Target Validation Information
TTD ID	T82028
Target Name	Sodium/hydrogen exchanger 1 (SLC9A1)
Type of Target	Clinical trial
Drug Potency against Target	5'-(N-ethyl-N-isopropyl)amiloride	Drug Info	IC50 = 800 nM	[3]
	CARIPORIDE	Drug Info	IC50 = 65 nM	[4]
	ENIPORIDE	Drug Info	IC50 = 8 nM	[6]
	HOE-694	Drug Info	IC50 = 130 nM	[5]
	N-(3-Methanesulfonyl-4-methoxy-benzoyl)-guanidine	Drug Info	IC50 = 270 nM	[5]
	N-(3-Methanesulfonyl-4-methyl-benzoyl)-guanidine	Drug Info	IC50 = 210 nM	[5]
	N-(4-Bromo-3-methanesulfonyl-benzoyl)-guanidine	Drug Info	IC50 = 180 nM	[5]
	N-(4-Chloro-3-methanesulfonyl-benzoyl)-guanidine	Drug Info	IC50 = 380 nM	[5]
	N-(4-Cyano-3-methanesulfonyl-benzoyl)-guanidine	Drug Info	IC50 = 140 nM	[5]
	N-(5-m-Tolyl-furan-2-carbonyl)-guanidine	Drug Info	IC50 = 6000 nM	[1]
	N-(5-Methanesulfonyl-2-methyl-benzoyl)-guanidine	Drug Info	IC50 = 150 nM	[5]
	N-(5-o-Tolyl-furan-2-carbonyl)-guanidine	Drug Info	IC50 = 340 nM	[1]
	N-(5-Phenyl-furan-2-carbonyl)-guanidine	Drug Info	IC50 = 3100 nM	[1]
	N-[2-(1H-benzoimidazol-2-yl)-benzoyl]-guanidine	Drug Info	IC50 = 295 nM	[2]
	N-[4-(1H-benzoimidazol-2-yl)-benzoyl]-guanidine	Drug Info	IC50 = 10000 nM	[2]
	N-[5-(2-Ethyl-phenyl)-furan-2-carbonyl]-guanidine	Drug Info	IC50 = 1400 nM	[1]
	N-[5-(2-Nitro-phenyl)-furan-2-carbonyl]-guanidine	Drug Info	IC50 = 2300 nM	[1]
References
REF 1	(5-Arylfuran-2-ylcarbonyl)guanidines as cardioprotectives through the inhibition of Na+/H+ exchanger isoform-1. J Med Chem. 2005 Apr 21;48(8):2882-91.
REF 2	Benzimidazol-2-yl or benzimidazol-2-ylthiomethyl benzoylguanidines as novel Na+/H+ exchanger inhibitors, synthesis and protection against ischemic-... Bioorg Med Chem Lett. 2007 May 1;17(9):2430-3.
REF 3	NHE1 inhibition by amiloride- and benzoylguanidine-type compounds. Inhibitor binding loci deduced from chimeras of NHE1 homologues with endogenous ... J Biol Chem. 2007 Jul 6;282(27):19716-27.
REF 4	Synthesis and bioactivity of substituted indan-1-ylideneaminoguanidine derivatives. Eur J Med Chem. 2009 Sep;44(9):3771-6.
REF 5	(2-Methyl-5-(methylsulfonyl)benzoyl)guanidine Na+/H+ antiporter inhibitors. J Med Chem. 1997 Jun 20;40(13):2017-34.
REF 6	Bicyclic acylguanidine Na+/H+ antiporter inhibitors. J Med Chem. 1998 Sep 10;41(19):3736-47.

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