Low-affinity binders

Three forms of folate appear to be transported ia the blood foHc acid, folate loosely bouad to low affinity binder semm proteins (such as albumin, a-macroglobulin, and transferrin), and folate bound to high affinity protein binders. Approximately 5% of total semm folate is being transported by high... 

Down the Rabbit Hole Pitfalls When Dealing with Low-Affinity Binders... 

As every bead presents multiple copies of a compoimd, the fluorescence signal may not correlate to the actual potency of the structure due to multiple binding. However, this effect can also be utilized to identify low-affinity binders with a polyvalent assay system [169]. 

Because of the improved sampling of chemical space, as well as the sometimes low-throughput biophysical methods needed to detect low-affinity binders. 

Fundamentally, FBDD is a general approach aimed at deriving high affinity ligands for macromolecular targets starting from low MW binders, which are usually identified by the use of the aforementioned biophysical techniques [1, 2, 7, 8]. 

Figure 7 Depiction of competition-based screening. Low- to medium-affinity binders are displaced from their binding site by higher affinity binders. In this experiment, only the signals of these low- to medium-affinity binders (reporter ligands) are monitored...

Crisman TJ, Bender A, Milik M et al (2008) Virtual fragment linking an approach to identify potent binders from low affinity fragment hits. J Med Chem 51 2481-2491... 

Crisman, T.J., Bender, A., Milik, M., Jenkins, J.L., Scheiber, J., Sukuru, S.C., Fejzo, J., Hommel, U., Davies, J.W, and Click, M. (2008) Virtual fragment linking an approach to identify potent binders from low affinity fragment hits. Journal of Medicinal Chemistry, 51, 2481-2491. 

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