Serine focused Covalent Fragments

Special selection of Serine focused irreversible binders

1 600 compounds

The Serine hydrolase enzyme family is one of the largest and most diverse protein classes, including proteases, lipases, esterases, thioesterases, amidases and peptidases. All these enzymes utilize a base-activated Serine residue cleavage of amide bonds in substrates via a covalent acyl-enzyme intermediate.

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Different specific covalent-acting chemical probes have increasingly been used in proteome-wide target identification and imaging and for finding inhibitors with high specificity among related enzymes and enzyme isoforms. Significant number of known covalent drugs and natural products have approved efficacy of such approach in drug discovery.

Our library of Serine focused covalent fragments is available in versatile pre-plated formats for most convenient and fast delivery. All compounds passed QC check (90%+ purity) before formatting to ensure quality of the library.

Typical Formats

Catalog No.
Compounds
Amount
Format
Price

Catalog No.

SER-1600-10-Y-100

Compounds

1 600
5 plates

Amount

10 µL of 100 mM DMSO solutions

Plates and formats

384-well plates Greiner Cat. No 781280,
first two and last two columns empty,
320 compounds per plate

Price

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Catalog No.

SER-1600-50-Y-100

Compounds

1 600
5 plates

Amount

50 µL of 100 mM solutions in DMSO

Plates and formats

384-well plates, Labcyte Cat. No PP-0200,
1,2 & 23,24 columns empty,
320 compounds per plate

Price

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Catalog No.

SER-1600-100-X-20

Compounds

1 600
20 plates

Amount

100 µL of 20 mM DMSO solutions

Plates and formats

96-well plates, Greiner Cat. No 651201,
1 & 12 columns empty,
80 compounds per plate

Price

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Catalog No.

SER-1600

Compounds

1 600

Amount

Custom

Plates and formats

Any custom format

Price

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Examples of compounds in the library

Library Design

Recently elaborated approaches to parallel synthesis, allowed Enamine to synthesize the largest commercial source of covalent binders. We focused our efforts on synthesis of compounds with most reliable covalent warheads, with well determined reactivity. Our Serine focused library was designed based on a combination of specific moieties, reported to form covalent bonds particularly with Serine residue and presence of a drug-like, MedChem friendly core in a molecule. The library has also been shaped with Ro3 criteria to meet all requirements of FBDD.

The following functional groups, reported to form covalent bonds in proteins with Ser residue, have been used for construction of the library:

  • Sulfonyl fluorides, fluorosulfonates and sulfamoyl fluorides
  • Epoxides
  • β-lactams and β-Propiolactone
  • Boronic acids and pinacolates
  • Aldehydes

Hits derived from this library can be easily followed with analogues from over 3M stock compounds or either synthesis of new compounds through REAL Database technology within 3 weeks only.

We provide Hit Confirmation support for all our libraries with the samples resupply from dry powders, QC check and HPLC repurification. Hits can be resynthesized in 2 weeks only.

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