Macrocycles · 15,200 compounds
MAC-15000 Macrocycle Screening Collection
Peptidomimetic macrocycles with conformationally constrained cores that mimic peptide secondary structure — 15,200 compounds for ligand discovery.
Peptidomimetic libraries are central to discovering ligands with high activity, specificity, and affinity for many therapeutically relevant targets. Synthetic analogs of natural peptides can mimic key structural elements of natural ligands and elicit the desired biological response, yet metabolic liabilities—peptidase cleavage and limited membrane permeability—still need to be addressed. Macrocyclization of peptidomimetics is a well-supported strategy for improving these properties, so macrocyclic peptidomimetic collections are a practical starting point for drug discovery.
TimTec continues to refine macrocyclic designs that mimic biologically relevant di- and tripeptide motifs and can serve as topological mimics of peptide secondary structure (for example, α-helices and β-turns). The approach centers on conformationally constrained macrocyclic cores that typically contain two to four cyclic amide groups, plus additional diversity points for introducing lipophilic or hydrophilic side chains. Two principal routes are used: macrolactamization of an amino acid precursor, and ring-closing metathesis (RCM) of bis-olefin precursors. TimTec’s peptidic macrocycles tend to be larger than scaffold-based non-peptidic macrocycles; many still show favorable aqueous solubility and membrane permeability in PAMPA and Caco-2 assays.
Physical-chemical range
| Parameter | Value |
|---|---|
| Compounds | 15,200 |
| Format | Plate-based (190 plates; well positions recorded) |
| MW (STRUCT_MW), min | ~248.3 g/mol |
| MW (STRUCT_MW), max | ~865.1 g/mol |
| MW (STRUCT_MW), average | ~503.9 g/mol |
| Identifiers | VIAL_ID, PLATE_ID, CELL |
Per-sample pricing (10 mM DMSO)
| Volume | Price |
|---|---|
| 50 µL | $18.00 |
| 100 µL | $21.00 |
Browse live collection listings at structure.timtec.org/collections or look up identifiers at ID / SMILES search.
Published screens
None listed yet.
Ask for the current SDF and plate map before designing a campaign; membership can change as lots are retired or replaced.