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First Structure-Activity-Relationship Study of Potent G2A Antagonists.

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Title: First Structure-Activity-Relationship Study of Potent G2A Antagonists.
Authors: Hernandez-Olmos V; Fraunhofer Institute for Translational Medicine and Pharmacology ITMP, Theodor-Stern-Kai 7, 60596 Frankfurt am Main, Germany.; Fraunhofer Cluster of Excellence Immune-Mediated Diseases CIMD, 60596 Frankfurt am Main, Germany., Heering J; Fraunhofer Institute for Translational Medicine and Pharmacology ITMP, Theodor-Stern-Kai 7, 60596 Frankfurt am Main, Germany.; Fraunhofer Cluster of Excellence Immune-Mediated Diseases CIMD, 60596 Frankfurt am Main, Germany., Lillich FF; Institute of Pharmaceutical Chemistry, Goethe University Frankfurt, Max-von-Laue-Str. 9, 60438 Frankfurt am Main, Germany., Marinescu B; Institute of Pharmaceutical Chemistry, Goethe University Frankfurt, Max-von-Laue-Str. 9, 60438 Frankfurt am Main, Germany., Nevermann S; Fraunhofer Institute for Translational Medicine and Pharmacology ITMP, Theodor-Stern-Kai 7, 60596 Frankfurt am Main, Germany.; Institute of Clinical Pharmacology, Pharmazentrum Frankfurt/ZAFES, Goethe-University, D-60590 Frankfurt am Main, Germany., Ehrler JHM; Institute of Pharmaceutical Chemistry, Goethe University Frankfurt, Max-von-Laue-Str. 9, 60438 Frankfurt am Main, Germany., Radchenko DS; Enamine Ltd. 78 Winston Churchill Street, Kyiv 02094, Ukraine., Moroz YS; Enamine Ltd. 78 Winston Churchill Street, Kyiv 02094, Ukraine.; Chemspace LLC, 85 Winston Churchill Street, Suite 1, Kyiv 02094, Ukraine.; National Taras Shevchenko University of Kyiv, 60 Volodymyrska Street, Kyiv 01601, Ukraine., Kaiser A; Institute of Pharmaceutical Chemistry, Goethe University Frankfurt, Max-von-Laue-Str. 9, 60438 Frankfurt am Main, Germany., Krämer A; Institute of Pharmaceutical Chemistry, Goethe University Frankfurt, Max-von-Laue-Str. 9, 60438 Frankfurt am Main, Germany., Knapp S; Institute of Pharmaceutical Chemistry, Goethe University Frankfurt, Max-von-Laue-Str. 9, 60438 Frankfurt am Main, Germany., Schubert-Zsilavecz M; Institute of Pharmaceutical Chemistry, Goethe University Frankfurt, Max-von-Laue-Str. 9, 60438 Frankfurt am Main, Germany., Alnouri MW; Department of Pharmacology, Max Planck Institute for Heart and Lung Research, 61231 Bad Nauheim, Germany., Offermanns S; Department of Pharmacology, Max Planck Institute for Heart and Lung Research, 61231 Bad Nauheim, Germany.; Center for Molecular Medicine, Goethe University Frankfurt, 60590 Frankfurt, Germany., Steinhilber D; Fraunhofer Institute for Translational Medicine and Pharmacology ITMP, Theodor-Stern-Kai 7, 60596 Frankfurt am Main, Germany.; Fraunhofer Cluster of Excellence Immune-Mediated Diseases CIMD, 60596 Frankfurt am Main, Germany.; Institute of Pharmaceutical Chemistry, Goethe University Frankfurt, Max-von-Laue-Str. 9, 60438 Frankfurt am Main, Germany., Sisignano M; Fraunhofer Institute for Translational Medicine and Pharmacology ITMP, Theodor-Stern-Kai 7, 60596 Frankfurt am Main, Germany.; Fraunhofer Cluster of Excellence Immune-Mediated Diseases CIMD, 60596 Frankfurt am Main, Germany.; Institute of Clinical Pharmacology, Pharmazentrum Frankfurt/ZAFES, Goethe-University, D-60590 Frankfurt am Main, Germany., Proschak E; Fraunhofer Institute for Translational Medicine and Pharmacology ITMP, Theodor-Stern-Kai 7, 60596 Frankfurt am Main, Germany.; Fraunhofer Cluster of Excellence Immune-Mediated Diseases CIMD, 60596 Frankfurt am Main, Germany.; Institute of Pharmaceutical Chemistry, Goethe University Frankfurt, Max-von-Laue-Str. 9, 60438 Frankfurt am Main, Germany.
Source: Journal of medicinal chemistry [J Med Chem] 2026 Jun 25; Vol. 69 (12), pp. 14309-14332. Date of Electronic Publication: 2026 Jun 11.
