Target Validation Information
Target ID T04902
Target Name Calpain
Target Type
Clinical Trial
Drug Potency against Target 3-(1H-Pyrrol-3-yl)-propionamide Drug Info IC50 = 1400 nM
SJA-6017 Drug Info IC50 = 7.5 nM [529551]
N-(1-Benzyl-2-oxo-ethyl)-benzamide Drug Info Ki = 4000 nM [532033]
BITHIONOL Drug Info IC50 = 4751.15 nM [531262]
MDL-28170 Drug Info Ki = 10 nM [527555]
GNF-PF-4453 Drug Info IC50 = 3921.06 nM [531262]
SJA-6017 Drug Info IC50 = 86 nM [528268]
(1-Benzyl-2-oxo-ethyl)-carbamic acid benzyl ester Drug Info Ki = 3000 nM [532033]
MDL-2170 Drug Info IC50 = 70 nM [529828]
DIHYDROXANTHOHUMOL Drug Info IC50 = 5000.36 nM [531262]
Aloxistatin Drug Info IC50 = 1774.2 nM [531262]
AW-00430 Drug Info IC50 = 12237.9 nM [531262]
References
Ref 529551Bioorg Med Chem. 2008 Jul 15;16(14):6911-23. Epub 2008 May 27.Synthesis, biological evaluation and molecular modelling of N-heterocyclic dipeptide aldehydes as selective calpain inhibitors.
Ref 532033J Med Chem. 1990 Jan;33(1):11-3.Alpha-diketone and alpha-keto ester derivatives of N-protected amino acids and peptides as novel inhibitors of cysteine and serine proteinases.
Ref 531262Bioorg Med Chem Lett. 2010 Dec 15;20(24):7331-6. Epub 2010 Oct 21.In silico identification and biochemical evaluation of novel inhibitors of NRH:quinone oxidoreductase 2 (NQO2).
Ref 527555Bioorg Med Chem Lett. 2005 Jun 15;15(12):3034-8.Synthesis of a small library of diketopiperazines as potential inhibitors of calpain.
Ref 531262Bioorg Med Chem Lett. 2010 Dec 15;20(24):7331-6. Epub 2010 Oct 21.In silico identification and biochemical evaluation of novel inhibitors of NRH:quinone oxidoreductase 2 (NQO2).
Ref 528268J Med Chem. 2006 Jun 29;49(13):3926-32.Exploration of orally available calpain inhibitors 2: peptidyl hemiacetal derivatives.
Ref 532033J Med Chem. 1990 Jan;33(1):11-3.Alpha-diketone and alpha-keto ester derivatives of N-protected amino acids and peptides as novel inhibitors of cysteine and serine proteinases.
Ref 529828Bioorg Med Chem Lett. 2009 Jan 15;19(2):502-7. Epub 2008 Nov 14.Design and synthesis of 4-aryl-4-oxobutanoic acid amides as calpain inhibitors.
Ref 531262Bioorg Med Chem Lett. 2010 Dec 15;20(24):7331-6. Epub 2010 Oct 21.In silico identification and biochemical evaluation of novel inhibitors of NRH:quinone oxidoreductase 2 (NQO2).
Ref 531262Bioorg Med Chem Lett. 2010 Dec 15;20(24):7331-6. Epub 2010 Oct 21.In silico identification and biochemical evaluation of novel inhibitors of NRH:quinone oxidoreductase 2 (NQO2).
Ref 531262Bioorg Med Chem Lett. 2010 Dec 15;20(24):7331-6. Epub 2010 Oct 21.In silico identification and biochemical evaluation of novel inhibitors of NRH:quinone oxidoreductase 2 (NQO2).

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