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| Hahn, M. G. et al. | Discovery of the soluble guanylate cyclase activator Runcaciguat (BAY 1101042) | J Med Chem 64, 9, 5323–5344 (2021) | https://doi.org/10.1021/acs.jmedchem.0c02154 |
| Delahaye, L. et al. | Feedback from the sixth European Bioanalysis Forum Young Scientist Symposium | Bioanalysis 13, 9, 669–674 (2021) | https://doi.org/10.4155/bio-2021-0051 |
| Ede, S. et al. | Improved diazo-transfer reaction for DNA-encoded chemistry and its potential application for macrocyclic DEL-libraries | Molecules 26, 6, 1790 (2021) | https://doi.org/10.3390/molecules26061790 |
| Liu, D. et al. | Nickel‐catalysed N‐arylation of NH‐sulfoximines with aryl halides via paired electrolysis | Angew Chem Int Ed 60, 17, 9444–9449 (2021) | https://doi.org/10.1002/anie.202016310 |
| Calogero, S. et al. | Feedback from the Science Café from the sixth European Bioanalysis Forum Young Scientist Symposium | Bioanalysis 13, 3, 129–133 (2021) | https://doi.org/10.4155/bio-2021-0017 |
| Sutherland, M. et al. | Rational design and synthesis of selective PRMT4 inhibitors: a new chemotype for development of cancer therapeutics | ChemMedChem 16, 7, 1116–1125 (2021) | https://doi.org/10.1002/cmdc.202100018 |
| Moosmayer, D. et al. | Crystal structures of the selenoprotein glutathione peroxidase 4 in its apo form and in complex with the covalently bound inhibitor ML162 | Acta Crystallogr D Struct Biol 77, 2, 237–248 (2021) | https://doi.org/10.1107/S2059798320016125 |
| Lemos, C. et al. | The potent AMPK inhibitor BAY-3827 shows strong efficacy in androgen-dependent prostate cancer models | Cell Oncol 44, 581–594 (2021) | https://doi.org/10.1007/s13402-020-00584-8 |
| Pischon, H. et al. | Artificial intelligence in toxicologic pathology: quantitative evaluation of compound-induced hepatocellular hypertrophy in rats | Toxicol Pathol 49, 4, 928–937 (2021) | https://doi.org/10.1177/0192623320983244 |
| Lissy, M. et al. | Thorough QT/QTc study evaluating the effect of macimorelin on cardiac safety parameters in healthy participants | Clinical Pharm in Drug Dev 10, 5, 494–501 (2021) | https://doi.org/10.1002/cpdd.872 |
| Atilaw, Y. et al. | Solution conformations shed light on PROTAC cell permeability | ACS Med Chem Lett 12, 1, 107–114 (2021) | https://doi.org/10.1021/acsmedchemlett.0c00556 |
| Author | Title | Journal | Link |
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| Hillisch, A. et al. | Design, synthesis and pharmacological characterisation of a neutral, non-prodrug thrombin inhibitor with good oral pharmacokinetics | J Med Chem 63, 21, 12574–12594 (2020) | https://doi.org/10.1021/acs.jmedchem.0c01035 |
| Goodman, J. et al. | Update to the European Bioanalysis Forum recommendation on biomarkers assays: bringing context of use into practice | Bioanalysis 12, 1427–1437 (2020) | https://doi.org/10.4155/bio-2020-0243 |
| Agueusop, I. et al. | Short-term variability of the human serum metabolome depending on nutritional and metabolic health status | Sci Rep 10, 16310 (2020) | https://doi.org/10.1038/s41598-020-72914-7 |
| Lemos, C. et al. | Identification of small molecules that modulate mutant p53 condensation | iScience 23, 11, 101517 (2020) | https://doi.org/10.1016/j.isci.2020.101517 |
| Panknin, O. et al. | Discovery and characterisation 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 | J Med Chem 63, 20, 11854–11881 (2020) | https://doi.org/10.1021/acs.jmedchem.0c01076 |
| Werbeck, N. D. et al. | A distal regulatory region of a class I human histone deacetylase | Nat Commun 11, 3841 (2020) | https://doi.org/10.1038/s41467-020-17610-w |
| Zhao, X.-Y. et al. | Targeted inhibition of activated protein C by a non-active-site inhibitory antibody to treat hemophilia | Nat Commun 11, 2992 (2020) | https://doi.org/10.1038/s41467-020-16720-9 |
