| ABP | activity-based probe |
| ABPP | activity-based protein profiling |
| ADME | absorption, distribution, metabolism, and excretion |
| ALPHA | amplified luminescent proximity homogeneous assay |
| AOMK | acyloxymethyl ketone |
| APT | attached proton test |
| BME | β-mercaptoethanol |
| BODIPY | fluorinated boron-dipyrromethene |
| CAA | chloroacetamide |
| CITe-Id | covalent inhibitor target-site identification |
| CoLDR | covalent ligand directed release |
| CRI | covalent reversible inhibitor |
| cryo-EM | cryogenic electron microscopy |
| CuAAC | Huisgen copper-catalyzed alkyne–azide cycloaddition |
| DNP | 2,4-dinitrophenyl |
| DPS | 2,2′-dipyridyldisulfide |
| DTT | dithiothreitol |
| DUB | deubiquitinating enzyme |
| ELISA | enzyme-linked immunosorbent assay |
| FBDD | fragment-based drug development |
| FBLD | fragment-based ligand discovery |
| FDA | food and drug administration (USA) |
| FFPE | formalin fixed paraffin embedded |
| G12C-TE | KRASG12C target engagement |
| GSH | glutathione |
| GST | glutathione S-transferase |
| HCV | hepatitis C virus |
| His- | polyhistidine tag |
| HTS | high-throughput screening |
| IAc | iodoacetamide |
| ICC | intrahepatic cholangiocarcinoma |
| IEDDA | inverse electron demand Diels Alder |
| isoDTB | isotopically-labeled desthiobiotin |
| isoTOP-ABPP | isotopic tandem orthogonal activity-based protein profiling |
| iTRAQ | isobaric tag for relative and absolute quantitation |
| KD | dissociation constant |
| Ki* | steady-state inhibition constant |
| LC | liquid chromatography |
| MMTS | S-methyl methanethiosulfonate |
| MS | mass spectrometry |
| NMR | nuclear magnetic resonance |
| NSCLC | non-small cell lung carcinoma |
| ODN | odanacatib |
| PD | pharmacodynamics |
| PDB | protein data bank |
| PDT | photodynamic therapy |
| PET | photo-induced electron transfer |
| PK | pharmacokinetics |
| PMK | phenoxymethyl ketone |
| Prg | propargyl |
| PROTAC | proteolysis-targeting chimera |
| qABP | quenched ABP |
| Rho | rhodamine |
| SAR | structure-activity relationship |
| SARS-CoV-2 | severe acute respiratory syndrome coronavirus 2 |
| SDS-PAGE | sodium dodecyl sulfate polyacrylamide gel electrophoresis |
| SILAC | stable-isotope labeling by amino acids in cell culture |
| SPAAC | strain-promoted alkyne–azide cycloaddition |
| SUMO | small ubiquitin-related modifier |
| TAMRA/TMR | tetramethylrhodamine |
| TCEP | tris(2-carboxyethyl)phosphine |
| TCI | targeted covalent inhibitor |
| TIC | total ion count |
| THF | tetrahydrofuran |
| THL | tetrahydrolipstatin |
| TMB | tetramethyl benzidine |
| TMT | tandem mass tag |
| Ub | ubiquitin |
| VME | vinyl methyl ester |
| XRD | X-ray diffraction |