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Comprehensive GPCR Assay Solutions for Drug Discovery

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GPCR Screening with Confidence Comprehensive GPCR Assay Solutions for Drug Discovery Why go anywhere else? Why go anywhere else? We cover the entire range of GPCR assay possibilities. Shop at the GPCR Super Store. From PerkinElmer — your one stop solution provider. PerkinElmer — a Source of Confidence for Your GPCR Research and Discovery G-Protein Coupled Receptors (GPCRs) continue to be significant therapeutic Contents targets, and thus GPCR assays and screening campaigns remain major •Assay Platforms for GPCR Binding Assays ...........2 components of drug discovery research • NEN Radioligands for GPCR Binding Assays .......4 programs worldwide. The need for • Cloned Receptors for GPCR Binding Assays.........4 reliable, proven, and versatile assay • Adenylyl Cyclase Activation/Inhibition and technologies and reagents is a key cAMP Quantitation ................................................5 component for successful and productive •Detection Instrumentation to Measure research. That’s why PerkinElmer GPCR Assays ........................................................11 has assembled the world’s most •Ordering Information: comprehensive product offering for DELFIA Ligands and Reagents.............................16 GPCR research and drug discovery, covering the entire range of GPCR GPCR-Specific NEN Radioligands.......................17 assay possibilities. SignalScreen® Cloned Receptors .........................18 Membrane Target Systems Cloned Receptors .....23 Our products and expertise span receptor ligand FlashBlue™ Scintillating Beads and binding assays through functional cellular assays. FlashPlate Microplates.........................................27 Our range of assay platforms and detection technologies Adenylyl Cyclase Assay Systems for includes essential radioisotopic technologies and state- Cell-Based Functional cAMP Measurement.........28 of-the-art luminescence and fluorescence alternatives. cAMP Assay Systems for cAMP Quantitation These are supported by a comprehensive range of in Plasma, Urine and Cell Culture Samples .........28 reagents including NEN® Radioligands, DELFIA® GTP Binding Assay Systems................................28 ligands and cloned receptor membranes, assay systems IP Functional Assay System ...............................29 using our AlphaScreen™, LANCE™, DELFIA, FlashPlate® 3 2 Reporter Gene Luminescence Assay Systems ......29 and [FP]™ technologies, plus versatile, scalable detec- tion instrumentation. Combined with our demonstrated Microplates for Filtration Assays and dedication to new product introductions— ligands, Cell-Based Assays ................................................29 receptors, functional assays, and technologies— you can be confident we’ll always be there to support this essential research area. You won’t find this commitment to GPCR research anywhere else. With PerkinElmer behind your GPCR assays, you can screen with confidence, today and in the future. Why go anywhere else? www.perkinelmer.com 1 Your Choice of Assay Platforms for GPCR Binding Assays PerkinElmer supports the widest range of assay tech- And, we’re the first to offer a viable and robust alterna- niques for GPCR binding assays. Our scintillation tive to radioisotopic assays, using our DELFIA technology, proximity assay platforms include FlashBlue™ beads a heterogeneous time resolved fluorescence assay and FlashPlate and Image FlashPlate microplates. platform. All of these options can now supplement These are all compatible with our extensive line of traditional filtration assays to increase the performance NEN Radioligands and SignalScreen® and Membrane and productivity of your GPCR assays. Target Systems (MTS) cloned receptor preparations. PerkinElmer Assay Platforms for Receptor Ligand Binding Assays Selection Criteria DELFIA FlashBlue FlashPlate Image Filtration Technology Beads Microplates FlashPlate Assays Microplates Homogeneous No Yes Yes Yes No Non-Rad Yes No No No No Format 96- and 384- 96- and 384- 96- and 384- 384-shallow 96-well plates well plates well plates well plates well plates Throughput >40,000 >20,000 >20,000 >50,000 >15,000 (wells in an 8-hour day) Recommended DELFIA Clear Bottom or N/A N/A UniFilter® Microplate Type AcroWell™ White OptiPlate Filter Plates Filter Plates Microplates Stability of Signal >24 hours >24 hours >24 hours >24 hours >24 hours DELFIA® TRF Technology Our DELFIA technology is a robust, time-resolved, Systems (MTS) cloned receptors. For easy assay setup, fluorometric assay (TRF) technology based on dissociative use DELFIA L*R Wash Solution and DELFIA L*R fluorescence enhancement using lanthanide chelates. Binding Buffer. After incubation unbound ligand is Invented by and available