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Page 1
Discovery of BAY 2413555, First Selective Positive Allosteric Modulator of the M2 Receptor to Restore Cardiac Autonomic Balance.
Vakalopoulos A, Basting D, Brechmann M, Teller H, Boultadakis Arapinis M, Straub A, Mittendorf J, Meininghaus M, Müller T, Nowak-Reppel K, Schäfer M, Wittwer M, Kullmann M, Terjung C, Lang D, Poethko T, Marquardt T, Freudenberger T, Mondritzki T, Hüser J, Heckmann M, Tinel H. Vakalopoulos A, et al. Among authors: nowak reppel k. J Med Chem. 2024 Nov 14;67(21):19165-19187. doi: 10.1021/acs.jmedchem.4c01590. Epub 2024 Oct 28. J Med Chem. 2024. PMID: 39463278
Discovery and Characterization of BAY-184: A New Potent and Selective Acylsulfonamide-Benzofuran In Vivo-Active KAT6AB Inhibitor.
Ter Laak A, Hillig RC, Ferrara SJ, Korr D, Barak N, Lienau P, Herbert S, Fernández-Montalván AE, Neuhaus R, Gorjánácz M, Puetter V, Badock V, Bone W, Strathdee C, Siegel F, Schatz C, Nowak-Reppel K, Doehr O, Gradl S, Hartung IV, Meyerson M, Bouché L. Ter Laak A, et al. Among authors: nowak reppel k. J Med Chem. 2024 Nov 14;67(21):19282-19303. doi: 10.1021/acs.jmedchem.4c01709. Epub 2024 Oct 25. J Med Chem. 2024. PMID: 39450890 Free PMC article.
BRD-810 is a highly selective MCL1 inhibitor with optimized in vivo clearance and robust efficacy in solid and hematological tumor models.
Rauh U, Wei G, Serrano-Wu M, Kosmidis G, Kaulfuss S, Siegel F, Thede K, McFarland J, Lemke CT, Werbeck N, Nowak-Reppel K, Pilari S, Menz S, Ocker M, Zhang W, Davis K, Poncet-Montange G, Roth J, Daniels D, Kaushik VK, Hubbard B, Ziegelbauer K, Golub TR. Rauh U, et al. Among authors: nowak reppel k. Nat Cancer. 2024 Oct;5(10):1479-1493. doi: 10.1038/s43018-024-00814-0. Epub 2024 Aug 23. Nat Cancer. 2024. PMID: 39179926 Free PMC article.
Discovery of YAP1/TAZ pathway inhibitors through phenotypic screening with potent anti-tumor activity via blockade of Rho-GTPase signaling.
Graham K, Lienau P, Bader B, Prechtl S, Naujoks J, Lesche R, Weiske J, Kuehnlenz J, Brzezinka K, Potze L, Zanconato F, Nicke B, Montebaur A, Bone W, Golfier S, Kaulfuss S, Kopitz C, Pilari S, Steuber H, Hayat S, Kamburov A, Steffen A, Schlicker A, Buchgraber P, Braeuer N, Font NA, Heinrich T, Kuhnke L, Nowak-Reppel K, Stresemann C, Steigemann P, Walter AO, Blotta S, Ocker M, Lakner A, von Nussbaum F, Mumberg D, Eis K, Piccolo S, Lange M. Graham K, et al. Among authors: nowak reppel k. Cell Chem Biol. 2024 Jul 18;31(7):1247-1263.e16. doi: 10.1016/j.chembiol.2024.02.013. Epub 2024 Mar 26. Cell Chem Biol. 2024. PMID: 38537632
Discovery and In Vitro Characterization of BAY 2686013, an Allosteric Small Molecule Antagonist of the Human Pituitary Adenylate Cyclase-Activating Polypeptide Receptor.