Publication Type: Journal Article
Journal Info: Publisher: American Chemical Society Country of Publication: United States NLM ID: 9716531 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1520-4804 (Electronic) Linking ISSN: 00222623 NLM ISO Abbreviation: J Med Chem Subsets: MEDLINE
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  Data: <searchLink fieldCode="AU" term="%22Hernandez-Olmos+V%22">Hernandez-Olmos V</searchLink>; Fraunhofer Institute for Translational Medicine and Pharmacology ITMP, Theodor-Stern-Kai 7, 60596 Frankfurt am Main, Germany.; Fraunhofer Cluster of Excellence Immune-Mediated Diseases CIMD, 60596 Frankfurt am Main, Germany.<br /><searchLink fieldCode="AU" term="%22Heering+J%22">Heering J</searchLink>; Fraunhofer Institute for Translational Medicine and Pharmacology ITMP, Theodor-Stern-Kai 7, 60596 Frankfurt am Main, Germany.; Fraunhofer Cluster of Excellence Immune-Mediated Diseases CIMD, 60596 Frankfurt am Main, Germany.<br /><searchLink fieldCode="AU" term="%22Lillich+FF%22">Lillich FF</searchLink>; Institute of Pharmaceutical Chemistry, Goethe University Frankfurt, Max-von-Laue-Str. 9, 60438 Frankfurt am Main, Germany.<br /><searchLink fieldCode="AU" term="%22Marinescu+B%22">Marinescu B</searchLink>; Institute of Pharmaceutical Chemistry, Goethe University Frankfurt, Max-von-Laue-Str. 9, 60438 Frankfurt am Main, Germany.<br /><searchLink fieldCode="AU" term="%22Nevermann+S%22">Nevermann S</searchLink>; Fraunhofer Institute for Translational Medicine and Pharmacology ITMP, Theodor-Stern-Kai 7, 60596 Frankfurt am Main, Germany.; Institute of Clinical Pharmacology, Pharmazentrum Frankfurt/ZAFES, Goethe-University, D-60590 Frankfurt am Main, Germany.<br /><searchLink fieldCode="AU" term="%22Ehrler+JHM%22">Ehrler JHM</searchLink>; Institute of Pharmaceutical Chemistry, Goethe University Frankfurt, Max-von-Laue-Str. 9, 60438 Frankfurt am Main, Germany.<br /><searchLink fieldCode="AU" term="%22Radchenko+DS%22">Radchenko DS</searchLink>; Enamine Ltd. 78 Winston Churchill Street, Kyiv 02094, Ukraine.<br /><searchLink fieldCode="AU" term="%22Moroz+YS%22">Moroz YS</searchLink>; Enamine Ltd. 78 Winston Churchill Street, Kyiv 02094, Ukraine.; Chemspace LLC, 85 Winston Churchill Street, Suite 1, Kyiv 02094, Ukraine.; National Taras Shevchenko University of Kyiv, 60 Volodymyrska Street, Kyiv 01601, Ukraine.<br /><searchLink fieldCode="AU" term="%22Kaiser+A%22">Kaiser A</searchLink>; Institute of Pharmaceutical Chemistry, Goethe University Frankfurt, Max-von-Laue-Str. 9, 60438 Frankfurt am Main, Germany.<br /><searchLink fieldCode="AU" term="%22Krämer+A%22">Krämer A</searchLink>; Institute of Pharmaceutical Chemistry, Goethe University Frankfurt, Max-von-Laue-Str. 9, 60438 Frankfurt am Main, Germany.<br /><searchLink fieldCode="AU" term="%22Knapp+S%22">Knapp S</searchLink>; Institute of Pharmaceutical Chemistry, Goethe University Frankfurt, Max-von-Laue-Str. 9, 60438 Frankfurt am Main, Germany.<br /><searchLink fieldCode="AU" term="%22Schubert-Zsilavecz+M%22">Schubert-Zsilavecz M</searchLink>; Institute of Pharmaceutical Chemistry, Goethe University Frankfurt, Max-von-Laue-Str. 9, 60438 Frankfurt am Main, Germany.<br /><searchLink fieldCode="AU" term="%22Alnouri+MW%22">Alnouri MW</searchLink>; Department of Pharmacology, Max Planck Institute for Heart and Lung Research, 61231 Bad Nauheim, Germany.<br /><searchLink fieldCode="AU" term="%22Offermanns+S%22">Offermanns S</searchLink>; Department of Pharmacology, Max Planck Institute for Heart and Lung Research, 61231 Bad Nauheim, Germany.; Center for Molecular Medicine, Goethe University Frankfurt, 60590 Frankfurt, Germany.<br /><searchLink fieldCode="AU" term="%22Steinhilber+D%22">Steinhilber D</searchLink>; Fraunhofer Institute for Translational Medicine and Pharmacology ITMP, Theodor-Stern-Kai 7, 60596 Frankfurt am Main, Germany.; Fraunhofer Cluster of Excellence Immune-Mediated Diseases CIMD, 60596 Frankfurt am Main, Germany.; Institute of Pharmaceutical Chemistry, Goethe University Frankfurt, Max-von-Laue-Str. 9, 60438 Frankfurt am Main, Germany.<br /><searchLink fieldCode="AU" term="%22Sisignano+M%22">Sisignano M</searchLink>; Fraunhofer Institute for Translational Medicine and Pharmacology ITMP, Theodor-Stern-Kai 7, 60596 Frankfurt am Main, Germany.; Fraunhofer Cluster of Excellence Immune-Mediated Diseases CIMD, 60596 Frankfurt am Main, Germany.; Institute of Clinical Pharmacology, Pharmazentrum Frankfurt/ZAFES, Goethe-University, D-60590 Frankfurt am Main, Germany.<br /><searchLink fieldCode="AU" term="%22Proschak+E%22">Proschak E</searchLink>; Fraunhofer Institute for Translational Medicine and Pharmacology ITMP, Theodor-Stern-Kai 7, 60596 Frankfurt am Main, Germany.; Fraunhofer Cluster of Excellence Immune-Mediated Diseases CIMD, 60596 Frankfurt am Main, Germany.; Institute of Pharmaceutical Chemistry, Goethe University Frankfurt, Max-von-Laue-Str. 9, 60438 Frankfurt am Main, Germany.
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  Data: <searchLink fieldCode="JN" term="%229716531%22">Journal of medicinal chemistry</searchLink> [J Med Chem] 2026 Jun 25; Vol. 69 (12), pp. 14309-14332. <i>Date of Electronic Publication: </i>2026 Jun 11.
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