The Novel ATR Inhibitor BAY 1895344 Is Efficacious as Monotherapy and Combined with DNA Damage–Inducing or Repair–Compromising Therapies in Preclinical Cancer Models

Antje M. Wengner, Gerhard Siemeister, Ulrich Lücking, +17

Molecular Cancer Therapeutics

Identification of Atuveciclib (BAY 1143572), the First Highly Selective, Clinical PTEFb/CDK9 Inhibitor for the Treatment of Cancer

Ulrich Lücking, Arne Scholz, Philip Lienau, +24

ChemMedChem

The Lab Oddity Prevails: Discovery of Pan‐CDK Inhibitor (<i>R</i>)‐<i>S</i>‐Cyclopropyl‐<i>S</i>‐(4‐{[4‐{[(1<i>R</i>,2<i>R</i>)‐2‐hydroxy‐1‐methylpropyl]oxy}‐5‐(trifluoromethyl)pyrimidin‐2‐yl]amino}phenyl)sulfoximide (BAY 1000394) for the Treatment of Cancer

Ulrich Lücking, Rolf Jautelat, Martin Krüger, +9

ChemMedChem

Aminopyrimidine Zk 304709Lab Oddity PrevailsLead IdentificationBay 1000394Zk 304709 +19

Mechanism-Based Inhibition: Deriving KI and kinact Directly from Time-Dependent IC50 Values

Ben‐Fillippo Krippendorff, Roland Neuhaus, Philip Lienau, +2

SLAS DISCOVERY

BAY 1000394, a Novel Cyclin-Dependent Kinase Inhibitor, with Potent Antitumor Activity in Mono- and in Combination Treatment upon Oral Application

Gerhard Siemeister, Ulrich Lücking, Antje M. Wengner, +5

Molecular Cancer Therapeutics

Oral ApplicationChemoprevention StrategyRetinoblastoma ProteinBay 1000394Pharmacotherapy +17

Novel Mps1 Kinase Inhibitors with Potent Antitumor Activity

Antje M. Wengner, Gerhard Siemeister, Marcus Koppitz, +17

Molecular Cancer Therapeutics

OncologyMedicinePotent Antitumor ActivityMolecular BiologyImmune Checkpoint Inhibitor +12

Characterization of novel MPS1 inhibitors with preclinical anticancer activity

Mohamed Jèmaà, Lorenzo Galluzzi, Oliver Kepp, +15

Cell Death and Differentiation

Novel Mps1 InhibitorsMedicineTumor TargetingAnti-cancer AgentPharmacology +3

Conformational Adaption May Explain the Slow Dissociation Kinetics of Roniciclib (BAY 1000394), a Type I CDK Inhibitor with Kinetic Selectivity for CDK2 and CDK9

Pelin Ayaz, Dorothee Andres, Dennis Kwiatkowski, +5

ACS Chemical Biology

Sagopilone crosses the blood–brain barrier in vivo to inhibit brain tumor growth and metastases

Jens Hoffmann, Iduna Fichtner, M Lemm, +5

Neuro-Oncology

Tumor InnervationImmunologyPathologyBrain Tumor GrowthPharmacotherapy +18

Cyclin-dependent kinase 9 is a novel specific molecular target in adult T-cell leukemia/lymphoma

Tomoko Narita, Takashi Ishida, Asahi Ito, +17

Blood