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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