Target Validation Information
TTD ID	T25464
Target Name	Calcineurin (PPP3CA)
Type of Target	Successful
Drug Potency against Target	Ciclosporin	Drug Info	IC50 = 10 ng/mL	[2]
	Pimecrolimus	Drug Info	IC50 = 0.6 ~ 1.0 nM	[4]
	Tacrolimus	Drug Info	IC50 = 11.1 nM	[1]
	Ciclosporin	Drug Info	IC50 = 100 nM	[3]
References
REF 1	32-Indolyl ether derivatives of ascomycin: three-dimensional structures of complexes with FK506-binding protein. J Med Chem. 1999 Jul 29;42(15):2798-804.
REF 2	Tissue distribution of calcineurin and its sensitivity to inhibition by cyclosporine. Am J Transplant. 2001 Nov;1(4):325-33.
REF 3	Substitution in position 3 of cyclosporin A abolishes the cyclophilin-mediated gain-of-function mechanism but not immunosuppression. J Biol Chem. 2004 Jan 23;279(4):2470-9.
REF 4	Pimecrolimus: absorption, distribution, metabolism, and excretion in healthy volunteers after a single oral dose and supplementary investigations i... Drug Metab Dispos. 2006 May;34(5):765-74.

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