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332 related items for PubMed ID: 30893553
1. Discovery of Branebrutinib (BMS-986195): A Strategy for Identifying a Highly Potent and Selective Covalent Inhibitor Providing Rapid in Vivo Inactivation of Bruton's Tyrosine Kinase (BTK). Watterson SH, Liu Q, Beaudoin Bertrand M, Batt DG, Li L, Pattoli MA, Skala S, Cheng L, Obermeier MT, Moore R, Yang Z, Vickery R, Elzinga PA, Discenza L, D'Arienzo C, Gillooly KM, Taylor TL, Pulicicchio C, Zhang Y, Heimrich E, McIntyre KW, Ruan Q, Westhouse RA, Catlett IM, Zheng N, Chaudhry C, Dai J, Galella MA, Tebben AJ, Pokross M, Li J, Zhao R, Smith D, Rampulla R, Allentoff A, Wallace MA, Mathur A, Salter-Cid L, Macor JE, Carter PH, Fura A, Burke JR, Tino JA. J Med Chem; 2019 Apr 11; 62(7):3228-3250. PubMed ID: 30893553 [Abstract] [Full Text] [Related]
2. Safety, pharmacokinetics and pharmacodynamics of branebrutinib (BMS-986195), a covalent, irreversible inhibitor of Bruton's tyrosine kinase: Randomised phase I, placebo-controlled trial in healthy participants. Catlett IM, Nowak M, Kundu S, Zheng N, Liu A, He B, Girgis IG, Grasela DM. Br J Clin Pharmacol; 2020 Sep 11; 86(9):1849-1859. PubMed ID: 32198939 [Abstract] [Full Text] [Related]
4. Discovery of 6-Fluoro-5-(R)-(3-(S)-(8-fluoro-1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)-2-methylphenyl)-2-(S)-(2-hydroxypropan-2-yl)-2,3,4,9-tetrahydro-1H-carbazole-8-carboxamide (BMS-986142): A Reversible Inhibitor of Bruton's Tyrosine Kinase (BTK) Conformationally Constrained by Two Locked Atropisomers. Watterson SH, De Lucca GV, Shi Q, Langevine CM, Liu Q, Batt DG, Beaudoin Bertrand M, Gong H, Dai J, Yip S, Li P, Sun D, Wu DR, Wang C, Zhang Y, Traeger SC, Pattoli MA, Skala S, Cheng L, Obermeier MT, Vickery R, Discenza LN, D'Arienzo CJ, Zhang Y, Heimrich E, Gillooly KM, Taylor TL, Pulicicchio C, McIntyre KW, Galella MA, Tebben AJ, Muckelbauer JK, Chang C, Rampulla R, Mathur A, Salter-Cid L, Barrish JC, Carter PH, Fura A, Burke JR, Tino JA. J Med Chem; 2016 Oct 13; 59(19):9173-9200. PubMed ID: 27583770 [Abstract] [Full Text] [Related]
5. Discovery of Evobrutinib: An Oral, Potent, and Highly Selective, Covalent Bruton's Tyrosine Kinase (BTK) Inhibitor for the Treatment of Immunological Diseases. Caldwell RD, Qiu H, Askew BC, Bender AT, Brugger N, Camps M, Dhanabal M, Dutt V, Eichhorn T, Gardberg AS, Goutopoulos A, Grenningloh R, Head J, Healey B, Hodous BL, Huck BR, Johnson TL, Jones C, Jones RC, Mochalkin I, Morandi F, Nguyen N, Meyring M, Potnick JR, Santos DC, Schmidt R, Sherer B, Shutes A, Urbahns K, Follis AV, Wegener AA, Zimmerli SC, Liu-Bujalski L. J Med Chem; 2019 Sep 12; 62(17):7643-7655. PubMed ID: 31368705 [Abstract] [Full Text] [Related]
