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2 000 new building blocks are synthesized monthly. Here is an important update to our MedChem Highlights from December 2021

Recent News

  • 22 November 2021   Press Releases

    Enamine makes HFIPS reagent more accessible

    Kyiv, Ukraine, 22 November 2021. Recently, Prof. Magolan and coworkers from McMaster University (Hamilton, Ontario, Canada) reported that hexafluoroisopropyl sulfamate (HFIPS) is a convenient reagent for the sulfamoylation of alcohols and amines (Org. Lett. 2021, 23, 3373–3378). HFIPS has also been used for metal-catalyzed C–H aminations (J. Am. Chem. Soc. 2014, 136, 5783–5789) and for the synthesis of aziridines using silver catalysis (Synthesis 2018, 50, 4462–4470) or electrochemical conditions (Angew. Chem. Int. Ed. 2018, 57, 5695–5698). Enamine has adapted and scaled-up the published procedure to synthesize HFIPS and make it more accessible to scientists worldwide. The reagent is now available in Enamine’s catalogue in multigram quantities.

    Iryna Iavniuk, Business Development Director at Enamine, comments: “We at Enamine are committed to making novel reagents immediately accessible to our customers. We have successfully applied the HFIPS reagent in one of our projects previously and were happy to produce it for commercialization.”

    Prof. Dr. Oleksandr Grygorenko, Consulting Scientist at Enamine, explains: “Dr. Jarrod Johnson, a Research Associate in the Magolan group, contacted us to point out that there was a supply gap with HFIPS. We recognized the usefulness of the reagent and happily agreed to begin commercialization. Our chemists quickly reproduced the published procedure to synthesize 50 grams of the reagent and HFIPS is now available from EnamineStore: https://www.enaminestore.com/catalog/EN300-1987789.”

    Dr. Jarrod Johnson from McMaster University, adds: “We like the ease and simplicity of using HFIPS for sulfamoylation chemistry and hope it might become the go-to reagent for medicinal chemists making sulfamates and sulfamides.”

    Prof. Dr. Jakob Magolan from McMaster University, comments: “It’s great to see Enamine now offering bulk HFIPS. I expect that this will enable creative scientists around the world to further extend the scope and applicability of this useful little reagent.”

    Conflict of interest statement: Hereby the parties confirm that Prof. Magolan and his group have no financial interest in commercialization of EN300-1987789. No specialized data was transferred to Enamine apart from that already published in the literature.


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  • 18 October 2021   Press Releases

    Enamine brings Levin “nitrogen-deleting” reagent to the market

    Kyiv, Ukraine, 18 October 2021. Several months ago, Prof. Levin and co-workers from University of Chicago developed an elegant method for the “skeletal editing” of organic molecules by nitrogen atom deletion (see Nature 2021, 593, 223–227). Their strategy included the use of an anomeric N-pivaloyloxy-N-alkoxyamide amide as the key reagent. Enamine, the world-leading compound supplier, is proud to announce that this reagent has been just added to the company’s product catalog. The compound is now available from the company’s stock in multigram quantities.

    Iryna Iavniuk, Business Development Director at Enamine, explains: “We at Enamine always look for the most recent scientific findings in all areas of chemistry and use them to expand and improve our products immediately. We were happy to collaborate with Mark Levin on the commercialization of his fascinating reagent – a remarkable addition to our reagent collection.”

    Prof. Dr. Oleksandr Grygorenko, Consulting Scientist at Enamine, adds: “I was really excited when I saw Prof. Levin’s Nature publication on the nitrogen deletion method while surfing the literature. When Mark contacted us, we readily agreed to collaborate. Our chemists quickly reproduced his published protocols, performed scale-up to 50 g of the reagent, demonstrated its applicability, and checked the storage stability. Now, the compound is available from EnamineStore: https://www.enaminestore.com/catalog/EN300-33050767

    Prof. Dr. Mark Levin, Assistant Professor at University of Chicago, comments: “Hopefully anyone who wants to give our methods a whirl will be able to take advantage of this wonderful offering from Enamine. I am looking forward to all the creative applications of nitrogen deletion that this will enable!”

    Conflict of interest statement: Hereby the parties confirm that Prof. Levin or his group has no financial interest in commercialization of EN300-33050767. No specialized data was transferred to Enamine apart from that already published in the literature.


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Upcoming events

We offer over 60 ready-to-deliver pre-plated compound libraries in a variety of custom formats. Our well-equipped liquid handling department will make a library copy in any convenient for you project format.


