Target Validation Information | |||||
---|---|---|---|---|---|
TTD ID | T04902 | ||||
Target Name | Calpain-2 (CAPN2) | ||||
Type of Target |
Clinical trial |
||||
Drug Potency against Target | Drug Info | IC50 = 70 nM | [4] | ||
(1-Benzyl-2-oxo-ethyl)-carbamic acid benzyl ester | Drug Info | Ki = 3000 nM | [6] | ||
3-(1H-Pyrrol-3-yl)-propionamide | Drug Info | IC50 = 1400 nM | |||
Aloxistatin | Drug Info | IC50 = 1774.2 nM | [5] | ||
AW-00430 | Drug Info | IC50 = 12237.9 nM | [5] | ||
BITHIONOL | Drug Info | IC50 = 4751.15 nM | [5] | ||
DIHYDROXANTHOHUMOL | Drug Info | IC50 = 5000.36 nM | [5] | ||
GNF-PF-4453 | Drug Info | IC50 = 3921.06 nM | [5] | ||
MDL-28170 | Drug Info | Ki = 10 nM | [1] | ||
N-(1-Benzyl-2-oxo-ethyl)-benzamide | Drug Info | Ki = 4000 nM | [6] | ||
SJA-6017 | Drug Info | IC50 = 7.5 nM | [3] | ||
SJA-6017 | Drug Info | IC50 = 86 nM | [2] | ||
References | |||||
REF 1 | Synthesis of a small library of diketopiperazines as potential inhibitors of calpain. Bioorg Med Chem Lett. 2005 Jun 15;15(12):3034-8. | ||||
REF 2 | Exploration of orally available calpain inhibitors 2: peptidyl hemiacetal derivatives. J Med Chem. 2006 Jun 29;49(13):3926-32. | ||||
REF 3 | Synthesis, biological evaluation and molecular modelling of N-heterocyclic dipeptide aldehydes as selective calpain inhibitors. Bioorg Med Chem. 2008 Jul 15;16(14):6911-23. | ||||
REF 4 | Design and synthesis of 4-aryl-4-oxobutanoic acid amides as calpain inhibitors. Bioorg Med Chem Lett. 2009 Jan 15;19(2):502-7. | ||||
REF 5 | In silico identification and biochemical evaluation of novel inhibitors of NRH:quinone oxidoreductase 2 (NQO2). Bioorg Med Chem Lett. 2010 Dec 15;20(24):7331-6. | ||||
REF 6 | Alpha-diketone and alpha-keto ester derivatives of N-protected amino acids and peptides as novel inhibitors of cysteine and serine proteinases. J Med Chem. 1990 Jan;33(1):11-3. | ||||
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