SAR structure-activity

M. G. J. Beets, SAR Structure—Activity Relationships in Human Chemoreception, AppHed Science Pubhshers, London, 1978. 

The third step is to optimize the lead molecule through iterative chemical synthesis and biological testing, aiming to obtain molecules with the required potency (typically nanomolar), selectivity, bioavailability, and DMPK (drug metabolism and pharmacokinetics) properties. This step usually requires considerable time and resources usually the synthesis of hundreds of compounds is needed to deduce a robust SAR (structure-activity relationship). Such resources can be considerably reduced and the... 

SAR—structure-activity relationship SC—subcutaneous SH—sulfhydryl SL—sublingual S02—sulfur dioxide... 

If the assignment is available or can be made in reasonable time (and preferably, but not necessarily, if the protein structure is approximately known), the location of the binding site may be easily derived. This method is currently implemented in the so-called SAR (Structure-Activity Relationship) by NMR technique [13]. 

IKK I/cB kinase NBD NEMO binding domain NEMO NF/cB essential modulator NOE Nuclear Overhauser elfect RDC Residual dipolar coupling SAR Structure-activity relationship trCCR Transferred OCR trNOE Transferred NOE... 

---