552892]
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one Drug Info Ki < 1000 nM [531079]
Trp-Ile-Ile-Asp-Leu-Hisc(Cys-Ser-Val-Tyr-Phe-Cys) Drug Info IC50 = 2800 nM
References
Ref 552745The endothelin system as a therapeutic target in cardiovascular disease: great expectations or bleak house? Br J Pharmacol. 2008 Mar;153(6):1105-19. Epub 2007 Oct 29.
Ref 552593Characterization and inhibition of SARS-coronavirus main protease. Curr Top Med Chem. 2006;6(4):361-76.
Ref 526255J Nat Prod. 2002 Jan;65(1):7-10.New chlorinated diphenyl ethers from an Aspergillus species.
Ref 525859J 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 527799J Med Chem. 2005 Oct 20;48(21):6523-43.Designed multiple ligands. An emerging drug discovery paradigm.
Ref 525859J 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 530519J 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 552892BCL-2 family antagonists for cancer therapy. Nat Rev Drug Discov. 2008 Dec;7(12):989-1000. doi: 10.1038/nrd2658.
Ref 531079J 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.

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