Non-confidential. Please email a copy of your completed application to targets@tech.mrc.ac.uk MRCT LIBRARY REQUEST FORM Our aim at the Centre for Therapeutics Discovery: To progress innovative therapeutic targets emerging from groundbreaking basic research through identification of tool compounds to validate their involvement in disease processes. Project Name: Target Name: Type of Target (e.g. kinase, protein:protein interaction etc): Primary Indication: Principle Investigator: Organisation: Address: Postcode: Telephone: Fax: Email: If you are an MRC employee please tick If you receive MRC grant funding please tick To help CTD assess the most appropriate library for you to screen please complete the following details. Consideration will be given to Target class Screening capacity in your lab Structural information/ known ligands Library Request Form 1 of 4 Version date 04Sep2012 Non-confidential. Please email a copy of your completed application to targets@tech.mrc.ac.uk Target rationale and background information Please give details of the molecule or mechanism being targeted and rationale for screening 300 words What disease is this molecule/mechanism implicated in and what is the evidence for disease association? 200 words What is the biological rationale that modulation of this target/ mechanism will achieve the predicted effects? 200 words Library Request Form 2 of 4 Version date 04Sep2012 Non-confidential. Please email a copy of your completed application to targets@tech.mrc.ac.uk Screen Proposal Target Type (please tick as appropriate) KINASE GPCR ENZYME RECEPTOR ION CHANNEL PROTEIN: PROTEIN INTERACTION TRANSCRIPTION FACTOR UNKNOWN/PHENOTYPIC OTHER (please supply details) Please give details of any known ligands or any structural information for the target. 100 words Assay Principle: Please give details of assay design, any kits used. 100 words Read Out (please tick as appropriate) Fluorescence Luminescence Absorbance Fluorescence Polarisation Time resolved fluorescence Imaging Label Free (please supply details) CTD can supply libraries in 96 and 384 formats. 20uL 1mM stock in 100% DMSO is provided for screening and counter screen single point hit confirmation. It is important that a robust screening strategy is in place to identify true hits. Assay Stats: (If the assay has not yet been developed, these can be supplied later, prior to any library supply). Average Standard deviation High Control Background Signal: background Z’* * For single point screening Z’>0.5 is expected. Zhang et al 1999 (J. Biomol screen. 4, 67-73) Z’ calculated as (1-((3*SD-Hi CTRL+3*SD-LoCTRL)/(Ave-Hi CTRL– Ave-Lo CTRL)) Library Request Form 3 of 4 Version date 04Sep2012 Non-confidential. Please email a copy of your completed application to targets@tech.mrc.ac.uk What is the screening capacity of your laboratory? (include details of any screens which have been conducted against this target already) 200 words Plate format required: 96 384 Other What Counter screens are planned for identifying false positives? 100 words For our proprietary compound libraries a further 20ul 10mM stock of confirmed hits is available for confirmation in dose response assay. Structures will be revealed after receipt of IC50s. What secondary assays/ orthologous assays do you have planned to validate your hits. 300 words Please email a copy of your completed application to targets@tech.mrc.ac.uk, fax to 020 7391 2800 or alternatively, please post to: Phil Coxon, Target Submissions, MRC Technology, Lynton House, 7-12 Tavistock Square, London WC1H 9LT. If you have any queries please call: +44(0)20 7391 2826 Library Request Form 4 of 4 Version date 04Sep2012