Mechanisms of action

In pharmacology, the term mechanism of action (MOA) refers to the specific biochemical interaction through which a drug substance produces its pharmacological effect. A mechanism of action usually includes mention of the specific molecular targets to which the drug binds, such as an enzyme or receptor. Receptor sites have specific affinities for drugs based on the chemical structure of the drug, as well as the specific action that occurs there. The information below combines data from the FDA, NIH, ChEMBL, UniProt and other sources cited throughout the CDEK website.

Target families in clinical trials

  • 1.Enzyme protein86,151
  • 2.Membrane receptor protein48,204
  • 3.Unclassified protein32,106
  • 4.Ion channel protein24,289
  • 5.Nucleic-acid22,697
  • 6.Secreted protein20,455
  • 7.Transcription factor protein20,115
  • 8.Transporter protein11,029
  • 9.Organism10,931
  • 10.Surface antigen protein10,790
  • 11.Small molecule10,138
  • 12.Structural protein9,850
  • 13.Unknown8,885
  • 14.Protein nucleic-acid complex7,845
  • 15.Other protein7,302
  • 16.Tissue4,669
  • 17.Other cytosolic protein4,524
  • 18.Cell-line3,387
  • 19.Epigenetic regulator protein2,820
  • 20.Metal2,252
  • 21.Adhesion protein1,477
  • 22.Subcellular1,432
  • 23.Other membrane protein1,326
  • 24.Auxiliary transport protein1,086
  • 25.Macromolecule725
  • 26.Oligosaccharide490
  • 27.Other nuclear protein285
  • 28.Lipid122

Top individual targets in clinical trials

Mechanism groups in clinical trials

  • 1.Inhibitor114,572
  • 2.Agonist46,732
  • 3.Antagonist35,044
  • 4.Supplementation23,187
  • 5.Unclear20,518
  • 6.Other18,630
  • 7.Binding agent13,880
  • 8.Immunity, active10,078
  • 9.Blocker7,758
  • 10.Activator7,251
  • 11.Stabiliser6,469
  • 12.Tissue restoration6,276
  • 13.Immunity, passive5,992
  • 14.Cross-linking agent5,412
  • 15.Modulator4,278
  • 16.Positive allosteric modulator3,356
  • 17.Antioxidant2,655
  • 18.Positive modulator2,646
  • 19.Opener2,404
  • 20.Negative allosteric modulator2,298

Mechanism breakdown by drug type — clinical trials

Small molecule 164,883

  • Inhibitor95,556
  • Agonist34,371
  • Antagonist28,701
  • Other13,616
  • Unclear11,382
  • Supplementation9,583
  • Blocker7,645
  • Binding agent7,275
  • Stabiliser6,460
  • Activator5,579

mAb 29,596

  • Inhibitor26,096
  • Binding agent6,259
  • Antagonist5,575
  • Other1,523
  • Immunity, passive1,469
  • Cross-linking agent1,015
  • Activator513
  • Supplementation498
  • Agonist441
  • Adcc328

Recombinant protein 13,022

  • Agonist8,368
  • Supplementation7,103
  • Inhibitor2,117
  • Positive modulator1,134
  • Exogenous protein605
  • Hydrolytic enzyme600
  • Immunity, active487
  • Activator482
  • Antagonist439
  • Binding agent230

Cell therapy 10,757

  • Tissue restoration5,340
  • Immunity, passive3,130
  • Supplementation2,055
  • Binding agent190
  • Other172
  • Immunity, active165
  • Unclear73
  • Immunity, desensitized32
  • Inhibitor10
  • Gene editing negative modulator8

Vaccine 9,235

  • Immunity, active9,161
  • Other1,324
  • Unclear1,134
  • Vaccine antigen625
  • Binding agent32
  • Antioxidant22
  • Immunity, desensitized20
  • Inhibitor12
  • Supplementation12
  • Immunity, passive9

Botanical 8,228

  • Unclear6,503
  • Supplementation938
  • Other649
  • Substrate261
  • Antioxidant219
  • Sequestering agent181
  • Inhibitor81
  • Astringent21
  • Agonist5
  • Immunity, desensitized5

Biological 6,078

  • Supplementation1,615
  • Inhibitor1,161
  • Other908
  • Hydrolytic enzyme860
  • Agonist825
  • Immunity, passive777
  • Unclear353
  • Immunity, active352
  • Tissue restoration263
  • Exogenous protein152

Peptide 5,552

  • Agonist4,041
  • Inhibitor711
  • Supplementation605
  • Activator484
  • Antagonist413
  • Unclear220
  • Binding agent152
  • Other104
  • Radiopharmaceutical93
  • Disrupting agent33

Animal product 3,088

  • Unclear1,012
  • Supplementation683
  • Immunity, passive626
  • Other444
  • Agonist428
  • Tissue restoration167
  • Activator39
  • Antioxidant28
  • Surfactant25
  • Antagonist23

Nucleic acid 1,268

  • Antisense inhibitor635
  • Inhibitor496
  • Supplementation113
  • Rnai inhibitor92
  • Agonist83
  • Antagonist53
  • Activator49
  • Positive modulator34
  • Modulator30
  • Unclear19

Gene therapy 913

  • Supplementation710
  • Inhibitor49
  • Exogenous gene46
  • Other40
  • Agonist28
  • Unclear23
  • Activator17
  • Immunity, passive11
  • Exogenous protein10
  • Antisense inhibitor10

Allergen 553

  • Immunity, desensitized494
  • Unclear19
  • Inhibitor2
  • Agonist1
  • Immunity, active1

Biologics 13

  • Unclear6
  • Supplementation4
  • Binding agent1
  • Degrader1
  • Immunity, desensitized1