J.K. Muckelbauer

Bristol-Myers Squibb (Germany) — Germany

Medicine · Health Sciences

21h-index1.6kcitations67works0.02yr avg
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Research Topics

Chronic Lymphocytic Leukemia Research(10), PI3K/AKT/mTOR signaling in cancer(7), Protein Kinase Regulation and GTPase Signaling(6), Computational Drug Discovery Methods(6), Synthesis and biological activity(6)

Publications67 total

Discovery of pyrrolo[2,1-f][1,2,4]triazine-based inhibitors of adaptor protein 2-associated kinase 1 for the treatment of pain
Medicinal Chemistry Research·2023· 1 citedOpen Access
Phthalazinone-based lactams and cyclic ureas as ROCK2 selective inhibitors
Bioorganic & Medicinal Chemistry Letters·2023· 4 citedOpen Access
Discovery of a Partial Glucokinase Activator Clinical Candidate: Diethyl ((3-(3-((5-(Azetidine-1-carbonyl)pyrazin-2-yl)oxy)-5-isopropoxybenzamido)-1<i>H</i>-pyrazol-1-yl)methyl)phosphonate (BMS-820132)
Journal of Medicinal Chemistry·2022· 9 citedOpen Access
Bicyclic Heterocyclic Replacement of an Aryl Amide Leading to Potent and Kinase-Selective Adaptor Protein 2-Associated Kinase 1 Inhibitors
Journal of Medicinal Chemistry·2022· 14 citedOpen Access
Identification and characterization of TYK2 pseudokinase domain stabilizers that allosterically inhibit TYK2 signaling
Methods in enzymology on CD-ROM/Methods in enzymology·2022· 6 cited
The journey of macromolecular crystallography in pharmaceutical discovery research at Abbvie and BMS
Acta Crystallographica Section A Foundations and Advances·2021Open Access
Discovery, Structure–Activity Relationships, and In Vivo Evaluation of Novel Aryl Amides as Brain Penetrant Adaptor Protein 2-Associated Kinase 1 (AAK1) Inhibitors for the Treatment of Neuropathic Pain
Journal of Medicinal Chemistry·2021· 16 citedOpen Access
CRYSTAL STRUCTURE OF AP2 ASSOCIATED KINASE 1 ISOFORM 1 COMPLEXED WITH LIGAND N-[3-METHOXY-4-(1,3-OXAZOL-5-YL)PHENYL]-3-(PROPAN-2-YL)PIPERIDINE-2-CARBOXAMIDE
2021
CRYSTAL STRUCTURE OF AP2 ASSOCIATED KINASE 1 ISOFORM 1 COMPLEXED WITH LIGAND (2R)-2-AMINO-N-[3-METHOXY-4- (1,3-OXAZOL-5-YL)PHENYL]-4-METHYLPENTANAMIDE
2021
Using yeast surface display to engineer a soluble and crystallizable construct of hematopoietic progenitor kinase 1 (HPK1)
Acta Crystallographica Section F Structural Biology Communications·2020· 16 citedOpen Access
Identification of 5H-chromeno[3,4-c]pyridine and 6H-isochromeno[3,4-c]pyridine derivatives as potent and selective dual ROCK inhibitors
Bioorganic & Medicinal Chemistry Letters·2020· 15 citedOpen Access
CRYSTAL STRUCTURE OF RHO-ASSOCIATED PROTEIN KINASE 2 (ROCK2) IN COMPLEX WITH A PHENYLPYRAZOLE AMIDE INHIBITOR
2020
CRYSTAL STRUCTURE OF RHO-ASSOCIATED PROTEIN KINASE 1 (ROCK1) IN COMPLEX WITH A PHENYLPYRAZOLE AMIDE INHIBITOR
2020
Identification of <i>N</i>-Methyl Nicotinamide and <i>N</i>-Methyl Pyridazine-3-Carboxamide Pseudokinase Domain Ligands as Highly Selective Allosteric Inhibitors of Tyrosine Kinase 2 (TYK2)
Journal of Medicinal Chemistry·2019· 84 citedOpen Access
Identification of Imidazo[1,2-<i>b</i>]pyridazine Derivatives as Potent, Selective, and Orally Active Tyk2 JH2 Inhibitors
ACS Medicinal Chemistry Letters·2019· 49 citedOpen Access
Identification of a Potent, Selective, and Efficacious Phosphatidylinositol 3-Kinase δ (PI3Kδ) Inhibitor for the Treatment of Immunological Disorders
Journal of Medicinal Chemistry·2017· 22 citedOpen Access
Identification of imidazo[1,2-<i>b</i>]pyridazine TYK2 pseudokinase ligands as potent and selective allosteric inhibitors of TYK2 signalling
MedChemComm·2016· 48 citedOpen Access
Discovery of furo[2,3-d][1,3]thiazinamines as beta amyloid cleaving enzyme-1 (BACE1) inhibitors
Bioorganic & Medicinal Chemistry Letters·2016· 16 citedOpen Access
CRYSTAL STRUCTURE OF BETA-SITE APP-CLEAVING ENZYME 1 COMPLEXED WITH N-(3-((4AS,7AS)-2-AMINO-4,4A,5,6-TETRAHYDRO-7AH-FURO[2,3-D][1,3]THIAZIN-7A-YL)-4-FLUOROPHENYL)-5-BROMO-2-PYRIDINECARBOXAMIDE
2016
CRYSTAL STRUCTURE OF TYROSINE KINASE 2 JH2 (PSEUDO KINASE DOMAIN) COMPLEXED WITH 6-[(3,5-DIMETHYLPHE NYL)AMINO]-8- (METHYLAMINO)IMIDAZO[1,2-B]PYRIDAZINE-3-CARBO XAMIDE
2016
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Frequent Co-authors

Joseph A. Tino(12), James R. Burke(11), John E. Macor(10), ChiehYing Chang(9), Percy H. Carter(9), ChiehYing Y. Chang(9), Kim W. McIntyre(8), Andrew J. Tebben(8), Jonathan Lippy(8), Celia D’Arienzo(7), Kathleen M. Gillooly(7), Catherine R. Burton(7), Daniel M. Camac(7), Douglas G. Batt(6), Arvind Mathur(6), Luisa Salter–Cid(6), Aberra Fura(6), Jeremy H. Toyn(6), Charles F. Albright(6), Lorin A. Thompson(6)