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Trial completion: Phase 1, Healthy Subject, Safety, Tolerability and Pharmacokinetic Study of mGlu5 NAM HTL0014242 (clinicaltrials.gov) - Apr 29, 2021 P1, N=71, Completed, Our data indicate for the first time that a consistent, unified relationship can be observed between exposure and mGlu receptor occupancy when unbound brain concentration and receptor affinity are taken into account across a range of species for a diverse set of mGlu NAMs, including a new drug candidate, HTL0014242. Recruiting --> Completed
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Journal: Structure-based discovery and development of metabotropic glutamate receptor 5 negative allosteric modulators. (Pubmed Central) - Oct 1, 2020 An alternative approach to drug discovery is to use structural knowledge to enable structure-based drug design (SBDD), which allows the design of molecules in a more rational, rather than empirical, fashion. Here we will describe the process of SBDD in the discovery of the mGlu negative allosteric modulator HTL0014242 and describe how knowledge of receptor structure can also be used to gain insights into the receptor activation mechanisms.
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Enrollment change, Trial completion date, Trial primary completion date: Phase 1, Healthy Subject, Safety, Tolerability and Pharmacokinetic Study of mGlu5 NAM HTL0014242 (clinicaltrials.gov) - Nov 9, 2019 P1, N=78, Recruiting, Here we will describe the process of SBDD in the discovery of the mGlu negative allosteric modulator HTL0014242 and describe how knowledge of receptor structure can also be used to gain insights into the receptor activation mechanisms. N=48 --> 78 | Trial completion date: Aug 2019 --> May 2020 | Trial primary completion date: Jul 2019 --> Apr 2020
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