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Soft Electrophiles


Recent research has shown that covalent inhibitors have a number ofadvantages in drug discovery, especially for targets where complete inactivation is required. ASINEX has, therefore, crafted a unique set of molecules containing mild electrophilic moieties that covalently interact with amino acid residues in the target protein. The diversity of our compounds for covalent drug discovery ranges from natural product-like scaffolds to macrocycles, creating multiple opportunities in hit generation for a selected target. All our soft electrophile compounds possess a reactive “warhead” which is designed to interact with a nucleophilic residue at the binding site while the remaining part of the compound is deemed to govern specific recognition.Examples of efficient electrophilic warheads include chloroacetamides, acrylamides, epoxides, nitriles, and electron-deficient ketones.
The Asinex covalent library encompasses a legacy of extensive enrichment of our compound collection with novel drug-like chemotypes based on natural product-inspired chemistry. New entities are added to the library on a regular basis to increase the number of freshly synthesized compounds that comprise this set. Due to the intrinsic reactivity of molecules containing a covalent reactive group we have implemented rigorous quality control and efficient compound management logistics (storage and handling) to ensure consistent screening results.

A number of smaller, more focused libraries (Signature Libraries) are also available for screening:

SL#019 Soft Electrophiles-1 (acrylamide derivatives)
SL#020 Soft Electrophiles-2 (heterocyclic cinnaminc acid derivatives)
SL#022 Soft Electrophiles-3 (kinase-oriented cinnaminc acid derivatives)
SL#027 Soft Electrophiles-4 (ɑ-oxyketone and spiro-lactone derivatives)
SL#037 Soft Electrophiles-5 (heteroaromatic nitrile derivatives)
Please visit our online catalog for available Covalent libraries or contact our customer support team for any additional information.

Product Name: Format/Size Descriptions Download
Soft Electrophiles
(Covalent Library 1)
782 compounds
For cherry-picking
Update: 2022-08
The file contains newly synthesized compounds that passed HPLC purification and strict quality control.
Soft Electrophiles
(Covalent Library 2)
8085 compounds
For cherry-picking
Update: 2021-04
The file contains all available Soft Electrophiles selected from our Signature & BioDesign Libraries.
SL#019
Soft Electrophiles-1
(acrylamide derivatives)
80 compounds
Pre-Plated Set
Release: 2016
ASINEX has created a library of acrylamide derivatives by combining proprietary glycomimetic or peptidomimetic fragments with selected amino acrylic acids known as “soft” electrophiles that bind to Cys residues.
SL#020
Soft Electrophiles-2
(heterocylic cinnaminc acid)
80 compounds
Pre-Plated Set
Release: 2016
ASINEX has created a library of heterocylic cinnaminc acid derivatives by coupling with proprietary fragments. Cinnamic acid and its derivatives are found among natural products that are known for their anti-inflammatory, anti-cancer, and cardio-protective properties. [1]
SL#022
Soft Electrophiles-3
(kinase+hetero-cinnamic acids)
80 compounds
Pre-Plated Set
Release: 2016
ASINEX has created a library of kinase-oriented small molecules by attaching electrophilic hetero-cinnamic acids to various kinase hinge-binding scaffolds. It is hypothesized that a Michael acceptor moiety of cinnamic acid is able to interact with Cys residues presented at the binding site. The resulting set represents a unique research tool for the discovery and optimization of new inhibitors across the kinome.
SL#027
Soft Electrophiles-4
(ɑ-oxyketone and
spiro-lactone)
80 compounds
Pre-Plated Set
Release: 2016
ASINEX has created a library of ɑ-oxyketone and spiro-lactone derivatives that contain mild electrophilic functional groups. Both lactones and oxyketones provide interesting small molecule probes for covalent drug discovery across multiple disease areas [2] as they interact with nucleophilic residues (e.g. Ser, Thr, Lys and Cys) of target proteins.
SL#037
Soft Electrophiles-5
(heteroaromatic nitrile
derivatives)
80 compounds
Pre-Plated Set
Release: 2016
ASINEX has created a library of heteroaromatic nitrile derivatives which have kinase-oriented pharmacophoric elements. These compounds are useful for the discovery of novel kinase inhibitors with improved safety, target selectivity, and pharmacokinetic properties.
Contact
Global

Ludmila Sadovenko

lsadovenko@asinex.com
North America

Mark Parisi

mparisi@asinex.com

Toll Free: +1 877 ASINEX1

Tel: +1 336 721 1617

Fax: +1 336 721 1618

N.Chestnut St., Ste.104

Winston-Salem, NC 27101

USA

Europe

Galina Afanasyeva

gafanasyeva@asinex.com

Tel: +31 (0) 203416183

Klaprozenweg 75C, 1033NN

Amsterdam, The Netherlands

Japan

Shingo Ota

sota@asinex.com

Tel: 080-3401-9097

30-2 Higashihazu, Nishio,

Aichi Japan

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