Enamine Ltd

We offer comprehensive support in developing your hit compounds. Naturally such programs are realised most efficiently when biological actives originate from our screening collection. However, even if the hit compounds are from the collections of other vendors lead identification and optimization projects can proceed most productively in our hands. Sometimes for this we only need to synthesize first examples of the given chemical series and validate synthesis route.

Re-supply and re-synthesis of hit compounds.

We will help you to assess quality of your hit compounds by pointing out at possible promiscuous structures, frequent hitters, and by revising their analytics in our archive. In most cases we can deliver additional amounts of the hit compounds directly from our stock. Otherwise we can re-synthesize them fairly quickly taking advantage of the chemical procedures and building blocks available in-house. All compounds from our screening collection were designed and synthesized in our laboratories. This means that we possess both knowledge and starting materials to prepare larger batches of the selected compounds within the shortest possible timeframe. Re-synthesis samples will be delivered with certificates of analysis including NMR and LCMS data reports. Upon project finalization we can provide you with detailed chemical procedures to use them in your publications or patent applications.

Compound libraries supplies for hit explosion, lead generation and optimization.

We will be happy to work with you and assist you, as you would need, in design of focused libraries in any phase of your project and provide you with adequate medicinal chemistry support. Usually synthesis of close analogues takes only a few weeks, if not already available on our stock. The compounds, especially in the early lead discovery phase, are delivered on a fixed-price basis implying zero risks on your side: you only pay for the compounds that are delivered according to your exact specifications and the final report provided. In the advanced collaboration phase with dynamically changing synthesis plans it becomes more appropriate to establish an FTE service agreement for several months. Exact duration depends on the nature of the project. Enamine offers most attractive FTE rate in Eastern Europe which, in addition, includes access to the world’s largest inventory of building blocks used in medicinal chemistry. Services for lead generation and optimization can be further supported with CADD and ADME-PK studies of the synthesized compounds directly at Enamine.

We are offering a broad range of in vitro ADMET services, either as separate studies or as value-adding extensions of our in-house biomolecular screening and medicinal chemistry service projects.

The list of standard in vitro ADMET tests includes:
Aqueous compound solubility (nephelometry, filter plate or shake flask protocols, UV or LS-MS-MS detection)
logD/logP (n-octanol:aqueous buffer)
Plasma protein binding (human, rat, mouse), albumin binding
Compound stability in plasma, aqueous buffers, solvents
Microsomal stability (human, rat, mouse)
CYP450 inhibition, major isoforms
PAMPA (GIT and BBB options)
Caco-2 assay
Cytotoxicity studies (HepG2 or other cells)

We are constantly expanding the list of the analytical services offered. In addition, our bioanalytical group can rapidly modify or develop bioanalytical methods according to customer specifications. Pharmacokinetic and toxicity studies in small animals can also be provided. Our bioanalytical laboratory has national regulatory certification for providing bioanalytical support of clinical bioavailability and bioequivalence studies.

The main purpose of the Screening Group is to provide hit identification and hit-to-lead optimization contract services to the biotech and pharmaceutical industry. We are also open to discuss shared-risk exploratory hit finding projects with the industry or academic partners, including the discovery and optimization of various assays and pharmacological tool compounds for new or poorly validated targets.
The HTS Laboratory is a well-equipped screening facility with a broad range of robotic liquid handling and signal readout technology capabilities and the capacity to run both biochemical and cell-based assays in 384-well plate format.

Assay read-out platforms:

• UV-VIS absorbance
  
• Luminescence
  
• Fluorescence intensity
  
• Fluorescence polarization
  
• Time-resolved fluorescence/energy transfer (FRET, TR-FRET, HTRF, DELFIA, LANCE)
  
• Cellular calcium mobilization (FLIPR)
  
• ELISA
  
• AlphaScreen
  
• Enzyme/reporter assays
  
• Cell viability assays
  

Our Protein Thermal Shift Screening Platform (or Differential Scanning Fluorimetry) includes a ViiA 7 System (Applied Biosystems) and two FluoDia T70 (Photal) readers.

The main purpose of the Screening Group is to provide hit identification and hit-to-lead optimization contract services to the biotech and pharmaceutical industry. We are also open to discuss shared-risk exploratory hit finding projects with the industry or academic partners, including the discovery and optimization of various assays and pharmacological tool compounds for new or poorly validated targets.
The HTS Laboratory is a well-equipped screening facility with a broad range of robotic liquid handling and signal readout technology capabilities and the capacity to run both biochemical and cell-based assays in 384-well plate format.

Assay read-out platforms:

• UV-VIS absorbance
  
• Luminescence
  
• Fluorescence intensity
  
• Fluorescence polarization
  
• Time-resolved fluorescence/energy transfer (FRET, TR-FRET, HTRF, DELFIA, LANCE)
  
• Cellular calcium mobilization (FLIPR)
  
• ELISA
  
• AlphaScreen
  
• Enzyme/reporter assays
  
• Cell viability assays
  

Ligand-Based Approach Targeted Libraries (LBA)
Receptor-Based Approach Targeted Libraries (RBA)
Hit Diversified Targeted Libraries (HD)

Cell based HTS assays
Biochemical HTS assays