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Discovery and optimization of a novel series of highly CNS penetrant M4 PAMs based on a 5,6-dimethyl-4-(piperidin-1-yl)thieno[2,3-d]pyrimidine core.
Wood MR, Noetzel MJ, Engers JL, Bollinger KA, Melancon BJ, Tarr JC, Han C, West M, Gregro AR, Lamsal A, Chang S, Ajmera S, Smith E, Chase P, Hodder PS, Bubser M, Jones CK, Hopkins CR, Emmitte KA, Niswender CM, Wood MW, Duggan ME, Conn PJ, Bridges TM, Lindsley CW. Wood MR, et al. Among authors: emmitte ka. Bioorg Med Chem Lett. 2016 Jul 1;26(13):3029-3033. doi: 10.1016/j.bmcl.2016.05.010. Epub 2016 May 5. Bioorg Med Chem Lett. 2016. PMID: 27185330 Free PMC article.
Discovery of thiophene inhibitors of polo-like kinase.
Emmitte KA, Andrews CW, Badiang JG, Davis-Ward RG, Dickson HD, Drewry DH, Emerson HK, Epperly AH, Hassler DF, Knick VB, Kuntz KW, Lansing TJ, Linn JA, Mook RA Jr, Nailor KE, Salovich JM, Spehar GM, Cheung M. Emmitte KA, et al. Bioorg Med Chem Lett. 2009 Feb 1;19(3):1018-21. doi: 10.1016/j.bmcl.2008.11.041. Epub 2008 Nov 18. Bioorg Med Chem Lett. 2009. PMID: 19097784
Discovery and optimization of imidazo[1,2-a]pyridine inhibitors of insulin-like growth factor-1 receptor (IGF-1R).
Emmitte KA, Wilson BJ, Baum EW, Emerson HK, Kuntz KW, Nailor KE, Salovich JM, Smith SC, Cheung M, Gerding RM, Stevens KL, Uehling DE, Mook RA Jr, Moorthy GS, Dickerson SH, Hassell AM, Leesnitzer MA, Shewchuk LM, Groy A, Rowand JL, Anderson K, Atkins CL, Yang J, Sabbatini P, Kumar R. Emmitte KA, et al. Bioorg Med Chem Lett. 2009 Feb 1;19(3):1004-8. doi: 10.1016/j.bmcl.2008.11.058. Epub 2008 Nov 20. Bioorg Med Chem Lett. 2009. PMID: 19101143
3-Cyano-5-fluoro-N-arylbenzamides as negative allosteric modulators of mGlu(5): Identification of easily prepared tool compounds with CNS exposure in rats.
Felts AS, Lindsley SR, Lamb JP, Rodriguez AL, Menon UN, Jadhav S, Jones CK, Conn PJ, Lindsley CW, Emmitte KA. Felts AS, et al. Among authors: emmitte ka. Bioorg Med Chem Lett. 2010 Aug 1;20(15):4390-4. doi: 10.1016/j.bmcl.2010.06.064. Epub 2010 Jun 15. Bioorg Med Chem Lett. 2010. PMID: 20598884 Free PMC article.
Discovery of 2-(2-benzoxazoyl amino)-4-aryl-5-cyanopyrimidine as negative allosteric modulators (NAMs) of metabotropic glutamate receptor 5 (mGlu₅): from an artificial neural network virtual screen to an in vivo tool compound.
Mueller R, Dawson ES, Meiler J, Rodriguez AL, Chauder BA, Bates BS, Felts AS, Lamb JP, Menon UN, Jadhav SB, Kane AS, Jones CK, Gregory KJ, Niswender CM, Conn PJ, Olsen CM, Winder DG, Emmitte KA, Lindsley CW. Mueller R, et al. Among authors: emmitte ka. ChemMedChem. 2012 Mar 5;7(3):406-14. doi: 10.1002/cmdc.201100510. Epub 2012 Jan 20. ChemMedChem. 2012. PMID: 22267125 Free PMC article. No abstract available.
64 results