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Drug Discovery Core

The Drug Discovery Core at the University of Utah is an established Service/Recharge center that provides compound collections for screening by University of Utah Faculty. Our mission is to provide customers low-cost and efficient access to chemical libraries for screening, to equipment for automation, and to synthetic chemistry support for the characterization and validation of compounds for potential use as therapeutics, diagnostics and biological tools.

  • Services
  • High-throughput screening
  • Small molecule chemical libraries
  • Pooled CRISPR-Cas9 libraries/Screening
  • Assay development
  • Consultation on target identification/validation, hit to lead optimization, PK/PD/Efficacy
  • Chemical support for drug discovery

CRISPR Knockout/Knockin Cell Line Production – In collaboration with the Mutation Generation and Detection Core, we started to offer a full cell line generation service from sgRNA design/construction to final cell line generation/verification. 

  • Viral Packaging Service
  • Small/large scale viral (lentivirus, adeno-associated virus) packaging, titrations, concentrations and transductions of cells of interest.
  • Lentivirus delivery of Cas9 and sgRNA

Commercial Compound Libraries Available for Screening

  • Chembridge DIVERSetTM100K Libraries: We offer two, complementary DIVERSet™ libraries: The DIVERSet™-EXP library and the DIVERSet™-CL library. Each library offers a diverse set of 50,000 compounds with extensive pharmacophore coverage for primary screening. Stringent druglike and desirable chemical group filters coupled with a 3D conformer analysis are used in selecting a premium set of 50,000 druglike compounds with maximum pharmacophore coverage and chemical diversity.
  • Microsource Spectrum Collection: 2000 compounds with varied of biological activity and structural diversity, including 1000 known drugs from United States, Europe, and Japan. (Spectrum Collection)
  • NIH Clinical Collection: 446 compounds that have been in phase I-III clinical trials and have not been represented in other arrayed collection.
  • Epigenetics Screening Library: 75 small molecules that are known to modulate the activity of a variety of epigenetic ‘writers and erasers’ and ‘reader’ proteins.
  • NCI Diversity Set IV: 1596 compounds with diverse pharmacophores which were derived from the almost 140,000 compounds available for distribution from the Developmental Therapeutics Program (DTP) repository at NCI/NIH.
  • Natural Products Set II: 120 natural product compounds from Developmental Therapeutics Program (DTP) repository at NCI/NIH.
  • Enamine 3D Diversity Set: 50240 compounds were selected from the drug-like portion of Enamine HTS collection (1.3 million compounds) by application of conformational analysis and shape clustering algorithms.
  • Protein Kinase Inhibitor Library: 160 well-characterized, cell-permeable, potent, and reversible protein kinase inhibitors; the majority of which are ATP-competitive.
  • Approved Oncology Drugs Set II: The current set (AODVII) consists of 129 agents and is intended to enable cancer research, drug discovery and combination drug studies.
  • Natural Products Set IV: The Natural Products Set IV consists of 419 compounds that were selected from the DTP Open Repository collection of 140,000 compounds.
  • Mechanistic Set III: The Mechanistic Set III, which consists of 813 compounds, was derived from the 37,836 open compounds that have been tested in the NCI human tumor 60 cell line screen. This mechanistic diversity set was chosen to represent a broad range of growth inhibition patterns in the 60 cell line screen, based on the GI50 activity of the compounds. Details of these three libraries can be found here: Available Plates 
  • University of Utah metabolite library v1.0:The University of Utah metabolite library v1.0 is composed of 453 endogenous and exogenous, primary and secondary metabolites nucleotides, cofactors, signaling molecules, and various precursors, intermediates, and byproducts thereof. All compounds are at 10 mM and solvated in DNase, RNase, Protease, free deionized.

Private Chemical Collections*

  • UUPCC –University of Utah Private Chemical Collection: A library of 120,000 compounds obtained from the former NPS Pharmaceutical Company. Many compounds in this library are unique and not commercially available, creating a valuable resource for the University. Due to the unique nature of this library, access will require a written proposal.
  • Dept of Chemistry Library: A diverse collection (800 compounds) of molecular skeletons that represent the chemical interests of individual principal investigators. These compounds are all prepared by chemical synthesis within their laboratories and generally reflect natural product substructures or analogues of proven pharmacophores.
  • Ireland Natural Product Collection: A set of natural products (240 compounds) isolated from marine invertebrate animals and micro-organisms. The collection reflects a wide array of natural product scaffolds and biosynthetic pathways. All compounds have been purified by HPLC and chemically characterized.

