Target Validation Information
TTD ID	T92328
Target Name	Ryanodine receptor 1 (RYR1)
Type of Target	Discontinued
Drug Potency against Target	Dantrolene	Drug Info	Ki = 1500 nM	[2]
	(O10eq)-Benzyloxycarbonyl-beta-alanylryanodine	Drug Info	IC50 = 5.9 nM	[1]
	(O10eq)-beta-alanyl-anhydro-ryanodine	Drug Info	IC50 = 149 nM	[1]
	(O10eq)-beta-alanylryanodine	Drug Info	IC50 = 2.6 nM	[1]
	(O10eq)-beta-guanidinopropionylryanodine	Drug Info	IC50 = 1.1 nM	[1]
	(O10eq)-guanidino acetylryanodine	Drug Info	IC50 = 1.8 nM	[1]
	ANHYDRORYANIDINE	Drug Info	IC50 = 8.9 nM	[1]
	Benzyloxycarbonyl-glycylryanodine	Drug Info	IC50 = 4.8 nM	[1]
	Di-Benzyloxycarbonyl-guanidino acetylryanodine	Drug Info	IC50 = 135.6 nM	[1]
	GLYCYLRYANODINE	Drug Info	IC50 = 1.8 nM	[1]
	N-methyl ryanodine-succinamidate	Drug Info	IC50 = 49.4 nM	[1]
References
REF 1	Amino- and guanidinoacylryanodines: basic ryanodine esters with enhanced affinity for the sarcoplasmic reticulum Ca(2+)-release channel. J Med Chem. 1993 May 14;36(10):1319-23.
REF 2	[3H]Azidodantrolene: synthesis and use in identification of a putative skeletal muscle dantrolene binding site in sarcoplasmic reticulum. J Med Chem. 1999 Jun 3;42(11):1872-80.

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