6. Discovery of GDC-0853: A Potent, Selective, and Noncovalent Bruton's Tyrosine Kinase Inhibitor in Early Clinical Development. Crawford JJ, Johnson AR, Misner DL, Belmont LD, Castanedo G, Choy R, Coraggio M, Dong L, Eigenbrot C, Erickson R, Ghilardi N, Hau J, Katewa A, Kohli PB, Lee W, Lubach JW, McKenzie BS, Ortwine DF, Schutt L, Tay S, Wei B, Reif K, Liu L, Wong H, Young WB. J Med Chem; 2018 Mar 22; 61(6):2227-2245. PubMed ID: 29457982 [Abstract] [Full Text] [Related]
7. Discovery of Zanubrutinib (BGB-3111), a Novel, Potent, and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase. Guo Y, Liu Y, Hu N, Yu D, Zhou C, Shi G, Zhang B, Wei M, Liu J, Luo L, Tang Z, Song H, Guo Y, Liu X, Su D, Zhang S, Song X, Zhou X, Hong Y, Chen S, Cheng Z, Young S, Wei Q, Wang H, Wang Q, Lv L, Wang F, Xu H, Sun H, Xing H, Li N, Zhang W, Wang Z, Liu G, Sun Z, Zhou D, Li W, Liu L, Wang L, Wang Z. J Med Chem; 2019 Sep 12; 62(17):7923-7940. PubMed ID: 31381333 [Abstract] [Full Text] [Related]
8. Targeting Bruton's tyrosine kinase (BTK) as a signaling pathway in immune-mediated diseases: from molecular mechanisms to leading treatments. Tavakoli GM, Yazdanpanah N, Rezaei N. Adv Rheumatol; 2024 Aug 21; 64(1):61. PubMed ID: 39169436 [Abstract] [Full Text] [Related]
9. Discovery of 5-Phenoxy-2-aminopyridine Derivatives as Potent and Selective Irreversible Inhibitors of Bruton's Tyrosine Kinase. Lee E, Cho H, Lee DK, Ha J, Choi BJ, Jeong JH, Ryu JH, Kang JS, Jeon R. Int J Mol Sci; 2020 Oct 28; 21(21):. PubMed ID: 33126415 [Abstract] [Full Text] [Related]
10. Discovery of potent, highly selective covalent irreversible BTK inhibitors from a fragment hit. Qiu H, Liu-Bujalski L, Caldwell RD, Follis AV, Gardberg A, Goutopoulos A, Grenningloh R, Head J, Johnson T, Jones R, Mochalkin I, Morandi F, Neagu C, Sherer B. Bioorg Med Chem Lett; 2018 Sep 15; 28(17):2939-2944. PubMed ID: 30122225 [Abstract] [Full Text] [Related]
11. ZYBT1, a potent, irreversible Bruton's Tyrosine Kinase (BTK) inhibitor that inhibits the C481S BTK with profound efficacy against arthritis and cancer. Ghoshdastidar K, Patel H, Bhayani H, Patel A, Thakkar K, Patel D, Sharma M, Singh J, Mohapatra J, Chatterjee A, Patel D, Bahekar R, Sharma R, Gupta L, Patel N, Giri P, Srinivas NR, Jain M, Bandyopadhyay D, Patel PR, Desai RC. Pharmacol Res Perspect; 2020 Aug 15; 8(4):e00565. PubMed ID: 32790160 [Abstract] [Full Text] [Related]
12. Discovery of potent and selective reversible Bruton's tyrosine kinase inhibitors. Qiu H, Ali Z, Bender A, Caldwell R, Chen YY, Fang Z, Gardberg A, Glaser N, Goettsche A, Goutopoulos A, Grenningloh R, Hanschke B, Head J, Johnson T, Jones C, Jones R, Kulkarni S, Maurer C, Morandi F, Neagu C, Poetzsch S, Potnick J, Schmidt R, Roe K, Viacava Follis A, Wing C, Zhu X, Sherer B. Bioorg Med Chem; 2021 Jun 15; 40():116163. PubMed ID: 33932711 [Abstract] [Full Text] [Related]
