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. Author manuscript; available in PMC: 2017 Sep 23.
Published in final edited form as: Chem Rev. 2015 Nov 9;115(22):12546–12629. doi: 10.1021/acs.chemrev.5b00434

Table 33.

Examples of caspases inhibitors with various P4 substituents designed using tethering technology.296

graphic file with name nihms905431t191.jpg enzyme assays IC50, μM cellular assays IC50, μM
rh-Casp-1 rh-Casp-3 rh-Casp-7 rh-Casp-8 NT2
graphic file with name nihms905431t192.jpg 350 0.90 0.080 > 10.0 9.10 15.30
graphic file with name nihms905431t193.jpg 351 0.087 0.14 3.28 8.22 30.0
graphic file with name nihms905431t194.jpg 352 0.065 0.036 0.81 2.09 4.56
graphic file with name nihms905431t195.jpg 353 0.92 0.071 9.73 7.65 > 10.0
graphic file with name nihms905431t196.jpg 354 1.93 0.018 9.71 > 10.0 5.74
graphic file with name nihms905431t197.jpg 355 0.13 0.026 1.13 1.75 3.08
graphic file with name nihms905431t198.jpg 356 0.19 0.012 0.49 6.59 3.42
graphic file with name nihms905431t199.jpg 357 0.22 0.0079 0.73 2.46 1.39
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