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Development of a Potent Nurr1 Agonist Tool for In Vivo Applications

Journal of medicinal chemistry, 2023-05, Vol.66 (9), p.6391-6402

2023

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Benocyclidine (BTCP) as Non‐labelled Reporter Ligand for MS Binding Assays for the PCP Ion Channel Binding Site of the Desensitized Torpedo Nicotinic Acetylcholine Receptor (nAChR)

ChemMedChem, 2023-05, Vol.18 (10), p.e202300048-n/a

2023

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Targeting the Alternative Vitamin E Metabolite Binding Site Enables Noncanonical PPARγ Modulation

Journal of the American Chemical Society, 2023-07, Vol.145 (27), p.14802-14810

2023

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Novel Allosteric Ligands of γ‑Aminobutyric Acid Transporter 1 (GAT1) by MS Based Screening of Pseudostatic Hydrazone Libraries

Journal of medicinal chemistry, 2018-11, Vol.61 (22), p.10310-10332

2018

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Combination of MS Binding Assays and affinity selection mass spectrometry for screening of structurally homogenous libraries as exemplified for a focused oxime library addressing the neuronal GABA transporter 1

European journal of medicinal chemistry, 2020-11, Vol.206, p.112598-112598, Article 112598

2020

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Synthesis and biological evaluation of new GABA-uptake inhibitors derived from proline and from pyrrolidine-2-acetic acid

European journal of medicinal chemistry, 2005-03, Vol.40 (3), p.231-247

2005

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Structure-Guided Design of Nurr1 Agonists Derived from the Natural Ligand Dihydroxyindole

Journal of medicinal chemistry, 2023-10, Vol.66 (19), p.13556-13567

2023

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MS binding assays for GlyT1 based on Org24598 as nonlabelled reporter ligand

Neuropharmacology, 2019-12, Vol.161, p.107561-107561, Article 107561

2019

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Screening for New Inhibitors of Glycine Transporter 1 and 2 by Means of MS Binding Assays

ChemMedChem, 2021-10, Vol.16 (19), p.3094-3104

2021

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Synthesis and biological evaluation of novel N-substituted nipecotic acid derivatives with an alkyne spacer as GABA uptake inhibitors

Bioorganic & medicinal chemistry, 2018-07, Vol.26 (12), p.3668-3687

2018

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Synthesis and biological evaluation of novel N-substituted nipecotic acid derivatives with a cis-alkene spacer as GABA uptake inhibitors

Bioorganic & medicinal chemistry, 2019-03, Vol.27 (5), p.822-831

2019

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Synthesis and biological evaluation of novel N-substituted nipecotic acid derivatives with a trans-alkene spacer as potent GABA uptake inhibitors

Bioorganic & medicinal chemistry, 2018-12, Vol.26 (22), p.5944-5961

2018

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Structural Modification of the Natural Product Valerenic Acid Tunes RXR Homodimer Agonism

ChemMedChem, 2023-11, Vol.18 (21), p.e202300404-e202300404

2023

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Design, synthesis and SAR studies of GABA uptake inhibitors derived from 2-substituted pyrrolidine-2-yl-acetic acids

Bioorganic & medicinal chemistry, 2015-03, Vol.23 (6), p.1284-1306

2015

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Application of the concept of oxime library screening by mass spectrometry (MS) binding assays to pyrrolidine-3-carboxylic acid derivatives as potential inhibitors of γ-aminobutyric acid transporter 1 (GAT1)

Bioorganic & medicinal chemistry, 2019-07, Vol.27 (13), p.2753-2763

2019

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Synthesis of 4-substituted nipecotic acid derivatives and their evaluation as potential GABA uptake inhibitors

Bioorganic & medicinal chemistry, 2016-05, Vol.24 (9), p.2072-2096

2016

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Generation and screening of pseudostatic hydrazone libraries derived from 5-substituted nipecotic acid derivatives at the GABA transporter mGAT4

Bioorganic & medicinal chemistry, 2019-01, Vol.27 (1), p.144-152

2019

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MS Binding Assays with UNC0642 as reporter ligand for the MB327 binding site of the nicotinic acetylcholine receptor

Toxicology letters, 2024-02, Vol.392, p.94-106

2024

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Development of New Photoswitchable Azobenzene Based γ‑Aminobutyric Acid (GABA) Uptake Inhibitors with Distinctly Enhanced Potency upon Photoactivation

Journal of medicinal chemistry, 2018-07, Vol.61 (14), p.6211-6235

2018

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Discovery of novel multifunctional ligands targeting GABA transporters, butyrylcholinesterase, β-secretase, and amyloid β aggregation as potential treatment of Alzheimer's disease