Diversity Libraries

Product name
Size
Descriptions
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Size

50 240 compounds

Descriptions

Top-quality diverse library of recently synthesized compounds

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10 240 compounds

Descriptions

High-quality diverse library of latest compounds

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Size

11 200 compounds

Descriptions

Diverse Covalent Library with most demanded warhead types

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Size

5 760 compounds

Descriptions

Special diversity library created for Phenotypic Screens

Download file

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PAINS Library

PAINS-320

Size

320 compounds

Descriptions

Special diverse selection of frequent hitters

Download file

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Macrocycles

MCR-320

Size

320 compounds

Descriptions

Original design beyong Ro5 compounds

Download file

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Covalent Libraries

Product name
Size
Descriptions
Download file

Size

11 200 compounds

Descriptions

Diverse Covalent Library with most demanded warhead types

Download file

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Size

12 560 compounds

Descriptions

Designed for discovery of mild electrophilic inhibitors of the largest enzyme class

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Size

2 640 compounds

Descriptions

Designed for the discovery of new SARS-CoV-2 and pan-Coronavirus antivirals

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Size

7 360 fragments

Descriptions

Diverse covalent warheads with balanced reactivity

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Size

3 200 fragments

Descriptions

Library of Cys-specific covalent electrophilic binders

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Size

1 600 fragments

Descriptions

Special selection of Serine focused irreversible binders

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Size

1 600 fragments

Descriptions

A unique set of 1 600 Lys specific binders

Download file

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Size

960 fragments

Descriptions

Characterized by a new HTS thiol-reactivity assay

Download file

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Acrylamide Library

sACR-4080

Size

4 080 compounds

Descriptions

Diverse screening Acrylamides pre-plated at 10 mM concentration

Download file

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Size

2 240 compounds

Descriptions

Representative selection of fragment Acrylamides pre-plated at 100 mM stock concentration

Download file

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Chloroacetamides

sCLA-1200

Size

1 200 compounds

Descriptions

Library of diverse HTS-size chloroacetamides pre-plated at 10 mM concentration

Download file

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Size

1 360 compounds

Descriptions

Diverse strict Ro3 compliant chloroacetamides plated at 100 mM stock concentartion

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Size

640 compounds

Descriptions

Representative selection of N-, O-linked and Aryl sulfonyl fluorides within fragment space

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Targeted Libraries

Product name
Size
Descriptions
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Size

10 240 compounds

Descriptions

Library of compounds intended for use in agro/crop science

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Size

14 400 compounds

Descriptions

Designed for discovery of novel allosteric ligands

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Size

4 800 compounds

Descriptions

Carefully selected molecules via docking and visual evaluation

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Size

3 200 compounds

Descriptions

Designed for discovery of new Nucleoside-like antivirals

Download file

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Size

10 560 compounds

Descriptions

Designed for discovery of new Voltage-gated calcium channel blockers

Download file

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CNS Library

CNS-56

Size

56 320 compounds

Descriptions

Library of novel small molecules with high CNS MPO scores

Download file

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Size

16 800 compounds

Descriptions

Designed for the discovery of new SARS-CoV-2 and pan-Coronavirus antivirals

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Size

2 470 compounds

Descriptions

Specially synthesized set of compounds able to mimic glycosides and their interaction with proteins

Download file

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GPCR Library

GPR-54

Size

54 080 compounds

Descriptions

Designed for discovery of new GPCR ligands

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Size

24 000 compounds

Descriptions

Designed for discovery of novel kinase ATP pocket binders

Download file

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Size

1 003 compounds

Descriptions

IDO focused library designed by a combination of structure- and ligand-based methods

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Size

36 800 compounds

Descriptions

Designed for discovery of new Ion Channels ligands

Download file

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Size

65 200 compounds

Descriptions

Designed for discovery of novel protein kinase inhibitors

Download file

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Size

5 440 compounds

Descriptions

A sub-library of Enamine’s GPCR Library designed for discovery of novel lipid GPCR ligands

Download file

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Size

2 468 compounds

Descriptions

A set of compounds focused on targeting molecular chaperones

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Size

320 compounds

Descriptions

Small library of specially synthesized compounds

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Size

1 920 compounds

Descriptions

Sublibrary of PPI-40

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Size

8 960 compounds

Descriptions

Selected molecules able to mimic common protein motifs

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Size

40 640 compounds

Descriptions

Designed for discovery of novel PPI inhibitors

Download file

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RNA Library

RNA-15520

Size

15 520 compounds

Descriptions

Library of compounds capable of binding to RNA

Download file

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Size

12 560 compounds

Descriptions

Designed for discovery of mild electrophilic inhibitors of the largest enzyme class