exclusively from PerkinElmer, removed by filtration, then signal is enhanced using it’s been widely adopted for many HTS applications DELFIA Enhancement Solution. It’s simple and reliable. due to its extremely high sensitivity and wide dynamic range. Receptor binding assays using DELFIA technology have been proven to be a robust non-radioactive alterna- tive to traditional receptor-radioligand binding assays. Europium-labeled ligands are stable reagents for DELFIA receptor-ligand binding assays. The binding assay may be done in an AcroWell FilterPlate using PerkinElmer’s SignalScreen or Membrane Target 2 FlashBlue™ GPCR Scintillating Beads Our FlashBlue GPCR beads are scintillating beads binding assays, radioligand molecules bound to the specifically designed and proven for high throughput membranes’ receptors activate the scintillating beads homogeneous GPCR-radioligand binding assays. Three and trigger a blue light emission. Assays can be read microns in diameter, they consist of a polystyrene core on PerkinElmer’s TopCount® and MicroBeta® Liquid covered by a hydrophilic coating that minimizes non- Scintillation and Luminescence Counters in 96- and specific binding. Wheat germ agglutinin (WGA) is 384-well formats, as well as our TriCarb LSC for covalently attached to the surface of FlashBlue GPCR tube-based assays. beads for the capture of cellular membranes. In GPCR FlashPlate® and Image FlashPlate® Microplates FlashPlate Microplates 125 3 35 33 14 Our popular FlashPlate microplates are designed for of a variety of isotopes (e.g., I, H, S, P and C) high-volume, homogeneous radioligand binding assays, without the addition of liquid scintillation cocktail. based on the principle of scintillation proximity. The FlashPlate microplates can be read on TopCount or interior of each well is permanently coated with a MicroBeta counters. thin layer of plastic scintillant, enabling detection Image FlashPlate Microplates Our 384-well Image FlashPlate microplate is coated The FlashPlate platform is especially suitable for with a special scintillant that emits in the red region of receptor binding assays using highly purified membrane the spectrum. This characteristic allows detection with preparations and/or receptor preparations known imaging readers, such as the PerkinElmer ViewLux™ to contain moderate to higher concentrations of ultraHTS Microplate Imager, enabling very high testing receptor protein. Use of FlashPlate pre-coated with throughput. Image FlashPlate also eliminates or greatly wheat germ agglutinin allows greater flexibility in reduces interference from colored compounds. These receptor choice and optimal ease-of-use. plates have shallower wells to permit lower volume assays and, therefore, use less reagent, which is ideal for further miniaturization. ScreenReady Targets™ ScreenReady Targets™ provide optimum performance of recombinant GPCR membranes pre-coated onto with FlashPlate microplates. They’re ready-to-use, fully FlashPlate microplates, the appropriate radioligand, 125 validated GPCR receptor binding assays that employ I and a validated assay protocol. For more information, 3 and H radioligands. This easy-to-use platform consists please contact [email protected]. www.perkinelmer.com 3 NEN Radioligands Keep Pace with Drug Discovery From the company that pioneered development work with you, scientist to scientist, to prepare a of the essential tools for receptor ligand binding, custom radioligand that meets your specifications. 3 125 PerkinElmer now offers over 400 NEN H and I A confidentiality agreement is available if required. ligands. A continuous pipeline of new product We are committed to your success. introductions ensures we’ll always keep pace with Please refer to the tables on pages 17–18 for a listing of discoveries and trends in receptor research and our available GPCR membranes with their compatible drug discovery. Each of our ultrapure radioligands NEN Radioligands. PerkinElmer also offers a number is fully characterized for pharmacological action of radioligands, some exclusive, specific for GPCRs and validated in a receptor binding assay. that are not found in the aforementioned tables. For If you don’t find exactly what you need, we invite our complete radioligand offering, please visit our you to take advantage of our custom services. We’ll website at www.perkinelmer.com/nenradioligands. World’s Most Comprehensive Line of Cloned Receptors for GPCR Binding Assays PerkinElmer offers more than 170 cloned receptor They provide excellent targets for GPCR assays using membrane preparations, with a constant flow of new the technique of your choice, including: receptors as they are identified. Our line includes • Receptor radioligand binding assays with FlashPlate over 150 GPCRs as well as several tyrosine kinase, microplates, FlashBlue beads,
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