Target Validation Information
TTD ID	T23499
Target Name	Endothelin A receptor (EDNRA)
Type of Target	Successful
Drug Potency against Target	Ambrisentan	Drug Info	IC50 = 21.7 nM
	Bosentan	Drug Info	IC50 = 4.1~4.7 nM	[8]
	Sitaxsentan	Drug Info	IC50 = 1.4 nM	[7]
	Zibotentan	Drug Info	EC50 = 23 nM	[6]
	4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one	Drug Info	Ki < 1000 nM	[5]
	Ac-bhg-F-N-Y-Y-W	Drug Info	IC50 = 1900 nM
	Asterric acid	Drug Info	IC50 = 10000 nM	[2]
	Bhg-F-N-Y-Y-W	Drug Info	IC50 = 9500 nM
	BMS-182874	Drug Info	Ki = 55 nM	[1]
	BMS-193884	Drug Info	Ki = 1.4 nM	[1]
	Endothelin-2	Drug Info	IC50 = 0.288 nM	[4]
	PD-155080	Drug Info	IC50 = 7.4 nM
	PD-163140	Drug Info	IC50 = 0.35 nM
	Sparsentan	Drug Info	Ki = 1.9 nM	[3]
	Trp-Ile-Ile-Asp-Leu-Hisc(Cys-Ser-Val-Tyr-Phe-Cys)	Drug Info	IC50 = 2800 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
References
REF 1	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 2	New chlorinated diphenyl ethers from an Aspergillus species. J Nat Prod. 2002 Jan;65(1):7-10.
REF 3	Designed multiple ligands. An emerging drug discovery paradigm. J Med Chem. 2005 Oct 20;48(21):6523-43.
REF 4	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 5	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 rec... J Med Chem. 2010 Sep 9;53(17):6386-97.
REF 6	Characterization and inhibition of SARS-coronavirus main protease. Curr Top Med Chem. 2006;6(4):361-76.
REF 7	The endothelin system as a therapeutic target in cardiovascular disease: great expectations or bleak house Br J Pharmacol. 2008 Mar;153(6):1105-19.
REF 8	BCL-2 family antagonists for cancer therapy. Nat Rev Drug Discov. 2008 Dec;7(12):989-1000.

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