Target Validation Information
Target ID T82028
Target Name Sodium/hydrogen exchanger 1
Target Type
Clinical Trial
Drug Potency against Target 5'-(N-ethyl-N-isopropyl)amiloride Drug Info IC50 = 800 nM [528830]
N-[4-(1H-benzoimidazol-2-yl)-benzoyl]-guanidine Drug Info IC50 = 10000 nM [528720]
N-[2-(1H-benzoimidazol-2-yl)-benzoyl]-guanidine Drug Info IC50 = 295 nM [528720]
N-(4-Chloro-3-methanesulfonyl-benzoyl)-guanidine Drug Info IC50 = 380 nM [534413]
N-[5-(2-Nitro-phenyl)-furan-2-carbonyl]-guanidine Drug Info IC50 = 2300 nM [527509]
N-[5-(2-Ethyl-phenyl)-furan-2-carbonyl]-guanidine Drug Info IC50 = 1400 nM [527509]
N-(3-Methanesulfonyl-4-methyl-benzoyl)-guanidine Drug Info IC50 = 210 nM [534413]
HOE-694 Drug Info IC50 = 130 nM [534413]
N-(5-o-Tolyl-furan-2-carbonyl)-guanidine Drug Info IC50 = 340 nM [527509]
N-(3-Methanesulfonyl-4-methoxy-benzoyl)-guanidine Drug Info IC50 = 270 nM [534413]
N-(4-Bromo-3-methanesulfonyl-benzoyl)-guanidine Drug Info IC50 = 180 nM [534413]
ENIPORIDE Drug Info IC50 = 8 nM [534705]
N-(5-Methanesulfonyl-2-methyl-benzoyl)-guanidine Drug Info IC50 = 150 nM [534413]
CARIPORIDE Drug Info IC50 = 65 nM [530180]
N-(5-m-Tolyl-furan-2-carbonyl)-guanidine Drug Info IC50 = 6000 nM [527509]
N-(5-Phenyl-furan-2-carbonyl)-guanidine Drug Info IC50 = 3100 nM [527509]
N-(4-Cyano-3-methanesulfonyl-benzoyl)-guanidine Drug Info IC50 = 140 nM [534413]
References
Ref 528830J Biol Chem. 2007 Jul 6;282(27):19716-27. Epub 2007 May 10.NHE1 inhibition by amiloride- and benzoylguanidine-type compounds. Inhibitor binding loci deduced from chimeras of NHE1 homologues with endogenous differences in inhibitor sensitivity.
Ref 528720Bioorg Med Chem Lett. 2007 May 1;17(9):2430-3. Epub 2007 Feb 17.Benzimidazol-2-yl or benzimidazol-2-ylthiomethyl benzoylguanidines as novel Na+/H+ exchanger inhibitors, synthesis and protection against ischemic-reperfusion injury.
Ref 528720Bioorg Med Chem Lett. 2007 May 1;17(9):2430-3. Epub 2007 Feb 17.Benzimidazol-2-yl or benzimidazol-2-ylthiomethyl benzoylguanidines as novel Na+/H+ exchanger inhibitors, synthesis and protection against ischemic-reperfusion injury.
Ref 534413J Med Chem. 1997 Jun 20;40(13):2017-34.(2-Methyl-5-(methylsulfonyl)benzoyl)guanidine Na+/H+ antiporter inhibitors.
Ref 527509J Med Chem. 2005 Apr 21;48(8):2882-91.(5-Arylfuran-2-ylcarbonyl)guanidines as cardioprotectives through the inhibition of Na+/H+ exchanger isoform-1.
Ref 527509J Med Chem. 2005 Apr 21;48(8):2882-91.(5-Arylfuran-2-ylcarbonyl)guanidines as cardioprotectives through the inhibition of Na+/H+ exchanger isoform-1.
Ref 534413J Med Chem. 1997 Jun 20;40(13):2017-34.(2-Methyl-5-(methylsulfonyl)benzoyl)guanidine Na+/H+ antiporter inhibitors.
Ref 534413J Med Chem. 1997 Jun 20;40(13):2017-34.(2-Methyl-5-(methylsulfonyl)benzoyl)guanidine Na+/H+ antiporter inhibitors.
Ref 527509J Med Chem. 2005 Apr 21;48(8):2882-91.(5-Arylfuran-2-ylcarbonyl)guanidines as cardioprotectives through the inhibition of Na+/H+ exchanger isoform-1.
Ref 534413J Med Chem. 1997 Jun 20;40(13):2017-34.(2-Methyl-5-(methylsulfonyl)benzoyl)guanidine Na+/H+ antiporter inhibitors.
Ref 534413J Med Chem. 1997 Jun 20;40(13):2017-34.(2-Methyl-5-(methylsulfonyl)benzoyl)guanidine Na+/H+ antiporter inhibitors.
Ref 534705J Med Chem. 1998 Sep 10;41(19):3736-47.Bicyclic acylguanidine Na+/H+ antiporter inhibitors.
Ref 534413J Med Chem. 1997 Jun 20;40(13):2017-34.(2-Methyl-5-(methylsulfonyl)benzoyl)guanidine Na+/H+ antiporter inhibitors.
Ref 530180Eur J Med Chem. 2009 Sep;44(9):3771-6. Epub 2009 May 5.Synthesis and bioactivity of substituted indan-1-ylideneaminoguanidine derivatives.
Ref 527509J Med Chem. 2005 Apr 21;48(8):2882-91.(5-Arylfuran-2-ylcarbonyl)guanidines as cardioprotectives through the inhibition of Na+/H+ exchanger isoform-1.
Ref 527509J Med Chem. 2005 Apr 21;48(8):2882-91.(5-Arylfuran-2-ylcarbonyl)guanidines as cardioprotectives through the inhibition of Na+/H+ exchanger isoform-1.
Ref 534413J Med Chem. 1997 Jun 20;40(13):2017-34.(2-Methyl-5-(methylsulfonyl)benzoyl)guanidine Na+/H+ antiporter inhibitors.

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