Scope of Collaboration:

This RFP seeks applications from institutions performing drug discovery and who are interested in screening compounds provided by AstraZeneca. The screening library will be provided free-of-charge to the selected proposals. AstraZeneca also offers the possibility of support of approximately $20k to $40k, which may come, in part, in the form of reagents and other material support.

Three specific libraries are available for collaboration. First is a 250,000 diversity set which provides a broad representation of AstraZeneca's industry-leading compound collection. Also available are a 14,000 annotated set covering 1200 human targets with at least 100 nM potency at the primary target and a low molecular weight fragment screening set of 17,000 compounds.

Institution that applies must meet the below criteria:

1. Each center must have high throughput screening (HTS) & medicinal chemistry development capabilities, specifically the capacity to test a 250K diversity set of compounds (or a 14k annotated set) provided by AstraZeneca and have the capability to perform hit-to-lead.
2. Each center's institution must sign an option agreement, which provides AstraZeneca the right to license compounds and data generated from the collaboration.
3. Interested centers would submit a target proposal to the steering committee for review. Target proposal should overlap with therapeutic areas of interest to AstraZeneca

Overview of the operations:

1. AstraZeneca will provide ready to screen plates (up to 250,000 compounds) directly to the center in a structure-blinded fashion. The compounds will broadly represent AstraZeneca's larger compound collection.
2. Institution will provide screening data to AstraZeneca who will identify the series/ clusters that have the potential to be developed. AstraZeneca will share with the center an agreed number of up to 50 chemical structures. Follow up plates may also be provided, including 'near neighbor' compounds, to establish active compound clusters.
3. For projects advanced to lead identification stage within the center, using these structures, first rights of negotiation would be offered to AstraZeneca.

Certain target proposals may be excluded if there are pre-existing contractual obligations or areas where AstraZeneca already has existing programs within the company.

Format of the Proposal:

Centers who want to take part in this screening collaboration should submit a five (5) page proposal covering the below areas.

1. Target background and rationale

2. Target validation (pharmacological and/or genetic)

3. Potential clinical utility

4. Currently available tool compound for the target

5. Funding for screen and hit follow-up

6. Competitive landscape

7. High Throughput Screening Readiness

i. HTS assay description

ii. Characterization

iii. Pilot screening data, if available

8. Plans for Hit confirmation/validation once hits are obtained

9. Drug discovery screening flow chart

10. Facilities description:

i. Ability to conduct HTS

ii. Ability to conduct Structure Activity Relationship (SAR) studies on the screening hits NIH Type Biosketch of Investigators

Review and Submission Process:

The dates will be announced for each round. A Steering committee comprising of ADDC members and Astra Zeneca will prioritize and review the proposals. Please email Matthew Hartman to request a copy of Appendix A: IP Guidelines.

For further information contact:

Matthew Hartman

Academic Drug Discovery Consortium

Email: mhartman@addconsortium.org