Oral administration is the first choice for clinical drug delivery, especially for long-term use. It is also the safest, most convenient, and most economical method of drug delivery. Oral bioavailability is the percentage of the absorbed drug dose successfully passed through the mucosa of the gastrointestinal tract and entered the bloodstream through the liver, to the original given oral dose. Drugs with high oral bioavailability can achieve efficacy at lower doses and effectively reduce toxic side effects; while when bioavailability is too low, even compounds with good pharmacological activity are unable to be fully exposed and utilized at the target site, resulting in therapeutic failure or high dose with large toxic side effects, which eventually leads to drug development failure and limits the application.

TargetMol has carefully collected 3160 compounds with publicly reported oral activity that can be used for drug repurposing and development of orally active drugs.