Selectivity Testing

NAEJA has assembled a large selection of assays to be used for testing the selectivity and assessing the potential of toxic effects toxicity of your compound (if any). The list includes:

Serine proteases

                      leukocyte elastase, HLE
                      leukocyte elastase - porcine (often used for selectivity with HLE)
                      cathepsin G
                      thrombin
                      plasmin
                      trypsin
                      chymotrypsin

Cysteine proteases

                      cathepsin B
                      cathepsin L
                      cathepsin K
                      cathepsin S
                      calpain I
                      gingipain R - bacterial enzyme
                      gingipain K - bacterial enzyme

Metallo protease

                      MMP 1, collagenase interstitial
                      MMP 2, gelatinase 72 kDa
                      MMP 3, stromelysin
                      MMP 7, matrilysin
                      MMP 8, neutrophil collagenase
                      MMP 9, gelatinese 92 kDa
                      aminopeptidase M
                      neutral endopeptidase

Cardiovascular / coagulation panel of enzymes

                      Cholesterol acyl transferase (responsible for cholesterol absorption in the intestines)

                      Thrombin

                      Factor VII a

                      Factor X a

                      Plasmim

Central nervous system and neurotransmitters enzymes (can be used for cross reactivity screening)

                      Acetycholinesterase, AChE

                      MAO - A ( Monoamine Oxidase A )

Active Transport enzymes (can be used for cross reactivity screening)

                      Na⁺ K⁺ ATP-ase

Bioactive Peptides Regulatory Enzymes (can be used for cross reactivity screening)

                       NEP , Neutral Endopeptidase

Cytochrome P 450 assays, to test for metabolic liabilities

                       CYP 1A2

                       CYP 2C9

                       CYP 2C19

                       CYP 2D6

Signal transduction pathway assay (to screen for novel compounds or cross reactivity testing)