Kenakin T - Search Results

1

Novel 4,4-disubstituted piperidine-based C-C chemokine receptor-5 inhibitors with high potency against human immunodeficiency virus-1 and an improved human ether-a-go-go related gene (hERG) profile.

Kazmierski WM, Anderson DL, Aquino C, Chauder BA, Duan M, Ferris R, Kenakin T, Koble CS, Lang DG, McIntyre MS, Peckham J, Watson C, Wheelan P, Spaltenstein A, Wire MB, Svolto A, Youngman M. Kazmierski WM, et al. Among authors: kenakin t. J Med Chem. 2011 Jun 9;54(11):3756-67. doi: 10.1021/jm200279v. Epub 2011 May 17. J Med Chem. 2011. PMID: 21539377

2

Discovery of bioavailable 4,4-disubstituted piperidines as potent ligands of the chemokine receptor 5 and inhibitors of the human immunodeficiency virus-1.

Kazmierski WM, Aquino C, Chauder BA, Deanda F, Ferris R, Jones-Hertzog DK, Kenakin T, Koble CS, Watson C, Wheelan P, Yang H, Youngman M. Kazmierski WM, et al. Among authors: kenakin t. J Med Chem. 2008 Oct 23;51(20):6538-46. doi: 10.1021/jm800598a. Epub 2008 Sep 24. J Med Chem. 2008. PMID: 18811134

3

Discovery of the Potent and Selective M1 PAM-Agonist N-[(3R,4S)-3-Hydroxytetrahydro-2H-pyran-4-yl]-5-methyl-4-[4-(1,3-thiazol-4-yl)benzyl]pyridine-2-carboxamide (PF-06767832): Evaluation of Efficacy and Cholinergic Side Effects.

Davoren JE, Lee CW, Garnsey M, Brodney MA, Cordes J, Dlugolenski K, Edgerton JR, Harris AR, Helal CJ, Jenkinson S, Kauffman GW, Kenakin TP, Lazzaro JT, Lotarski SM, Mao Y, Nason DM, Northcott C, Nottebaum L, O'Neil SV, Pettersen B, Popiolek M, Reinhart V, Salomon-Ferrer R, Steyn SJ, Webb D, Zhang L, Grimwood S. Davoren JE, et al. Among authors: kenakin tp. J Med Chem. 2016 Jul 14;59(13):6313-28. doi: 10.1021/acs.jmedchem.6b00544. Epub 2016 Jul 1. J Med Chem. 2016. PMID: 27275946

4

Enantiospecific Allosteric Modulation of Cannabinoid 1 Receptor.

Laprairie RB, Kulkarni PM, Deschamps JR, Kelly MEM, Janero DR, Cascio MG, Stevenson LA, Pertwee RG, Kenakin TP, Denovan-Wright EM, Thakur GA. Laprairie RB, et al. ACS Chem Neurosci. 2017 Jun 21;8(6):1188-1203. doi: 10.1021/acschemneuro.6b00310. Epub 2017 Feb 7. ACS Chem Neurosci. 2017. PMID: 28103441

5

Identification of the first biased NPS receptor agonist that retains anxiolytic and memory promoting effects with reduced levels of locomotor stimulation.

Clark SD, Kenakin TP, Gertz S, Hassler C, Gay EA, Langston TL, Reinscheid RK, Runyon SP. Clark SD, et al. Neuropharmacology. 2017 May 15;118:69-78. doi: 10.1016/j.neuropharm.2017.03.001. Epub 2017 Mar 3. Neuropharmacology. 2017. PMID: 28267583 Free PMC article.

6

Differential Roles of Extracellular Histidine Residues of GPR68 for Proton-Sensing and Allosteric Modulation by Divalent Metal Ions.

Huang XP, Kenakin TP, Gu S, Shoichet BK, Roth BL. Huang XP, et al. Biochemistry. 2020 Sep 29;59(38):3594-3614. doi: 10.1021/acs.biochem.0c00576. Epub 2020 Sep 10. Biochemistry. 2020. PMID: 32865988 Free PMC article.

7

Human native kappa opioid receptor functions not predicted by recombinant receptors: Implications for drug design.

Broad J, Maurel D, Kung VW, Hicks GA, Schemann M, Barnes MR, Kenakin TP, Granier S, Sanger GJ. Broad J, et al. Sci Rep. 2016 Aug 5;6:30797. doi: 10.1038/srep30797. Sci Rep. 2016. PMID: 27492592 Free PMC article.

8

Characterization of the various functional pathways elicited by synthetic agonists or antagonists at the melatonin MT₁ and MT₂ receptors.

Legros C, Dupré C, Brasseur C, Bonnaud A, Bruno O, Valour D, Shabajee P, Giganti A, Nosjean O, Kenakin TP, Boutin JA. Legros C, et al. Pharmacol Res Perspect. 2019 Dec 29;8(1):e00539. doi: 10.1002/prp2.539. eCollection 2020 Feb. Pharmacol Res Perspect. 2019. PMID: 31893123 Free PMC article.

9

Know your molecule: pharmacological characterization of drug candidates to enhance efficacy and reduce late-stage attrition.

Kenakin T. Kenakin T. Nat Rev Drug Discov. 2024 Aug;23(8):626-644. doi: 10.1038/s41573-024-00958-9. Epub 2024 Jun 18. Nat Rev Drug Discov. 2024. PMID: 38890494 Review.

10

A Pharmacological perspective on the temporal properties of sweeteners.

Servant G, Kenakin T. Servant G, et al. Among authors: kenakin t. Pharmacol Res. 2024 Jun;204:107211. doi: 10.1016/j.phrs.2024.107211. Epub 2024 May 12. Pharmacol Res. 2024. PMID: 38744400 Free article.

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