| Lücking, U. et al. | Damage incorporated: discovery of the potent, highly selective, orally available ATR inhibitor BAY 1895344 with favorable pharmacokinetic properties and promising efficacy in monotherapy and in combination treatments in preclinical tumour models | J Med Chem 63, 13, 7293–7325 (2020) | https://doi.org/10.1021/acs.jmedchem.0c00369 |
| Schulze, V. K. et al. | Treating cancer by spindle assembly checkpoint abrogation: discovery of two clinical candidates, BAY 1161909 and BAY 1217389, targeting MPS1 kinase | J Med Chem 63, 15, 8025–8042 (2020) | https://doi.org/10.1021/acs.jmedchem.9b02035 |
| Timmerman, P. et al. | European Bioanalysis Forum feedback on draft ICH M10 guideline on bioanalytical method validation during the step 2b public consultation period | Bioanalysis 12, 1–11 (2020) | https://doi.org/10.4155/bio-2020-0065 |
| Klaus, B. et al. | Safety, tolerability, pharmacokinetics and pharmacodynamics of Macimorelin in healthy adults: results of a single-dose, randomised controlled study | Growth Hormone & IGF Research 52, 101321 (2020) | https://doi.org/10.1016/j.ghir.2020.101321 |
| Mortier, J. et al. | Computationally empowered workflow identifies novel covalent allosteric binders for KRASG12C | ChemMedChem 15, 10, 827–832 (2020) | https://doi.org/10.1002/cmdc.201900727 |
| Eaton, J. K. et al. | Selective covalent targeting of GPX4 using masked nitrile-oxide electrophiles | Nat Chem Biol 16, 497–506 (2020) | https://doi.org/10.1038/s41589-020-0501-5 |
| Wu, X. et al. | Mechanistic insights into cancer cell killing through interaction of phosphodiesterase 3A and Schlafen family member 12 | J Biol Chem 295, 11, 3431–3446 (2020) | https://doi.org/10.1074/jbc.RA119.011191 |
| Taavitsainen, P. et al. | Absorption, distribution, metabolism and excretion of darolutamide (a novel non-steroidal androgen receptor antagonist) in rats | Xenobiotica 50, 8, 967–979 (2020) | https://doi.org/10.1080/00498254.2020.1723038 |
| Brzezinka, K. et al. | Characterisation of the menin-MLL interaction as therapeutic cancer target | Cancers (Basel) 12, 1, 201 (2020) | https://doi.org/10.3390/cancers12010201 |
| Parker, V. E. R. et al. | Efficacy, safety and mechanistic insights of Cotadutide, a dual receptor glucagon-like peptide-1 and glucagon agonist | The Journal of Clinical Endocrinology & Metabolism 105, 803–820 (2020) | https://doi.org/10.1210/clinem/dgz047 |
| Lefranc, J. et al. | Discovery of BAY-985, a highly selective TBK1/IKKε inhibitor | J Med Chem 63, 601–612 (2020) | https://doi.org/10.1021/acs.jmedchem.9b01460 |
| Wengner, A. M. et al. | The novel ATR inhibitor BAY 1895344 is efficacious as monotherapy and combined with DNA damage-inducing or repair-compromising therapies in preclinical cancer models | Mol Cancer Ther 19, 1, 26–38 (2020) | https://doi.org/10.1158/1535-7163.MCT-19-0019 |
| Author | Title | Journal | Link |
|---|---|---|---|
| Werner, S. et al. | Discovery and characterisation of the potent and selective P2X4 inhibitor N-[4-(3-chlorophenoxy)-3-sulfamoylphenyl]-2-phenylacetamide (BAY-1797) and structure-guided amelioration of its CYP3A4 induction profile | J Med Chem 62, 24, 11194–11217 (2019) | https://doi.org/10.1021/acs.jmedchem.9b01304 |
| Pihl, S. et al. | EBF recommendation on practical management of critical reagents for antidrug antibody ligand-binding assays | Bioanalysis 11, 19, 1787–1798 (2019) | https://doi.org/10.4155/bio-2019-0248 |
| Lewis, T. A. et al. | Optimisation of PDE3A modulators for SLFN12-dependent cancer cell killing | ACS Med Chem Lett 10, 11, 1537–1542 (2019) | https://doi.org/10.1021/acsmedchemlett.9b00360 |
| Zurth, C. et al. | Drug-drug interaction potential of darolutamide: in vitro and clinical studies | Eur J Drug Metab Pharmacokinet 44, 747–759 (2019) | https://doi.org/10.1007/s13318-019-00577-5 |
