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Proteases

Protease Drug Discovery

Proteases are essential enzymes that cleave peptide bonds and regulate physiological processes including digestion, immune response, and cell signaling. Dysregulated protease activity is associated with cancer, cardiovascular disorders, neurodegenerative diseases, infectious diseases, and inflammatory conditions.

Advances in structural biology, drug design, and screening technologies have expanded the development of protease inhibitors. Accurate measurement of enzyme activity remains essential for identifying and validating selective inhibitors.

Assay Principle

Fluorescence-intensity detection of protease activity

Our protease assays use Fluorescence Intensity (FI) technology to measure enzymatic activity. An active protease recognizes and cleaves a defined peptide sequence containing a fluorescent tag. Cleavage separates the fluorescent tag from the peptide substrate and increases the fluorescence signal. The fluorescence intensity therefore reflects the extent of substrate cleavage and protease activity, supporting quantitative inhibitor evaluation.

Assay Strategy

Protease inhibitor activity and selectivity profiling

01 / TARGET COVERAGE

Activity assays cover serine, cysteine, aspartyl, metalloprotease, aminopeptidase, caspase, coagulation, kallikrein, and viral protease targets.

02 / SELECTIVITY

Panel profiling supports comparison across protease families and evaluation of inhibitor selectivity among related targets.

03 / REFERENCE CONTROLS

Reference inhibitors are available for assay validation and comparative characterization of test compounds.

Target Coverage

Available protease activity assays

TargetSynonymsReference CompoundAssay Format
Neutrophil ElastaseELA2, ELANESivelestatFI
Chymotrypsin CELA4, CTRCChymostatinFI
PlasminogenplasminZK824859FI
u-Plasminogen ActivatorUrokinase, uPAUK-371804FI
t-Plasminogen ActivatorReteplase, tPAZK824859FI
Trypsin 2PRSS2, TRYP2BMS-262084FI
DPP3/Spinorphin TFAFI
DPP4CD26LinagliptinFI
DPP7DPP2, QPPTalabostatFI
DPP8DPRP11G244FI
DPP9DPRP21G244FI
Coagulation Factor IIThrombinDabigatranFI
Coagulation Factor VIISPCAPCI-27483FI
Coagulation Factor XaStuart FactorEdoxabanFI
Coagulation Factor XIPTAAsundexianFI
Coagulation Factor XIIa/Nafamostat (mesylate)FI
Coagulation Factor XIVProtein C, APCNafamostatFI
TMPRSS2PRSS10CamostatFI
FurinPCSK3SSM3FI
Kallikrein 1KLK1AvoralstatFI
Kallikrein 2KLK2AvoralstatFI
Kallikrein 4KLK4AvoralstatFI
Kallikrein 5KLK5AvoralstatFI
Kallikrein 6KLK6AvoralstatFI
Kallikrein 8KLK8AvoralstatFI
Kallikrein 11KLK11AvoralstatFI
Kallikrein 12KLK12AvoralstatFI
Kallikrein 13KLK13AvoralstatFI
Kallikrein 14KLK14AvoralstatFI
Plasma KallikreinKLKB1, PPKAvoralstatFI
Cathepsin BCTSB, APPSLeupeptinFI
Cathepsin CCTSC, DPP1, PALSAZD7986FI
Cathepsin GCTSGCTSG inhibitor IFI
Cathepsin HACC-4, ACC-5, aleurainE-64FI
Cathepsin KCTSK, CTSO, CTSO2OdanacatibFI
Cathepsin LCTSL, CTSL1SID-26681509FI
Cathepsin SCTSSLY-3000328FI
Cathepsin VCathepsin L2, CTSL2E-64FI
Cathepsin XCTSX, CTSZLeupeptinFI
3CL ProteaseMproPF-07321332FI
Papain-like ProteasePLpro, pp1aGRL0617FI
MALT1PCASP1, MLT1, IMD12MLT-748FI
AEPLegumainRR-11aFI
Cathepsin DCTSDPepstatinFI
Cathepsin ECTSEPepstatinFI
ReninRENAliskirenFI
BACE-1ASP2, beta-secretase 1LY2886721FI
MMP-1CLGNIlomastatFI
MMP-2CLG4, Gelatinase AIlomastatFI
MMP-3STR1, stromelysin-1IlomastatFI
MMP-7Matrilysin, PUMP-1BatimastatFI
MMP-8Collagenase 2, PMNL-CLXL-784FI
MMP-9Gelatinase B, GELBIlomastatFI
MMP-10Stromelysin 2, transin 2IlomastatFI
MMP-12Macrophage elastaseUK-370106FI
MMP-13CLG3XL-784FI
MMP-14MT1-MMPMarimastatFI
MMP-15SMCP-2IlomastatFI
MMP-16MMP-X2IlomastatFI
IDE/ML345FI
PSMAFOLH1, GCP2PSMA-617FI
ACECD143, DCPCaptoprilFI
ACE2ACEHMLN-4760FI
Aminopeptidase AENPEP, APACD249RB150FI
ERAP1Aminopeptidase PILS, ARTS1ERAP1-IN-1FI
Complement Component C1sC1 esterase, C1SBCX-1470FI
APNAminopeptidase NBestatinFI
QPCTGlutaminyl-peptide cyclotransferaseSEN177FI
FAP/PT-100FI
Caspase 1CASP1, IL1BC, IL1BCEBelnacasanFI
Caspase 2CASP2, ICH1, NEDD2Ac-DEVD-CHOFI
Caspase 3CASP3, CPP32Ac-DEVD-CHOFI
Caspase 4CASP4, ICH2BelnacasanFI
Caspase 6CASP6, MCH2Ac-DEVD-CHOFI
Caspase 7CASP7, MCH3Ac-DEVD-CHOFI
Caspase 8CASP8, MCH5Ac-DEVD-CHOFI
Caspase 10CASP10, MCH4Ac-DEVD-CHOFI

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