Nuclear Receptor Ligands
Nuclear receptors are involved in a wide range of physiological key functions and constitute an important class of drug targets for treatment of cancer, inflammatory diseases and diabetes.
- Collection of 99 bioactive compounds targeting nuclear receptors used in Nuclear Receptor compound screening
- Supported with full bioactivity annotation, pathway indications and all related chemical structure information (structure, CAS, smiles, molecular parameters)
- NMR and HPLC validated to ensure the highest purity
- Supplied in 96 or 384-well plates, ready for shipping
- Minimal preparation – just peel, dilute & transfer to assay plate
Target distribution
Transporters
Transporters play a particularly important role in chemical signaling between neurons in the CNS, where they act to control the concentration of neurotransmitters in the synapse. Another key role for transporters is in excluding undesirable xenobiotics from the cell, whilst allowing key molecules required for the cell life cycle to enter. The majority of transporters are targets for drug discovery.
- Collection offers near 200 transporter modulators proposed for screening and drug development projects
- Supported with full bioactivity annotation, pathway indications and all related chemical structure information (structure, CAS, smiles, molecular parameters)
- NMR and HPLC validated to ensure the highest purity
- Supplied in 96 or 384-well plates, ready for shipping
- Minimal preparation – just peel, dilute & transfer to assay plate
Target distribution
Protease Inhibitors
A convenient and cost-effective way to purchase a panel of protease inhibitors for chemical genomics, assay development, and other applications
Protease inhibitors are well known as one of the prime candidates to have numerous applications in biotechnology and medicine. These are very important tools for better interpretation of basic principles of protein interactions and the designing of new compounds for the control of pathologic processes and many diseases.
- Collection includes about 117 known protease inhibitors
- Supported with full bioactivity annotation, pathway indications and all related chemical structure information (structure, CAS, smiles, molecular parameters)
- NMR and HPLC validated to ensure the highest purity
- Supplied in 96 or 384-well plates, ready for shipping
- Minimal preparation – just peel, dilute & transfer to assay plate
Target distribution
Compounds with annotated activity data
more than 30,000 compounds
Our Bioactive Collection brings together over 30,000 compounds with documented biological activity. This includes around 1,200 FDA-approved drugs, as well as tool compounds, metabolites, prodrugs, and drug candidates currently in clinical trials.
Through our collaboration with Pfizer, Enamine also offers a curated selection of Pfizer Reference Compounds EnamineStore — including exploratory molecules, research tools, investigational drugs, and isotope-labeled standards. All compounds are fully characterized and quality-controlled, providing trusted tools for drug discovery research.
- Data you can rely on
Every compound is fully annotated with literature references and biological activity data. - Custom sourcing
Need something beyond the catalog? We can deliver almost any compound through in-house synthesis or our global supplier network. - Expand with analogs
Discover analogs through searches across 94.5B compounds across our Screening Collections, REAL Database and REAL Space or by enumeration of new hit follow-up libraries.
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A comprehensive searchable database including literature references and activity/selectivity values towards different targets is available through a custom request form.
The World largest and continuously enhanced source of in-stock fragments
330 020 compounds
Fragment screening has become a mainstream technology in small molecules Drug Discovery programs and not only. Chemical Biology, which is extremely rapidly evolving now, needs reliable tools to navigate research. Fragments have also proved their efficacy in the discovery of new chemical probes, which reveal fundamental biological insights.
Committed to expanding chemical space Enamine has synthesized over 300 000 building blocks and developed REAL Compounds, both to contribute to the success of its abundant Fragment Collection. Not only reflect our fragments contemporary trends in FBDD, such as fragments bearing covalent warheads and photolabels, but also can they be easily grown into leads. All fragments can be easily followed with analogues from stock or through express synthesis.
We collaborate with the leading experts in FBDD to design and synthesize libraries for the most challenging projects filling gaps in the accessible chemical space. We continuously improve the quality of our fragments by providing more assurance on their solubility and stability. We keep screening our new fragments to assure stability of DMSO solutions and comply with solubility of at least 100 mM in DMSO and 1 mM in aqueous buffer.
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Key features
- Novelty and high chemotype diversity
- Replenished, significant amount in stock, typically 100 mg+ and purity 95%
- Design of custom libraries – target focused, assay-dedicated or chemotype based
- Close analogs in stock and quick follow-up library synthesis
- Hit confirmation and follow-up support
Currently, we offer 14 different pre-plated fragment libraries. We extensively work on improvement of all fragment libraries to bring the best starting points to your Fragment screening campaign.
Our presence in global FBDD
- Moonshot COVID-19 project: Fragment to lead
- Enamine to be the exclusive supplier of Astex’ MiniFrag Library. Read press release >>>
- Enamine Supplies DSI Poised Fragment and Analogue Libraries to Diamond Light Source1 XChem Facility and SGC Oxford. Read press release >>>
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Fragment libraries designed to be functionally diverse recover protein binding information more efficiently than standard structurally diverse libraries
Carbery A., Skyner R., von Delft F., Deane CM. Cold Spring Harbor Laboratory 2022. DOI: 10.1101/2022.03.18.484642 -
Rapid Covalent-Probe Discovery by Electrophile-Fragment Screening
Resnick E., Bradley A., Gan J. et al. J. Am. Chem. Soc. 2019, 141, 22, 8951–8968. DOI: 10.1021/jacs.9b02822 -
Expanding the Repertoire of Low-Molecular-Weight Pentafluorosulfanyl-Substituted Scaffolds
Jose A., Guest D., LeGay R. et al. ChemMedChem. 2022, 17(7), e202100641. DOI: 10.1002/cmdc.202100641 -
An automatic pipeline for the design of irreversible derivatives identifies a potent SARS-CoV-2 Mpro inhibitor
Zaidman D., Gehrtz P., Filep M. et al. Cell Chem Biol. 2021, 28(12), 1795-1806. DOI: 10.1016/j.chembiol.2021.05.018 -
(Chlorosulfonyl)benzenesulfonyl Fluorides-Versatile Building Blocks for Combinatorial Chemistry: Design, Synthesis and Evaluation of a Covalent Inhibitor Library
Tolmachova K., Moroz Y., Konovets A. et al. ACS Comb. Sci. 2018, 20, 11, 672–680. DOI: 10.1021/acscombsci.8b00130 -
NMR quality control of fragment libraries for screening
Sreeramulu S., Richter C., Kuehn T. et al. J Biomol NMR. 2020, 74(10-11), 555-563. DOI: 10.1007/s10858-020-00327-9 -
Crystallographic and electrophilic fragment screening of the SARS-CoV-2 main protease
Douangamath A., Fearon D., Gehrtz P. et al. Nat Commun. 2020, 11(1), 5047. DOI: 10.1038/s41467-020-18709-w