2. Academic Validation
  3. The Identification of GPR52 Agonist HTL0041178, a Potential Therapy for Schizophrenia and Related Psychiatric Disorders

The Identification of GPR52 Agonist HTL0041178, a Potential Therapy for Schizophrenia and Related Psychiatric Disorders

  • ACS Med Chem Lett. 2023 Mar 14;14(4):499-505. doi: 10.1021/acsmedchemlett.3c00052.
Simon Poulter 1,  Nigel Austin 1,  Rachel Armstrong 1,  Matt Barnes 1,  Sarah Joanne Bucknell 1,  Alicia Higueruelo 1,  Joydeep Banerjee 2,  Andy Mead 1,  Richard Mould 1,  Cliona MacSweeney 1,  M Alistair O'Brien 1,  Lisa Alice Stott 1,  Stephen P Watson 1 2
Affiliations

Affiliations

  • 1 Sosei Heptares, Steinmetz Building, Granta Park, Great Abington, Cambridge CB21 6DG, United Kingdom.
  • 2 Syngene International, Biocon Park, Bommasandra, Bangalore 560099, India.
PMID: 37077397 DOI: 10.1021/acsmedchemlett.3c00052
Abstract

HTL0041178 (1), a potent GPR52 agonist with a promising pharmacokinetic profile and exhibiting oral activity in preclinical models, has been identified. This molecule was the outcome of a judicious molecular property-based optimization approach, focusing on balancing potency against metabolic stability, solubility, permeability, and P-gp efflux.

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