Small Molecule Agonists

Agonists can induce excitatory or inhibitory responses and modulate or enhance the basal activity of tissues. Small molecule agonists are substances that can enhance another molecule's activity and therefore stimulate an action. Agonists often mimic the effects of natural substances. The action caused by agonists can be blocked by antagonists. Agonists and antagonists are key players in the chemistry of the human body and in pharmacology.

Small molecule agonists can be mainly classified into two categories depending on whether the function is full or partial. Full agonists can bind and activate receptors and produce full efficacy equal to that of the endogenous ligand. Partial agonists also can bind and activate receptors, but have only partial efficacy relative to full agonists even at maximal receptor occupancy. However, a full agonist also can act as a partial agonist in another issue and vice versa.

Small molecule agonists also can be classified according to the mode of action. Co-agonists need to work together with other agonists to produce the desired effect. Selective agonists selectively promote specific types of reaction. Inverse agonists are agents that bind to the same receptor binding-site as agonists for that receptor but induce the opposite pharmacological response. Irreversible agonists can permanently bind to receptors by forming covalent bonds. Super agonist is capable of producing a greater response for the target receptor and its efficacy can exceed 100%.

Scientists, including biologists, chemists, and pharmacologists, and pharmaceutical companies are using all the options of receptors, ligands, biological pathways and pharmacology to develop the most effective drugs for human disease treatment. Small molecule agonists are one of the options. They have been widely involved in the treatment of a variety of diseases, such as neurological diseases, diabetes, cancer, metabolic diseases, infectious diseases and cardiovascular diseases. It is sensible to develop small molecule agonists that are more stable, more safety, more effective and less expensive as drugs.

Strategy for development of first- and best-in-class adiponectin receptor (AdipoR) agonists in the treatment of obesity-related diseases such as type 2 diabetes.Figure 1. Strategy for development of first- and best-in-class adiponectin receptor (AdipoR) agonists in the treatment of obesity-related diseases such as type 2 diabetes. (Okada-Iwabu, M., et al., 2015)

Creative Biolabs provides powerful risk-based preclinical data verification services for small molecule agonist research and development to deal with data reproducibility crisis which is a big obstacle for drug research and development and may lead to failure and high risk of investment. We have extensive experience in different kinds of small molecule agonists and different disease areas. Our services focus on target validation, hit validation, lead validation, safety assessment and efficacy evaluation.

Creative Biolabs’ professional scientific team involving biologists, chemists, and pharmacologists can offer customized and most suitable methods to meet your specific needs based on various cell lines and animal models. With advanced equipment and up-to-date technology, we are confident to give our clients high-quality and reliable results in a timely and cost-effective manner.

Through a comprehensive assessment of you drug candidates, Creative Biolabs provides our clients with project feasibility assessment to help you make wise decisions, thereby reducing investment risk and speeding up the progress of your project.

Given our professional in drug discovery and development, you’ll benefit from our full-service lab capabilities. If you are interested or have any other questions, please feel free to contact us. We look forward to working with you in the near future.


  1. Okada-Iwabu, M., et al., 2015. Perspective of small-molecule AdipoR agonist for type 2 diabetes and short life in obesity. Diabetes & metabolism journal, 39(5), pp. 363-372.

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