ActiTarg Series · 2,000+ compounds
ActiTarg-P Protease Inhibitors
Low-molecular-weight, drug-like compounds with potential protease inhibitory activity — 2,000+ members, with a 1,520-compound diversity-selected set.
ActiTarg-P is a screening set of low-molecular-weight, drug-like compounds from TimTec stock with potential protease inhibitory activity. The collection includes 2,000+ pre-filtered compounds from several chemical series. Structural constraints and novel pendants provide variability for hit optimization. A top diversity-selected set of 1,520 protease inhibitors is available in smaller sets of 3, 5, 10, 15, or 19 plates with 80 compounds per plate. Dense subsets listed in the catalog are ActiTarg-240, ActiTarg-400, ActiTarg-800, and ActiTarg-1,520. Compounds are available for cherry-picking and/or as the 1,520-compound collection in 96- or 384-well plates and in vials.
Lattices represented
| Protease context | Lattice type |
|---|---|
| Coagulation cascade | Various |
| Aspartyl | N-AcAla |
| MMP | Succinate-OH; acylGly-OH; sulfonylGly-OH; N-ArethylGly-OH; pyrimidine-trione |
Published screens that used ActiTarg-P
These are literature reports, not TimTec efficacy claims:
- Pribis, J. P.; Al-Abed, Y.; Yang, H.; et al. The HIV protease inhibitor saquinavir inhibits HMGB1-driven inflammation by targeting the interaction of cathepsin V with TLR4/MyD88. Mol. Med. 2015, 21, 749–757. doi:10.2119/molmed.2015.00197. Screened the TimTec ACTITARG-P library (1,520 protease inhibitors).
- Druzhyna, N.; et al. Screening of a composite library of clinically used drugs and well-characterized pharmacological compounds for cystathionine β-synthase inhibition identifies benserazide as a drug potentially suitable for repurposing for the experimental therapy of colon cancer. Pharmacol. Res. 2016, 113, 18–37. doi:10.1016/j.phrs.2016.08.016. Composite screen included ActiTarg-P (1,140 proteinase inhibitors) from TimTec.
ActiTarg is one of TimTec’s targeted series. See the ActiTarg Series for the other letter collections.