Download file

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Size

5 440 compounds

Descriptions

Designed for discovery of new Nav1.7 channel blockers

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Bioreference Libraries

Product name
Size
Descriptions
Download file

Size

2 100 compounds

Descriptions

Library of well-known bioactive compounds with extensive target classes’ coverage and the broadest possible therapeutic areas applications – from CNS agents and anti-infectives to anticancer drugs and steroids

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Size

646 compounds

Descriptions

A unique library of most diverse drugs

Download file

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Size

5 760 compounds

Descriptions

Special diversity library created for Phenotypic Screens

Download file

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CLOUD

CLOUD-293

Size

293 compounds

Descriptions

The comprehensive Drug Collection

Download file

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Size

1 454 compounds

Descriptions

Versatile product to use in Drug Discovery

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PAINS Library

PAINS-320

Size

320 compounds

Descriptions

Special diverse selection of frequent hitters

Download file

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Fragment Libraries

Product name
Size
Descriptions
Download file

Size

320 compounds

Descriptions

Elaborated tool for initial screen

Download file

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Size

1 920 compounds

Descriptions

Fragments of high MedChem tractability

Download file

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Size

860 compounds

Descriptions

Designed for easy and rapid follow-up synthesis

Download file

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Size

80 compounds

Descriptions

Guiding optimisation of fragment-derived lead compounds

Download file

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Size

7 360 fragments

Descriptions

Diverse covalent warheads with balanced reactivity

Download file

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Size

1 000 compounds

Descriptions

Specially designed for 19F NMR ligand-based screening

Download file

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Size

640 fragments

Descriptions

Designed for easy and efficient exploration of novel protein targets

Download file

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Size

4 160 compounds

Descriptions

Source of biologically validated starting points

Download file

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Size

1 200 compounds

Descriptions

Unique 3D diversity among shaped molecules

Download file

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Size

3 600 compounds

Descriptions

Fragments able to mimic protein structural motifs and hot-spot residues

Download file

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Size

1 500 compounds

Descriptions

Fragments for easy-to-analyse protein-ligand interaction

Download file

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Size

4 000 compounds

Descriptions

Designed for specific protein targets and sensible onset

Download file

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Size

960 fragments

Descriptions

Characterized by a new HTS thiol-reactivity assay

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Cereblon ligands and functionalized intermediates

CRBN binders and their functionalized analogs

Cereblon (CRBN) is one of the most explored E3 ligase used for the construction of PROTACs and different functionalized tool compounds. The most extensive research has been done in this area. We have also been working on thalidomide-like and glutarimide chemistry for years and gained versatile experience in this chemistry field. New Building Blocks have been synthesized along with extensively elaborated approaches in modification of common intermediates. This knowledge allowed as to create over 500 000 REAL CRBN focused compounds based on a range of synthesized in-stock intermediates.


Building Blocks for parallel chemistry

  • CRBN Building Blocks in stock – over 200 intermediates
  • CRBN MADE Building Blocks – 10 000+ compounds
  • CRBN MADE Building Blocks with linkers – over 80 000 compounds

CRBN focused products

  • Thalidomide-like, and other celebron ligands and ligands with linkers in-stock – 2 000
  • Glutarimides in stock – over 3 000 compounds
  • CRBN binders – pre-plated 320 compounds
  • REAL Molecular Glues – 1M+ compounds
  • Custom CRBN ligands and ligands with linkers
  • REAL CRBN ligands with covalent warheads

  Contact our experts

Representative examples of CRBN binders with varying linkers

PAINS Library

Special diverse selection of frequent hitters

320 compounds

Pan-Assay Interference Compounds (PAINS) are the most recognized filters among medicinal chemists. Since first publication in 2010 by John Bell these filters have become industry standard in Drug Discovery. While carefully removing all PAINS-related compounds from Enamine libraries we realized that these compounds can be very useful in HTS assay set-up & validation.

Special diversity set of PAINS available for prompt delivery in various plated formats including the most popular listed below:

Catalog No.
Compounds
Amount
Format
Price

Catalog No.