| Shore, N. et al. | Evaluation of clinically relevant drug-drug interactions and population pharmacokinetics of darolutamide in patients with nonmetastatic castration-resistant prostate cancer: results of pre-specified and post hoc analyses of the phase III ARAMIS trial | Target Oncol 14, 527–539 (2019) | https://doi.org/10.1007/s11523-019-00674-0 |
| Protti, M. et al. | Feedback from the fifth European Bioanalysis Forum Young Scientist Symposium | Bioanalysis 11, 16, 1453–1458 (2019) | https://doi.org/10.4155/bio-2019-0206 |
| Brzezinka, K. et al. | Functional diversity of inhibitors tackling the differentiation blockage of MLL-rearranged leukemia | J Hematol Oncol 12, 66 (2019) | https://doi.org/10.1186/s13045-019-0749-y |
| Renders, L. et al. | First-in-human phase I studies of PRS-080#22, a hepcidin antagonist, in healthy volunteers and patients with chronic kidney disease undergoing hemodialysis | PLoS ONE 14, e0212023 (2019) | https://doi.org/10.1371/journal.pone.0212023 |
| Grünewald, S. et al. | Rogaratinib: a potent and selective pan-FGFR inhibitor with broad antitumour activity in FGFR-overexpressing preclinical cancer models | Int J Cancer 145, 5, 1346–1357 (2019) | https://doi.org/10.1002/ijc.32224 |
| Siemeister, G. et al. | Inhibition of BUB1 kinase by BAY 1816032 sensitises tumour cells toward taxanes, ATR and PARP inhibitors in vitro and in vivo | Clin Cancer Res 25, 4, 1404–1414 (2019) | https://doi.org/10.1158/1078-0432.CCR-18-0628 |
| Zahner, C. et al. | No clinically relevant interactions of St. John's wort extract Ze 117 low in hyperforin with cytochrome P450 enzymes and P‐glycoprotein | Clin Pharma and Therapeutics 106, 2, 432–440 (2019) | https://doi.org/10.1002/cpt.1392 |
| Vriens, K. et al. | Evidence for an alternative fatty acid desaturation pathway increasing cancer plasticity | Nature 566, 403–406 (2019) | https://doi.org/10.1038/s41586-019-0904-1 |
| Hillig, R. C. et al. | Discovery of potent SOS1 inhibitors that block RAS activation via disruption of the RAS-SOS1 interaction | Proc Natl Acad Sci U S A 116, 7, 2551–2560 (2019) | https://doi.org/10.1073/pnas.1812963116 |
| Wilson, A. et al. | European Bioanalysis Forum recommendation on the best practices to demonstrate processed sample stability | Bioanalysis 11, 1, 7–11 (2019) | https://doi.org/10.4155/bio-2018-0271 |
| Nguyen, D. et al. | Discovery and characterisation of the potent and highly selective (piperidin-4-yl)pyrido[3,2- d]pyrimidine based in vitro probe BAY-885 for the kinase ERK5 | J Med Chem 62, 2,928–940 (2019) | https://doi.org/10.1021/acs.jmedchem.8b01606 |
| Author | Title | Journal | Link |
|---|---|---|---|
| Kall, M. A. et al. | Incurred sample reproducibility: 10 years of experiences: views and recommendations from the European Bioanalysis Forum | Bioanalysis 10, 21, 1723–1732 (2018) | https://doi.org/10.4155/bio-2018-0194 |
| Quanz, M. et al. | Preclinical efficacy of the novel monocarboxylate transporter 1 inhibitor BAY-8002 and associated markers of resistance | Mol Cancer Ther 17, 11, 2285–2296 (2018) | https://doi.org/10.1158/1535-7163.MCT-17-1253 |
| Timmerman, P. et al. | Toward decision-based acceptance criteria for bioanalytical method validation: a proposal for discussion from the European Bioanalysis Forum | Bioanalysis 10, 16, 1255–1259 (2018) | https://doi.org/10.4155/bio-2018-0131 |
| Klutzny, S. et al. | PDE5 inhibition eliminates cancer stem cells via induction of PKA signalling | Cell Death Dis 9, 192 (2018) | https://doi.org/10.1038/s41419-017-0202-5 |
| Goodman, J. et al. | Feedback from the European Bioanalysis Forum: focus workshop on current analysis of immunogenicity: best practices and regulatory hurdles | Bioanalysis 10, 8, 197–204 (2018) | https://doi.org/10.4155/bio-2017-4971 |