Langer G, Scott J, Lind C, Otto C, Bothe U, Laux-Biehlmann A, Müller J, le Roy B, Irlbacher H, Nowak-Reppel K, Schlüter A, Davenport AJ, Slack M, Bäurle S. Langer G, et al. Among authors: nowak reppel k. Mol Pharmacol. 2023 Sep;104(3):105-114. doi: 10.1124/molpharm.122.000662. Epub 2023 Jun 22. Mol Pharmacol. 2023. PMID: 37348913
Discovery and Characterization of BAY 1214784, an Orally Available Spiroindoline Derivative Acting as a Potent and Selective Antagonist of the Human Gonadotropin-Releasing Hormone Receptor as Proven in a First-In-Human Study in Postmenopausal Women.
Panknin O, Wagenfeld A, Bone W, Bender E, Nowak-Reppel K, Fernández-Montalván AE, Nubbemeyer R, Bäurle S, Ring S, Schmees N, Prien O, Schäfer M, Friedrich C, Zollner TM, Steinmeyer A, Mueller T, Langer G. Panknin O, et al. Among authors: nowak reppel k. J Med Chem. 2020 Oct 22;63(20):11854-11881. doi: 10.1021/acs.jmedchem.0c01076. Epub 2020 Oct 6. J Med Chem. 2020. PMID: 32960053
Discovery of BAY-298 and BAY-899: Tetrahydro-1,6-naphthyridine-Based, Potent, and Selective Antagonists of the Luteinizing Hormone Receptor Which Reduce Sex Hormone Levels in Vivo.
Wortmann L, Lindenthal B, Muhn P, Walter A, Nubbemeyer R, Heldmann D, Sobek L, Morandi F, Schrey AK, Moosmayer D, Günther J, Kuhnke J, Koppitz M, Lücking U, Röhn U, Schäfer M, Nowak-Reppel K, Kühne R, Weinmann H, Langer G. Wortmann L, et al. Among authors: nowak reppel k. J Med Chem. 2019 Nov 27;62(22):10321-10341. doi: 10.1021/acs.jmedchem.9b01382. Epub 2019 Nov 13. J Med Chem. 2019. PMID: 31670515
Discovery and Characterization of the Potent and Highly Selective (Piperidin-4-yl)pyrido[3,2- d]pyrimidine Based in Vitro Probe BAY-885 for the Kinase ERK5.
Nguyen D, Lemos C, Wortmann L, Eis K, Holton SJ, Boemer U, Moosmayer D, Eberspaecher U, Weiske J, Lechner C, Prechtl S, Suelzle D, Siegel F, Prinz F, Lesche R, Nicke B, Nowak-Reppel K, Himmel H, Mumberg D, von Nussbaum F, Nising CF, Bauser M, Haegebarth A. Nguyen D, et al. Among authors: nowak reppel k. J Med Chem. 2019 Jan 24;62(2):928-940. doi: 10.1021/acs.jmedchem.8b01606. Epub 2019 Jan 9. J Med Chem. 2019. PMID: 30563338
Novel Class of Potent and Cellularly Active Inhibitors Devalidates MTH1 as Broad-Spectrum Cancer Target.
Ellermann M, Eheim A, Rahm F, Viklund J, Guenther J, Andersson M, Ericsson U, Forsblom R, Ginman T, Lindström J, Silvander C, Trésaugues L, Giese A, Bunse S, Neuhaus R, Weiske J, Quanz M, Glasauer A, Nowak-Reppel K, Bader B, Irlbacher H, Meyer H, Queisser N, Bauser M, Haegebarth A, Gorjánácz M. Ellermann M, et al. Among authors: nowak reppel k. ACS Chem Biol. 2017 Aug 18;12(8):1986-1992. doi: 10.1021/acschembio.7b00370. Epub 2017 Jul 12. ACS Chem Biol. 2017. PMID: 28679043 Free article.
Characterization of 12 GnRH peptide agonists - a kinetic perspective.
Nederpelt I, Georgi V, Schiele F, Nowak-Reppel K, Fernández-Montalván AE, IJzerman AP, Heitman LH. Nederpelt I, et al. Among authors: nowak reppel k. Br J Pharmacol. 2016 Jan;173(1):128-41. doi: 10.1111/bph.13342. Epub 2015 Nov 4. Br J Pharmacol. 2016. PMID: 26398856 Free PMC article.