Preclinical evaluation of benzazepine-based PET radioligands (R)-and (S)-11C-Me-NB1 reveals distinct enantiomeric binding patterns and a tightrope walk between GluN2B-and σ1 … A Haider, AM Herde, SD Krämer, J Varisco, C Keller, K Frauenknecht, ... Journal of Nuclear Medicine 60 (8), 1167-1173, 2019 | 27 | 2019 |
Design, synthesis, pharmacological evaluation and docking studies of GluN2B‐selective NMDA receptor antagonists with a benzo [7] annulen‐7‐amine scaffold S Gawaskar, L Temme, JA Schreiber, D Schepmann, A Bonifazi, D Robaa, ... ChemMedChem 12 (15), 1212-1222, 2017 | 25 | 2017 |
GluN2B‐Selective N‐Methyl‐d‐aspartate (NMDA) Receptor Antagonists Derived from 3‐Benzazepines: Synthesis and Pharmacological Evaluation of Benzo[7 … A Benner, A Bonifazi, C Shirataki, L Temme, D Schepmann, W Quaglia, ... ChemMedChem 9 (4), 741-751, 2014 | 25 | 2014 |
Hinge binder scaffold hopping identifies potent calcium/calmodulin-dependent protein kinase kinase 2 (CAMKK2) inhibitor chemotypes BJ Eduful, SN O’Byrne, L Temme, CRM Asquith, Y Liang, A Picado, ... Journal of medicinal chemistry 64 (15), 10849-10877, 2021 | 22 | 2021 |
Synthesis and pharmacological evaluation of enantiomerically pure GluN2B selective NMDA receptor antagonists F Börgel, M Szermerski, JA Schreiber, L Temme, N Strutz‐Seebohm, ... ChemMedChem 13 (15), 1580-1587, 2018 | 22 | 2018 |
Comparative pharmacological study of common NMDA receptor open channel blockers regarding their affinity and functional activity toward GluN2A and GluN2B NMDA receptors L Temme, D Schepmann, JA Schreiber, B Frehland, B Wünsch ChemMedChem 13 (5), 446-452, 2018 | 20 | 2018 |
eEF2K: an atypical kinase target for cancer L Temme, CRM Asquith Nat. Rev. Drug Discov 20 (577), 10.1038, 2021 | 16 | 2021 |
Hydroxymethyl bioisosteres of phenolic GluN2B-selective NMDA receptor antagonists: Design, synthesis and pharmacological evaluation L Temme, B Frehland, D Schepmann, D Robaa, W Sippl, B Wünsch European Journal of Medicinal Chemistry 144, 672-681, 2018 | 16 | 2018 |
Deconstruction–reconstruction approach to analyze the essential structural elements of tetrahydro-3-benzazepine-based antagonists of GluN2B subunit containing NMDA receptors S Dey, L Temme, JA Schreiber, D Schepmann, B Frehland, K Lehmkuhl, ... European Journal of Medicinal Chemistry 138, 552-564, 2017 | 15 | 2017 |
Negative allosteric modulators of the GluN2B NMDA receptor with phenylethylamine structure embedded in ring-expanded and ring-contracted scaffolds L Temme, E Bechthold, JA Schreiber, S Gawaskar, D Schepmann, ... European Journal of Medicinal Chemistry 190, 112138, 2020 | 11 | 2020 |
STK19: a new target for NRAS-driven cancer. CRM Asquith, L Temme Nature Reviews Drug Discovery 19 (9), 579-580, 2020 | 4 | 2020 |
Impact of hydroxy moieties at the benzo [7] annulene ring system of GluN2B ligands: Design, synthesis and biological evaluation L Temme, F Boergel, D Schepmann, D Robaa, W Sippl, C Daniliuc, ... Bioorganic & Medicinal Chemistry 27 (23), 115146, 2019 | 4 | 2019 |
Do GluN2B subunit containing NMDA receptors tolerate a fluorine atom in the phenylalkyl side chain? Y Shuto, S Thum, L Temme, D Schepmann, M Kitamura, B Wünsch MedChemComm 8 (5), 975-981, 2017 | 4 | 2017 |
Identification of 4‐Anilinoquin (az) oline as a Cell‐Active Protein Kinase Novel 3 (PKN3) Inhibitor Chemotype CRM Asquith, L Temme, MP East, T Laitinen, J Pickett, FE Kwarcinski, ... ChemMedChem 17 (12), e202200161, 2022 | 2 | 2022 |
Identification and Optimization of cell active 4-anilino-quin (az) oline Inhibitors for Protein Kinase Novel 3 (PKN3) CRM Asquith, L Temme, T Laitinen, J Pickett, FE Kwarcinski, P Sinha, ... bioRxiv, 2020.03. 02.972943, 2020 | 2 | 2020 |
The second PI(3,5)P2 binding site in the S0 helix of KCNQ1 stabilizes PIP2-at the primary PI1 site with potential consequences on intermediate-to-open state … M Dellin, I Rohrbeck, P Asrani, JA Schreiber, N Ritter, F Glorius, ... Biological Chemistry 404 (4), 241-254, 2023 | 1 | 2023 |
PKN3: a target in cancer metastasis L Temme, T Laitinen, CRM Asquith, CRM Asquith Nat. Rev. Drug Discovery 49, 217-235, 2022 | | 2022 |