Target Validation Information | |||||
---|---|---|---|---|---|
TTD ID | T98269 | ||||
Target Name | Caspase-1 (CASP1) | ||||
Type of Target |
Clinical trial |
||||
Drug Potency against Target | L-709049 | Drug Info | Ki = 9 nM | [3] | |
PRALNACASAN | Drug Info | IC50 = 3.6 nM | [2] | ||
Z-VAD-CHO | Drug Info | Ki = 8 nM | [1] | ||
Z-YVAD-CHO | Drug Info | Ki = 180 nM | [1] | ||
References | |||||
REF 1 | Tethering identifies fragment that yields potent inhibitors of human caspase-1. Bioorg Med Chem Lett. 2006 Feb;16(3):559-62. | ||||
REF 2 | Synthesis and evaluation of thiazepines as interleukin-1beta converting enzyme (ICE) inhibitors. Bioorg Med Chem Lett. 2006 Sep 15;16(18):4728-32. | ||||
REF 3 | Succinic acid amides as P2-P3 replacements for inhibitors of interleukin-1beta converting enzyme (ICE or caspase 1). Bioorg Med Chem Lett. 2010 Sep 1;20(17):5184-90. | ||||
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