| Schultze-Mosgau, M.-H. et al. | Characterisation of the pharmacokinetics of Vilaprisan: Bioavailability, excretion, biotransformation and drug-drug interaction potential | Clin Pharmacokinet 57, 1001–1015 (2018) | https://doi.org/10.1007/s40262-017-0607-4 |
| Author | Title | Journal | Link |
|---|---|---|---|
| Lücking, U. et al. | Identification of Atuveciclib (BAY 1143572), the first highly selective, clinical PTEFb/CDK9 inhibitor for the treatment of cancer |
ChemMedChem 12, 21, 1776–1793 (2017) | https://doi.org/10.1002/cmdc.201700447 |
| Ellermann, M. et al. | Novel class of potent and cellularly active inhibitors devalidates MTH1 as broad-spectrum cancer target |
ACS Chem Biol 12, 8, 1986–1992 (2017) |
https://doi.org/10.1021/acschembio.7b00370 |
| Willuda, J. et al. | Preclinical antitumour efficacy of BAY 1129980 - a novel Auristatin-based anti-C4.4A (LYPD3) antibody-drug conjugate for the treatment of non-small cell lung cancer |
Mol Cancer Ther 16, 5, 893–904 (2017) |
https://doi.org/10.1158/1535-7163.MCT-16-0474 |
| Undre, N. & Dickinson, J. | Relative bioavailability of single doses of prolonged-release tacrolimus administered as a suspension, orally or via a nasogastric tube, compared with intact capsules: a phase 1 study in healthy participants |
BMJ Open 7, 4, e012252 (2017) |
https://doi.org/10.1136/bmjopen-2016-012252 |
| Santag, S. et al. | BAY 1143269, a novel MNK1 inhibitor, targets oncogenic protein expression and shows potent anti-tumour activity |
Cancer Lett 390, 21–29 (2017) |
https://doi.org/10.1016/j.canlet.2016.12.029 |
| Klutzny, S. et al. | Functional inhibition of acid sphingomyelinase by Fluphenazine triggers hypoxia-specific tumour cell death |
Cell Death Dis 8, e2709 (2017) |
https://doi.org/10.1038/cddis.2017.130 |
| Basit, F. et al. | Mitochondrial complex I inhibition triggers a mitophagy-dependent ROS increase leading to necroptosis and ferroptosis in melanoma cells |
Cell Death Dis 8, e2716 (2017) |
https://doi.org/10.1038/cddis.2017.133 |
| Ericzon, B. et al. | Pharmacokinetics of prolonged‐release tacrolimus versus immediate‐release tacrolimus in de novo liver transplantation: a randomised phase III substudy |
Clinical Transplantation 31, 6, e12958 (2017) |
https://doi.org/10.1111/ctr.12958 |
| Pusch, S. et al. | Pan-mutant IDH1 inhibitor BAY 1436032 for effective treatment of IDH1 mutant astrocytoma in vivo |
Acta Neuropathol 133, 629–644 (2017) |
https://doi.org/10.1007/s00401-017-1677-y |
| Politz, O. et al. | BAY 1125976, a selective allosteric AKT1/2 inhibitor, exhibits high efficacy on AKT signalling-dependent tumour growth in mouse models |
Int J Cancer 140, 2, 449–459 (2017) |
https://doi.org/10.1002/ijc.30457 |
| Author | Title | Journal | Link |
|---|---|---|---|
| Sommer, A. et al. |
Preclinical efficacy of the Auristatin-based antibody-drug conjugate BAY 1187982 for the treatment of FGFR2-positive solid tumors | Cancer Res 76, 21, 6331–6339 (2016 | https://doi.org/10.1158/0008-5472.CAN-16-0180 |
| Schütt, B. et al. | Pharmacodynamics and safety of the novel selective progesterone receptor modulator Vilaprisan: a double-blind, randomised, placebo-controlled phase 1 trial in healthy women | Hum Reprod 31, 8, 1703–1712 (2016) | https://doi.org/10.1093/humrep/dew140 |
| Eggert, E. et al. | Discovery and characterisation of a highly potent and selective aminopyrazoline-based in vivo probe (BAY-598) for the protein lysine methyltransferase SMYD2 | J Med Chem 59, 10, 4578–4600 (2016) | https://doi.org/10.1021/acs.jmedchem.5b01890 |
| Kapoor, K. et al. | Mechanism of inhibition of human glucose transporter GLUT1 is conserved between cytochalasin B and phenylalanine amides |
Proc Natl Acad Sci U S A 113, 17, 4711–4716 (2016) | https://doi.org/10.1073/pnas.1603735113 |
