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Due to their often central roles in diseases and their favorable drugability profiles, GPCRs are considered prime candidates for drug discovery efforts. However, GPCRs may also trigger unwanted drug safety events. Hence, there is a need to improve their therapeutic index as early as possible in discovery. With the opnMe GPCR Route 66+ project, scientists from the High Throughput Biology department at Boehringer Ingelheim plan to set up a fast and resource-effective methodology to detect unselective GPCR binding to ease and streamline the selection of safe candidates. The goal is to set up a GPCR selectivity binding assay panel that should enable large-scale profiling of the binding affinities and kinetics of test compounds for a variety of receptors. To facilitate the process, sixty-six suitable GPCR constructs have been prepared that are ready for human cell culture expression. To fulfill the mission of providing the scientific community with a high-quality, broad GPCR selectivity panel, we now ask for your contribution in obtaining suitable fluorescent probes, also known as tracers, which are currently limited. All incoming tracer(s) will be extensively profiled, and results will be made available with submitting scientists. In addition, the best tracer(s) will be included in the final opnMe GPCR 66+ assay panel. All results will be made available as part of an open access publication.

As participant to this opn2EXPERTS call, you will have the chance to outline and share your expertise, skill set, and prior successes in the field with a top 20 pharmaceutical company. As part of the 1^st phase of this opnMe call, you will receive 200 euros as a reimbursement of your shipping costs for the fluorescent tracer(s) delivery for a maximum of one delivery. We kindly ask you to refrain from sending individual shipments for individual tracers; rather we encourage you to combine the shipment. The subsequent assay development including the other reagents needed will be covered by us. You will receive all data that Boehringer Ingelheim will generate, and the potential prospect for a publication on this assay development. Overall, it opens the opportunity to work on a scientific topic in the field of GPCR research and accelerate the drug development of potential compounds targeting essential GPCRs. All submitted IP will continue to stay with you and you are free to use it for other purposes.

Should your tracer(s) become selected as part of the final GPCR panel, you will receive a 2,000 euros award per accepted and validated fluorescent probe that will serve as a non-exclusive license fee. Also, you will receive a detailed protocol describing the assay conditions including detailed validation data. You may have the opportunity to receive the plasmid-DNA to set up the assay in your own laboratory. In addition, we offer you the possibility to co-author a broader scope scientific publication describing our overall efforts to improve early drug safety screening in a high impact factor journal upon conclusion of this call. To be eligible for co-authorship you should be willing to disclose your tracer structure in the publication.

Furthermore, you will have the opportunity to nominate a maximum of five compound tools for validation studies and gain pre-publication access to the data of the broader GPCR panel generated. Your contribution will be valued in the community and offers you the possibility of high visibility as well as a network opportunity and link with likeminded scientists.

As part of our opnMe GPCR Route 66+ call we invite all experts in the GPCR field who may have access to defined tracer(s) matching any of the sixty-six GPCRs included in our call. We offer reimbursement for shipped tracer(s) and a monetary award of 2,000 euros per selected tracer for winning scientists. In contrast to our other opn2EXPERTS calls which are aiming at a longer-term collaboration period, the interaction between the participating scientists and the researchers from our High Throughput Biology department is more ad-hoc. Hence, we do not offer any additional research funding as part of this call.

To all scientists who have been selected as winners of the opnMe GPCR Route 66+ call we offer the possibility to co-author a planned open access publication that will summarize the efforts of this project. To be eligible for co-authorship you should be willing to disclose your tracer structure in the publication as the structural information might be required by the selected high-profile journal.

This call is structured into two main phases. As part of the first phase which runs from June 11 until September 27, 2023, we kindly ask for tracer submissions from participating GPCR experts. The duration of this first phase has been adopted for the summer period already when many scientists may be difficult to reach.

During the following six months from September 28, 2023, until March 29, 2024, an in-depth characterization of the submitted tracers is planned on our end. As we expect many submissions, we want to reserve sufficient time on our end to do our job well.

