Stage of project Please indicate which stage in drug discovery /development is applicable to your project LO (Lead optimisation) Clinical Phase 1 Prenomination / CD (clinical drug Clinical Phase 2 candidate) selection Other Briefly describe: Target Biology Knowledge about the target Unknown target Novel target (no known function) Novel target Other Known drug target / family What evidence do you have that the target is relevant to human disease Hypothetical studies In vitro Genetic or proteomic data from human animal models In vivo Expression studies in human Exploratory clinical studies Registry clinical studies Other What is the actual/proposed mechanism of action (MoA) on the target Agonist Reversible Antagonist Irreversible Modulator Other, describe Allosteric Comment on Target Biology: Preclinical Package NB for small molecules only – Do you have biological assays in place for lead Yes No optimisation? Not applicable No assays model(s) In vivo Primary assay Other: Cellular assay Other: Selectivity assays What kind of pharmacological data has the project generated? in vitro Describe briefly Does the project have a chemical series with DMPK Yes No Not in vitro data suitable for the target? assessed What parameters have been determined? MDR1-MDCK permeability Microsomal stability Clint Log D7.4
Stage of project Please indicate which stage in drug discovery /development is applicable to your project LO (Lead optimisation) Prenomination / CD (clinical drug candidate) selection Clinical Phase 1 Clinical Phase 2 Other Briefly describe: Target Biology Knowledge about the target Unknown target Novel target Known drug target / family Novel target (no known function) Other What evidence do you have that the target is relevant to human disease Hypothetical Genetic or proteomic data from human Expression studies in human Registry clinical studies In vitro studies In vivo animal models Exploratory clinical studies Other What is the actual/proposed mechanism of action (MoA) on the target Agonist Antagonist Modulator Allosteric Reversible Irreversible Other, describe Comment on Target Biology: Preclinical Package – NB for small molecules only Do you have biological assays in place for lead optimisation? Yes No Not applicable No assays Primary assay Cellular assay Selectivity assays In vivo model(s) Other: Other: What kind of in vitro pharmacological data has the project generated? Describe briefly Does the project have a chemical series with in vitro DMPK data suitable for the target? Yes No Not assessed What parameters have been determined? Microsomal stability Clint MDR1-MDCK permeability Log D7.4