*These sets of molecules are proprietary and users will be asked to sign an intellectual property advisory notice

Service Rates

Requesting Services

If you are new to the Cores, you must complete a work authorization form through the Work Authorization System prior to requesting services. Work authorizations may be used for any services offered by facilities managed by HSC Cores. After your work authorization has been approved you will be able to login to the Resource System.

Existing users may login directly to the Resource Scheduling System to schedule or order services. This system is cores-wide and uses University of Utah uNID authentication.

Work Authorization
System On Campus / UU
Work Authorization
System Off Campus / Business
Resource Scheduling
System

If you encounter financial/account issues, contact the Cores Admin office.
For technical issues with any of the web applications, contact the developers.

Charge Rates Procedure /
Federal Facilities and Administration (F&A) Rate

Part of the University’s agreement with the Federal Government regarding F&A is that the University will not offer a lower than F&A rate to other kinds of sponsors. That means that the University has to use, at minimum, the same rates for commercial sponsors as it does for the Federal Government. The University would jeopardize its relationship with the Federal Government (the University’s single largest sponsor) if it were to accept rates lower than the current federal F&A rate.

The current F&A Rate is: 54%

The facility internal rate is used when exclusively internal funding sources are used. The F&A / external academic rate applies when external funding sources are used i.e. Federal Government or other academic universities. For more information about F&A rates at the University of Utah please see: 6.3 Indirect Costs/Facilities and Administrative Costs (F&A)

Bai Liu

Facility Director

Contact

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Hours of Operation

9:00 am to 5:00 pm
Monday - Friday

Recent Mentions

  1. Hicks, K. G., A. A. Cluntun, H. L. Schubert, S. R. Hackett, J. A. Berg, P. G. Leonard, M. A. Ajalla Aleixo, Y. Zhou, A. J. Bott, S. R. Salvatore, F. Chang, A. Blevins, P. Barta, S. Tilley, A. Leifer, A. Guzman, A. Arok, S. Fogarty, J. M. Winter, H. C. Ahn, K. N. Allen, S. Block, I. A. Cardoso, J. Ding, I. Dreveny, W. C. Gasper, Q. Ho, A. Matsuura, M. J. Palladino, S. Prajapati, P. Sun, K. Tittmann, D. R. Tolan, J. Unterlass, A. P.VanDemark, M. G. Vander Heiden, B. A. Webb, C. H. Yun, P. Zhao, B. Wang, F. J. Schopfer, C. P. Hill, M. C. Nonato, F. L. Muller, J. E. Cox and J. Rutter (2023). Protein-metabolite interactomics of carbohydrate metabolism reveal regulation of lactate dehydrogenase. Science 379(6636): 996-1003.10.1126/science.abm3452
  2. McCullough, B. S., H. Wang and A. M. Barrios (2022). Inhibitor Screen Identifies Covalent Inhibitors of the Protein Histidine Phosphatase PHPT1. ACS Med Chem Lett 13(7): 1198- 1201.10.1021/acsmedchemlett.2c00053

Citing Our Facility

Acknowledgments

We would like to thank you for acknowledging the our facility. This recognition allows us to highlight the impact of your work and demonstrates the important contributions of our facility makes to research across the University of Utah. The recognition our core receives from your acknowledgments also aids in receiving grants and further funding for equipment and services we can provide to our users.

Self-Run Services / Instrumentation Usage:

In published papers that used instruments at our facility and notably involved staff members please use the following format:

We acknowledge (facility name) at the University of Utah for use of equipment (insert instrument/service details here), and thank (insert any notable staff member – if desired) for their assistance.

Assisted Services:

In published papers where a staff member assisted you in addition to the requested services please use the following format:

We acknowledge (facility name) at the University of Utah for use of equipment (insert instrument/service details here), and thank (insert staff member-required) for their assistance in (service provided).

Collaboration:

For publications resulting from collaborations that assisted with the methodologies, planning process and execution of your experiment in addition to equipment usage we require Co-author attribution on your publication for our facility and any staff members who provided substantial contributions to the originating project.