| Target Validation Information | |||||
|---|---|---|---|---|---|
| Target ID | T25464 | ||||
| Target Name | Calcineurin | ||||
| Target Type | Successful |
||||
| Drug Potency against Target | Pimecrolimus | Drug Info | IC50 = 0.6 ~ 1.0 nM | [552581] | |
| Tacrolimus | Drug Info | IC50 = 11.1 nM | [552193] | ||
| Cyclosporine | Drug Info | IC50 = 100 nM | [552389] | ||
| Cyclosporine | Drug Info | IC50 = 10 ng/mL | [552299] | ||
| References | |||||
| Ref 552581 | Pimecrolimus: absorption, distribution, metabolism, and excretion in healthy volunteers after a single oral dose and supplementary investigations in vitro. Drug Metab Dispos. 2006 May;34(5):765-74. Epub 2006 Feb 7. | ||||
| Ref 552193 | 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 552389 | 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. Epub 2003 Oct 28. | ||||
| Ref 552299 | Tissue distribution of calcineurin and its sensitivity to inhibition by cyclosporine. Am J Transplant. 2001 Nov;1(4):325-33. | ||||
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