PAINS-320-10-Y-10

Compounds

320
one plate

Amount

10 μL of 10 mM DMSO solutions

Plates and formats

384-well acoustic plates, Labcyte #PP-0200,
last two columns empty;

Price

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Catalog No.

PAINS-320-50-Y-10

Compounds

320
one plate

Amount

50 μL of 10 mM DMSO solutions

Plates and formats

384-well plates, Greiner #784201,
1, 2 and 23, 24 columns empty;
320 compounds per plate

Price

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Catalog No.

PAINS-320-100-X-10

Compounds

320
four plates

Amount

100 μL of 10 mM DMSO solutions

Plates and formats

96-well plates, Greiner #65021,
1 and 12 columns empty;
80 compounds per plate

Price

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Please request for any other options through our contact form. We will be happy to deliver our library in any convenient for your project formats.

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Library design

The design is based on substructural motifs of known PAINS compounds. We used originally reported PAINS filters to identify a set of 75k+ in-stock compounds. This set was clustered using fingerprint-based approach and Tanimoto similarity distance calculations. The most populated clusters with at least 5 compounds were extracted and one representative example was selected from each cluster resulting in a library of 320 compounds. The library of most diverse 320 PAINS is available in plate format for your convenience. Examples are given below.

Key features

  • Represents the most common false positives
  • Substructure & scaffold diversity
  • All compounds suitable for storage as DMSO solutions

Example of structures and their specific PAINS filters

SPLicing inhibitor sulfonAMides (SPLAMs)

New aryl sulfonamides designed to target DCAF family of E3 ligases

For a long time, Indisulam and a few other clinically tested aryl sulfonamides such as Tasisulam and chloroquinoxaline sulfonamide (CQS) remained compounds with pronounced selective in vitro anticancer activity with unclear mechanism of action.

Recent extensive investigations in cancer genome sequencing together with X-Ray crystallography and cryo-electron microscopy showed that these compounds (also known as SPLAMs - SPLicing inhibitor sulfonAMides) act as a “molecular glue” to induce degradation via binding to DCAF15. This insight provided structural and mechanistic data that significantly extend our understanding of their mode of action.

E7820

Indisulam

Tasisulam

CQS

Based on these emerging data we have designed several focused compound libraries of aryl sulfonamides both using selections from our Screening Collection and employing enumerations of new REAL compounds that we can confidently synthesize:

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Library design

Recent studies demonstrated that SPLAMs promote the interaction between RBM39 and DCAF15 E3 ligase receptor, leading to ubiquitination of RBM39 and proteasome-mediated degradation.

According to the structural data Indisulam and Tasisulam bind DCAF15 in an overall configuration similar to E7820, maintaining the backbone hydrogen bonds from the sulfonyl groups to DCAF15 Ala234 and Phe235 and the water mediated hydrogen bonds. However, the methyl to hydrogen substitution at C4 in Indisulam limits the hydrophobic interactions with DCAF15 Val477 and Val556, while Tasisulam lacks the indole NH hydrogen bond to the backbone carbonyl of DCAF15 Phe231.

Based on the available structural data we have designed DCAF15 Focused Library from our stock Screening Collection using the following approach:

  • Generation and selection of close chemotypes/scaffolds based on diverse aryl and heteroaryl (five-membered inclusive) sulfonamides;
  • Further selection based on pharmacophore modelling and docking results using available structural data of DCAF15;
  • MedChem filtering according to criteria of lead/drug likeness.
Docking results

Figure 1. Docking results

Figure 2. Examples of SPLAM analogues

Sodium Ion Channel Library

Designed for discovery of new Nav1.7 channel blockers

5 440 compounds

Sodium voltage-gated ion channel considered to be an important component in nociception. Therefore, selective Nav1.7 channel blockers are considered as important novel analgesics.

Analyzing the structures of recently developed ligands several main features have been identified:

  • the most abundant are relatively flat aromatic cores;
  • presence of highly polar backbone fragments/moieties (e.g. CONH2, SO2NHR, polar heterocycles, etc);
  • compounds lay squarely in the middle of drug-like chemical space.

A set of substructure queries and 2D-fingerprintes based on found common structural motives and pharmacophores was used in searching Enamine screening collection to result in 6,209 compounds after application of medchem filters. The Nav1.7 Targeted Library is rich in compounds bearing saturated backbones that can be often seen in structures of other ion-channel blockers. All compounds meet requirements of Ro5, and 67% compounds are considered lead-like.

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Molecular properties

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