Discovery of GLPG1972/S201086, a Potent, Selective, and Orally Bioavailable ADAMTS-5 Inhibitor for the Treatment of Osteoarthritis

F. Brebion; Romain Gosmini; Pierre Deprez; Marie Varin; Christophe Peixoto; Luke J. Alvey; Hélène Jary; Natacha Bienvenu; Nicolas Triballeau; Roland Blanqué; C. Cottereaux; Thierry Christophe; Nele Vandervoort; Patrick Mollat; Robert Touitou; Philip M. Leonard; Frédéric De Ceuninck; Iuliana Botez; Alain Monjardet; Ellen van der Aar; David Amantini

doi:10.1021/acs.jmedchem.0c02008

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Abstract

< 1.5 μM). The cocrystal structure of GLPG1972/S201086 with human recombinant ADAMTS-5 is discussed. GLPG1972/S201086 has been investigated in a phase 2 clinical study in patients with knee OA (NCT03595618).

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Brebion et al. (2021) studied this question.

synapsesocial.com/papers/69fd17757467cb4cde270341 https://doi.org/10.1021/acs.jmedchem.0c02008

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Discovery of GLPG1972/S201086, a Potent, Selective, and Orally Bioavailable ADAMTS-5 Inhibitor for the Treatment of Osteoarthritis

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Abstract

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Discovery of GLPG1972/S201086, a Potent, Selective, and Orally Bioavailable ADAMTS-5 Inhibitor for the Treatment of Osteoarthritis

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Abstract

Discussion

Cite This Study

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