| Wengner, A. M. et al. | Novel Mps1 kinase inhibitors with potent antitumour activity | Mol Cancer Ther 15, 4, 583–592 (2016) | https://doi.org/10.1158/1535-7163.MCT-15-0500 |
| Reynoird, N. et al. | Coordination of stress signals by the lysine methyltransferase SMYD2 promotes pancreatic cancer |
Genes Dev 30, 7, 772–785 (2016) | https://doi.org/10.1101/gad.275529.115 |
| Baron, A. P. et al. | Probing the catalytic functions of BUB1 kinase using the small molecule inhibitors BAY-320 and BAY-524 |
Elife 5, e12187 (2016) | https://doi.org/10.7554/eLife.12187 |
| Hernando, H. et al. | EZH2 inhibition blocks multiple myeloma cell growth through upregulation of epithelial tumour suppressor genes |
Mol Cancer Ther 15, 2, 287–298 (2016) | https://doi.org/10.1158/1535-7163.MCT-15-0486 |
| Ferreira de Freitas, R. et al. | Discovery of a potent class I protein arginine methyltransferase fragment inhibitor | J Med Chem 59, 3, 1176–1183 (2016) | https://doi.org/10.1021/acs.jmedchem.5b01772 |
| Sugawara, T. et al. | BAY 1024767 blocks androgen receptor mutants found in castration-resistant prostate cancer patients | Oncotarget 7, 6015–6028 (2016) | https://doi.org/10.18632/oncotarget.6864 |
| Hartung, I. V. et al. | Optimisation of allosteric MEK inhibitors. Part 2: taming the sulfamide group balances compound distribution properties |
Bioorg Med Chem Lett 26, 1, 186–193 (2016) | https://doi.org/10.1016/j.bmcl.2015.11.004 |
| Author | Title | Journal | Link |
|---|---|---|---|
| Luense, S. et al. |
Quantification of histone H3 Lys27 trimethylation (H3K27me3) by high-throughput microscopy enables cellular large-scale screening for small-molecule EZH2 inhibitors |
J Biomol Screen 20, 2, 190–201 (2015) |
https://doi.org/10.1177/1087057114559668 |
| Meier, J. C. et al. |
Knockdown of platinum-induced growth differentiation factor 15 abrogates p27-mediated tumour growth delay in the chemoresistant ovarian cancer model A2780cis |
Cancer Med 4, 2, 253–267 (2015) |
https://doi.org/10.1002/cam4.354 |
| Schulze, J. et al. | Cell-based protein stabilisation assays for the detection of interactions between small-molecule inhibitors and BRD4 |
J Biomol Screen 20, 2, 180–189 (2015) |
https://doi.org/10.1177/1087057114552398 |
| von Nussbaum, F. and Süssmuth, R. D. |
Multiple attack on bacteria by the new antibiotic teixobactin |
Angew Chem Int Ed Engl 54, 23, 6684–6686 (2015) |
https://doi.org/10.1002/anie.201501440 |
| von Nussbaum, F. et al. |
Freezing the bioactive conformation to boost potency: the identification of BAY 85-8501, a selective and potent inhibitor of human neutrophil elastase for pulmonary diseases |
Chem Med Chem 10, 7, 1163–1173 (2015) |
https://doi.org/10.1002/cmdc.201500131 |
| Gentili, C. et al. |
Chromosome missegregation associated with RUVBL1 deficiency |
PLoS One 10, 7, e0133576 (2015) |
https://doi.org/10.1371/journal.pone.0133576 |
| Nakamaru, Y. et al. |
Investigation of potential pharmacokinetic interactions between Teneligliptin and Metformin in steady-state conditions in healthy adults |
Clinical Therapeutics 37, 9, 2007–2018 (2015) |
https://doi.org/10.1016/j.clinthera.2015.06.012 |
| von Nussbaum, F. and Li, V. M.-J. | Neutrophil elastase inhibitors for the treatment of (cardio)pulmonary diseases: into clinical testing with pre-adaptive pharmacophores |
Bioorg Med Chem Lett 25, 20, 4370–4381 (2015) |
https://doi.org/10.1016/j.bmcl.2015.08.049 |
| Wenzel, C. et al. |
A novel 3D high-content assay identifies compounds that prevent fibroblast invasion into tissue surrogates |
Exp Cell Res 339, 1, 35–43 (2015) |
https://doi.org/10.1016/j.yexcr.2015.10.003 |
| Hartung, I. V. et al. |
Modular assembly of allosteric MEK inhibitor structural elements unravels potency and feedback-modulation handles |
Chem Med Chem 10, 12, 2004–2013 (2015) |
https://doi.org/10.1002/cmdc.201500442 |