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Discovery of lirafugratinib (RLY-4008), a highly selective irreversible small-molecule inhibitor of FGFR2.
Proc Natl Acad Sci U S A. 2024 Feb 6;121(6):e2317756121. doi: 10.1073/pnas.2317756121. Epub 2024 Feb 1.
Proc Natl Acad Sci U S A. 2024.
PMID: 38300868
Free PMC article.
Discovery and Clinical Proof-of-Concept of RLY-2608, a First-in-Class Mutant-Selective Allosteric PI3Kα Inhibitor That Decouples Antitumor Activity from Hyperinsulinemia.
Varkaris A, Pazolli E, Gunaydin H, Wang Q, Pierce L, Boezio AA, Bulku A, DiPietro L, Fridrich C, Frost A, Giordanetto F, Hamilton EP, Harris K, Holliday M, Hunter TL, Iskandar A, Ji Y, Larivée A, LaRochelle JR, Lescarbeau A, Llambi F, Lormil B, Mader MM, Mar BG, Martin I, McLean TH, Michelsen K, Pechersky Y, Puente-Poushnejad E, Raynor K, Rogala D, Samadani R, Schram AM, Shortsleeves K, Swaminathan S, Tajmir S, Tan G, Tang Y, Valverde R, Wehrenberg B, Wilbur J, Williams BR, Zeng H, Zhang H, Walters WP, Wolf BB, Shaw DE, Bergstrom DA, Watters J, Fraser JS, Fortin PD, Kipp DR.
Varkaris A, et al. Among authors: mclean th.
Cancer Discov. 2024 Feb 8;14(2):240-257. doi: 10.1158/2159-8290.CD-23-0944.
Cancer Discov. 2024.
PMID: 37916956
Free PMC article.
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Human HDAC7 harbors a class IIa histone deacetylase-specific zinc binding motif and cryptic deacetylase activity.
Schuetz A, Min J, Allali-Hassani A, Schapira M, Shuen M, Loppnau P, Mazitschek R, Kwiatkowski NP, Lewis TA, Maglathin RL, McLean TH, Bochkarev A, Plotnikov AN, Vedadi M, Arrowsmith CH.
Schuetz A, et al. Among authors: mclean th.
J Biol Chem. 2008 Apr 25;283(17):11355-63. doi: 10.1074/jbc.M707362200. Epub 2008 Feb 19.
J Biol Chem. 2008.
PMID: 18285338
Free PMC article.
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1-Aminomethylbenzocycloalkanes: conformationally restricted hallucinogenic phenethylamine analogues as functionally selective 5-HT2A receptor agonists.
McLean TH, Parrish JC, Braden MR, Marona-Lewicka D, Gallardo-Godoy A, Nichols DE.
McLean TH, et al.
J Med Chem. 2006 Sep 21;49(19):5794-803. doi: 10.1021/jm060656o.
J Med Chem. 2006.
PMID: 16970404
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C-(4,5,6-trimethoxyindan-1-yl)methanamine: a mescaline analogue designed using a homology model of the 5-HT2A receptor.
McLean TH, Chambers JJ, Parrish JC, Braden MR, Marona-Lewicka D, Kurrasch-Orbaugh D, Nichols DE.
McLean TH, et al.
J Med Chem. 2006 Jul 13;49(14):4269-74. doi: 10.1021/jm060272y.
J Med Chem. 2006.
PMID: 16821786
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Sulfur-substituted alpha-alkyl phenethylamines as selective and reversible MAO-A inhibitors: biological activities, CoMFA analysis, and active site modeling.
Gallardo-Godoy A, Fierro A, McLean TH, Castillo M, Cassels BK, Reyes-Parada M, Nichols DE.
Gallardo-Godoy A, et al. Among authors: mclean th.
J Med Chem. 2005 Apr 7;48(7):2407-19. doi: 10.1021/jm0493109.
J Med Chem. 2005.
PMID: 15801832
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Blockade of neuronal sodium channels by the antiepileptic drugs phenytoin, carbamazepine and sodium valproate.
Pugsley MK, Yu EJ, Mclean TH, Goldin AL.
Pugsley MK, et al. Among authors: mclean th.
Proc West Pharmacol Soc. 1999;42:105-8.
Proc West Pharmacol Soc. 1999.
PMID: 10697707
No abstract available.
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