European journal of medicinal chemistry, 2023-12, Vol.261, p.115832-115832, Article 115832

2023

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Synthesis and Biological Evaluation of Nipecotic Acid and Guvacine Derived 1,3‐Disubstituted Allenes as Inhibitors of Murine GABA Transporter mGAT1

ChemMedChem, 2019-06, Vol.14 (12), p.1135-1151

2019

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Development of Highly Potent GAT1 Inhibitors: Synthesis of Nipecotic Acid Derivatives with N‐Arylalkynyl Substituents

ChemMedChem, 2017-03, Vol.12 (5), p.362-371

2017

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Discovery of new, highly potent and selective inhibitors of BuChE - design, synthesis, in vitro and in vivo evaluation and crystallography studies

European journal of medicinal chemistry, 2023-03, Vol.249, p.115135, Article 115135

2023

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A novel binding site in the nicotinic acetylcholine receptor for MB327 can explain its allosteric modulation relevant for organophosphorus-poisoning treatment

Toxicology letters, 2023-01, Vol.373, p.160-171

2023

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MS Binding Assays for D 1 and D 5 Dopamine Receptors

ChemMedChem, 2015-11, Vol.10 (11), p.1924-1931

2015

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Development of a Potent Nurr1 Agonist Tool for In Vivo Applications

Benocyclidine (BTCP) as Non‐labelled Reporter Ligand for MS Binding Assays for the PCP Ion Channel Binding Site of the Desensitized Torpedo Nicotinic Acetylcholine Receptor (nAChR)

Targeting the Alternative Vitamin E Metabolite Binding Site Enables Noncanonical PPARγ Modulation

Novel Allosteric Ligands of γ‑Aminobutyric Acid Transporter 1 (GAT1) by MS Based Screening of Pseudostatic Hydrazone Libraries

Combination of MS Binding Assays and affinity selection mass spectrometry for screening of structurally homogenous libraries as exemplified for a focused oxime library addressing the neuronal GABA transporter 1

Synthesis and biological evaluation of new GABA-uptake inhibitors derived from proline and from pyrrolidine-2-acetic acid

Structure-Guided Design of Nurr1 Agonists Derived from the Natural Ligand Dihydroxyindole

MS binding assays for GlyT1 based on Org24598 as nonlabelled reporter ligand

Screening for New Inhibitors of Glycine Transporter 1 and 2 by Means of MS Binding Assays

Synthesis and biological evaluation of novel N-substituted nipecotic acid derivatives with an alkyne spacer as GABA uptake inhibitors

Synthesis and biological evaluation of novel N-substituted nipecotic acid derivatives with a cis-alkene spacer as GABA uptake inhibitors

Synthesis and biological evaluation of novel N-substituted nipecotic acid derivatives with a trans-alkene spacer as potent GABA uptake inhibitors

Structural Modification of the Natural Product Valerenic Acid Tunes RXR Homodimer Agonism

Design, synthesis and SAR studies of GABA uptake inhibitors derived from 2-substituted pyrrolidine-2-yl-acetic acids

Application of the concept of oxime library screening by mass spectrometry (MS) binding assays to pyrrolidine-3-carboxylic acid derivatives as potential inhibitors of γ-aminobutyric acid transporter 1 (GAT1)

Synthesis of 4-substituted nipecotic acid derivatives and their evaluation as potential GABA uptake inhibitors

Generation and screening of pseudostatic hydrazone libraries derived from 5-substituted nipecotic acid derivatives at the GABA transporter mGAT4

MS Binding Assays with UNC0642 as reporter ligand for the MB327 binding site of the nicotinic acetylcholine receptor

Development of New Photoswitchable Azobenzene Based γ‑Aminobutyric Acid (GABA) Uptake Inhibitors with Distinctly Enhanced Potency upon Photoactivation

Discovery of novel multifunctional ligands targeting GABA transporters, butyrylcholinesterase, β-secretase, and amyloid β aggregation as potential treatment of Alzheimer's disease

Synthesis and Biological Evaluation of Nipecotic Acid and Guvacine Derived 1,3‐Disubstituted Allenes as Inhibitors of Murine GABA Transporter mGAT1

Development of Highly Potent GAT1 Inhibitors: Synthesis of Nipecotic Acid Derivatives with N‐Arylalkynyl Substituents

Discovery of new, highly potent and selective inhibitors of BuChE - design, synthesis, in vitro and in vivo evaluation and crystallography studies

A novel binding site in the nicotinic acetylcholine receptor for MB327 can explain its allosteric modulation relevant for organophosphorus-poisoning treatment

MS Binding Assays for D 1 and D 5 Dopamine Receptors

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