Zobrazeno 1 - 2
of 2
pro vyhledávání: '"Kishore Renduchintala"'
Autor:
Neil Flynn, Mary Jane Cullen, Hongwei Zhang, Wei Wang, Susan Glick, Lisa Zhang, Jeffrey A. Robl, Pratik Devasthale, Andres S. Hernandez, Christian Caporuscio, Brian J. Murphy, Suzanne Rooney, Ning Huang, Mary Ann Pelleymounter, Kenneth W. Rohrbach, Kishore Renduchintala, Anthony V. Azzara, Helen E. Godonis, Yi-Xin Li, Radhakrishnan Sridhar, Michael Thomas, Susan Harvey, Paul Stetsko, Mary F. Grubb, Chris Freeden, Fang Moore, Christine Huang, James Devenny, Daniel Longhi, William N. Washburn
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 25:2793-2799
Our investigation of the structure–activity and structure–liability relationships for dihydropyrrolopyrazol-6-one MCHR1 antagonists revealed that off-rate characteristics, inferred from potencies in a FLIPR assay following a 2 h incubation, can i
Autor:
Brian J. Murphy, James Devenny, Suzanne Rooney, Jagannath Selvaraj, James Mignone, Susan Glick, Sridhar Radhakrishnan, Helen E. Godonis, Neil Flynn, Rajesh Kuppusamy, Jayanthi Dhanapal, Mary Ann Pelleymounter, Chris Freeden, Pratik Devasthale, Daniel Longhi, William N. Washburn, Ning Huang, Christian Caporuscio, Mary F. Grubb, Paul Stetsko, Kenneth W. Rohrbach, Mary Jane Cullen, Christine Huang, Wei Wang, Susan Harvey, Hongwei Zhang, Lisa Zhang, Michael Thomas, Jeffrey A. Robl, Kishore Renduchintala, Anthony V. Azzara
Publikováno v:
Bioorganicmedicinal chemistry letters. 25(20)
Non-basic azolotriazinones were explored using an empirical free brain exposures-driven approach to identify potent MCHR1 antagonists for evaluation in in vivo efficacy studies. An optimized lead from this series, 1j (rMCHR1 Ki=1.8 nM), demonstrated