The second phase of this opnMe call begins with contacting of the winning scientists starting on April 1, 2024. Subsequently, we will generate GPCR selectivity profiling data on selected GPCR drugs. During this time, winners of the phase 1 can submit small molecule test candidates for consideration for GPCR profiling. They will also get pre-publication access to the GPCR dataset. The remainder of 2024 and 2025 is reserved for the planned publication and further follow-ups with the winning scientists. We aim to close this call on December 31, 2025.

The key success criteria for this opn2EXPERTS call are determined by the elements of the scoping chapters of our call that define the criteria for tracer selection and define which solutions will be considered out of scope. Please check our profile for more details.

Hence, providing as much information as possible as part of your submission will increase the chances of success.

With your submission, you provide us with the right to carry out defined analyses with your submitted tracer(s). Hence, formally it serves as a material transfer agreement that defines and secures your intellectual property (IP) contribution that ONLY provides Boehringer Ingelheim with the license to develop and perform an assay based on your shared fluorescent probe (tracer). The IP remains with you otherwise and you are free to use the tracer(s) for other purposes. Therefore, it is important that you do not disclose any tracer structures or SMILES codes with your submission.

We would like to ensure that all intellectual property (IP) of your tracer(s) stay with you. Hence, initially we will only request non-confidential information as part of your submission and most importantly, no structural information. For those tracers that will not become selected, we will delete all remaining materials and data after we have shared it with the submitting scientists. Should you be selected as a winner for Phase 2 of this call, from April 2024 until March 2025 you will have the possibility to file intellectual property rights for any tracer(s) that have been selected as part of the call. Boehringer Ingelheim will seek to obtain a non-exclusive license fee from you to carry out further analyses and to set up the final GPCR panel. Please note that a planned publication that aims to summarize all efforts may result in the need to release the structure of our tracer(s) into the public domain as a journal requirement.

As part of this call, we kindly ask you to refrain from sharing any confidential data, in particular structures or similar information.

If confidential data exists that would strengthen the proposal, please indicate that information is available to share under a Confidential Disclosure Agreement (CDA). If we find the non-confidential concept proposal sufficiently interesting, we will execute a CDA for confidential discussions.

In this opn2EXPERTS call we aim to study the selectivity of the initial sixty-six GPCRs selected because plasmids are available. We are interested in increasing the panel and would like to get in contact with you for future projects. Please send us your idea without including any confidential information or tracer structures.

For initial validation studies an amount of 1 mg would be desired. If you, however, only can provide less material please include that information in your submission document.

In the current opn2EXPERTS call we aim to receive ready-to-use tracers or biotinylated adducts. If you have a precurser molecule that is ready to be coupled, we encourage you to send it to us including the information which reactive group would be available to be coupled on your molecule. Please make sure a simple coupling reaction would result in only a single product as we discourage a mixture of differently linked tracers.  Please also indicate in your submission document that this is a precurser to be coupled and do NOT include any structures of your tracers/precursers.

From September 28, 2023, until March 29, 2024, an in-depth characterization of all submitted tracers is planned on our end. As we expect many submissions, we want to reserve sufficient time on our end to do our job well. Hence, we reserved an extra-long review period during which we will carry out many planned experiments to further characterize your tracers, such as assessing tracer selectivity among the sixty-six GPCRs of interest, determining binding K_D,app where feasible, investigating tracer unspecific cytotoxicity and studying your tracers binding kinetic properties. Based on these criteria we select the best molecules to cover the GPCRs of interest and contact the winners on April 1, 2024.

We enable submitting scientists to propose up to five candidates for full profiling in the final GPCR panel. We do not plan any commercialization efforts.

No. All submissions will only be shared inside Boehringer Ingelheim amongst a team of scientists designated to evaluate all submitted tracers for eligibility for Phase 2. They will not be visible to, or shared with, scientists from other institutions.

Please register via our opnMe GPCR Route 66+ newsletter to stay up to date with the progress of our project. You should not expect more than maybe a newsletter every 4 to 6 months. During the newsletter registration process, you will also have the opportunity to agree to be contacted individually by our research team in case of interest.