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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 13.

Several examples of early ICE (caspase-1) reversible and irreversible inhibitors with various leaving groups attached to Cbz-Val-Ala-Asp-scaffold

graphic file with name nihms905431u2.jpg
95–104
R = Ki, μM IC50, μM Ref R = kobs/[I], M−1s−1 Ref
H (aldehyde) 95 0.055 - 268 graphic file with name nihms905431t56.jpg
100 		280000 264
graphic file with name nihms905431t57.jpg
96 		0.1340 0.9760 262 graphic file with name nihms905431t58.jpg
101 		340000 257
graphic file with name nihms905431t59.jpg
97 		0.0040 0.0720 262 graphic file with name nihms905431t60.jpg
102 		252000 248
graphic file with name nihms905431t61.jpg
98 		0.003 0.002 269 graphic file with name nihms905431t62.jpg
103 		406700 263
graphic file with name nihms905431t63.jpg
99 		0.001 0.003 269 graphic file with name nihms905431t64.jpg
104 		230000 265