13. Bruton's Tyrosine Kinase (BTK) Inhibitors and Autoimmune Diseases: Making Sense of BTK Inhibitor Specificity Profiles and Recent Clinical Trial Successes and Failures. Ringheim GE, Wampole M, Oberoi K. Front Immunol; 2021 Jun 15; 12():662223. PubMed ID: 34803999 [Abstract] [Full Text] [Related]
14. HZ-A-005, a potent, selective, and covalent Bruton's tyrosine kinase inhibitor in preclinical development. Huang W, Wang S, Zhang Z, Zhang C, Zeng S, Liang M, Shen Z, Liu X. Bioorg Chem; 2020 Dec 15; 105():104377. PubMed ID: 33091668 [Abstract] [Full Text] [Related]
15. Utilizing structure based drug design and metabolic soft spot identification to optimize the in vitro potency and in vivo pharmacokinetic properties leading to the discovery of novel reversible Bruton's tyrosine kinase inhibitors. Hopkins BT, Bame E, Bell N, Bohnert T, Bowden-Verhoek JK, Bui M, Cancilla MT, Conlon P, Cullen P, Erlanson DA, Fan J, Fuchs-Knotts T, Hansen S, Heumann S, Jenkins TJ, Gua C, Liu Y, Liu Y, Lulla M, Marcotte D, Marx I, McDowell B, Mertsching E, Negrou E, Romanowski MJ, Scott D, Silvian L, Yang W, Zhong M. Bioorg Med Chem; 2021 Aug 15; 44():116275. PubMed ID: 34314938 [Abstract] [Full Text] [Related]
16. Biochemical characterization of tirabrutinib and other irreversible inhibitors of Bruton's tyrosine kinase reveals differences in on - and off - target inhibition. Liclican A, Serafini L, Xing W, Czerwieniec G, Steiner B, Wang T, Brendza KM, Lutz JD, Keegan KS, Ray AS, Schultz BE, Sakowicz R, Feng JY. Biochim Biophys Acta Gen Subj; 2020 Apr 15; 1864(4):129531. PubMed ID: 31953125 [Abstract] [Full Text] [Related]
18. Discovery of LOU064 (Remibrutinib), a Potent and Highly Selective Covalent Inhibitor of Bruton's Tyrosine Kinase. Angst D, Gessier F, Janser P, Vulpetti A, Wälchli R, Beerli C, Littlewood-Evans A, Dawson J, Nuesslein-Hildesheim B, Wieczorek G, Gutmann S, Scheufler C, Hinniger A, Zimmerlin A, Funhoff EG, Pulz R, Cenni B. J Med Chem; 2020 May 28; 63(10):5102-5118. PubMed ID: 32083858 [Abstract] [Full Text] [Related]
19. Discovery and biological evaluation of N-(3-(7-((2-methoxy-4-(4-methylpiperazin-1-yl)phenyl)amino)-4-methyl-2-oxo-2H-pyrimido[4,5-d][1,3]oxazin-1(4H)-yl)phenyl)acrylamide as potent Bruton's tyrosine kinase inhibitors. Lai MZ, Song PR, Dou D, Diao YY, Tong LJ, Zhang T, Xie H, Li HL, Ding J. Acta Pharmacol Sin; 2020 Mar 28; 41(3):415-422. PubMed ID: 31316181 [Abstract] [Full Text] [Related]
20. Discovery of potent and highly selective covalent inhibitors of Bruton's tyrosine kinase bearing triazine scaffold. Teng Y, Lu X, Xiao M, Li Z, Zou Y, Ren S, Cheng Y, Luo G, Xiang H. Eur J Med Chem; 2020 Aug 01; 199():112339. PubMed ID: 32402933 [Abstract] [Full Text] [Related] Page: [Next] [New Search]