150 related articles for article (PubMed ID: 27406798)
1. Lead optimization of a pyrazolo[1,5-a]pyrimidin-7(4H)-one scaffold to identify potent, selective and orally bioavailable KDM5 inhibitors suitable for in vivo biological studies.
Liang J; Zhang B; Labadie S; Ortwine DF; Vinogradova M; Kiefer JR; Gehling VS; Harmange JC; Cummings R; Lai T; Liao J; Zheng X; Liu Y; Gustafson A; Van der Porten E; Mao W; Liederer BM; Deshmukh G; Classon M; Trojer P; Dragovich PS; Murray L
Bioorg Med Chem Lett; 2016 Aug; 26(16):4036-41. PubMed ID: 27406798
[TBL] [Abstract][Full Text] [Related]
2. From a novel HTS hit to potent, selective, and orally bioavailable KDM5 inhibitors.
Liang J; Labadie S; Zhang B; Ortwine DF; Patel S; Vinogradova M; Kiefer JR; Mauer T; Gehling VS; Harmange JC; Cummings R; Lai T; Liao J; Zheng X; Liu Y; Gustafson A; Van der Porten E; Mao W; Liederer BM; Deshmukh G; An L; Ran Y; Classon M; Trojer P; Dragovich PS; Murray L
Bioorg Med Chem Lett; 2017 Jul; 27(13):2974-2981. PubMed ID: 28512031
[TBL] [Abstract][Full Text] [Related]
3. Identification of potent, selective KDM5 inhibitors.
Gehling VS; Bellon SF; Harmange JC; LeBlanc Y; Poy F; Odate S; Buker S; Lan F; Arora S; Williamson KE; Sandy P; Cummings RT; Bailey CM; Bergeron L; Mao W; Gustafson A; Liu Y; VanderPorten E; Audia JE; Trojer P; Albrecht BK
Bioorg Med Chem Lett; 2016 Sep; 26(17):4350-4. PubMed ID: 27476424
[TBL] [Abstract][Full Text] [Related]
4. Identification of novel lysine demethylase 5-selective inhibitors by inhibitor-based fragment merging strategy.
Miyake Y; Itoh Y; Hatanaka A; Suzuma Y; Suzuki M; Kodama H; Arai Y; Suzuki T
Bioorg Med Chem; 2019 Mar; 27(6):1119-1129. PubMed ID: 30745098
[TBL] [Abstract][Full Text] [Related]
5. Design and discovery of 6-[(3S,4S)-4-methyl-1-(pyrimidin-2-ylmethyl)pyrrolidin-3-yl]-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one (PF-04447943), a selective brain penetrant PDE9A inhibitor for the treatment of cognitive disorders.
Verhoest PR; Fonseca KR; Hou X; Proulx-Lafrance C; Corman M; Helal CJ; Claffey MM; Tuttle JB; Coffman KJ; Liu S; Nelson F; Kleiman RJ; Menniti FS; Schmidt CJ; Vanase-Frawley M; Liras S
J Med Chem; 2012 Nov; 55(21):9045-54. PubMed ID: 22780914
[TBL] [Abstract][Full Text] [Related]
6. Rapid hit to lead evaluation of pyrazolo[3,4-d]pyrimidin-4-one as selective and orally bioavailable mGluR1 antagonists.
Wang X; Kolasa T; El Kouhen OF; Chovan LE; Black-Shaefer CL; Wagenaar FL; Garton JA; Moreland RB; Honore P; Lau YY; Dandliker PJ; Brioni JD; Stewart AO
Bioorg Med Chem Lett; 2007 Aug; 17(15):4303-7. PubMed ID: 17532216
[TBL] [Abstract][Full Text] [Related]
7. Preparation of 1-(4-methoxyphenyl)-1H-pyrazolo[4,3-d]pyrimidin-7(6H)-ones as potent, selective and bioavailable inhibitors of coagulation factor Xa.
Fevig JM; Cacciola J; Buriak J; Rossi KA; Knabb RM; Luettgen JM; Wong PC; Bai SA; Wexler RR; Lam PY
Bioorg Med Chem Lett; 2006 Jul; 16(14):3755-60. PubMed ID: 16682200
[TBL] [Abstract][Full Text] [Related]
8. Design and synthesis of a novel pyrrolidinyl pyrido pyrimidinone derivative as a potent inhibitor of PI3Kα and mTOR.
Le PT; Cheng H; Ninkovic S; Plewe M; Huang X; Wang H; Bagrodia S; Sun S; Knighton DR; LaFleur Rogers CM; Pannifer A; Greasley S; Dalvie D; Zhang E
Bioorg Med Chem Lett; 2012 Aug; 22(15):5098-103. PubMed ID: 22749419
[TBL] [Abstract][Full Text] [Related]
9. 2-(2-Phenylmorpholin-4-yl)pyrimidin-4(3H)-ones; a new class of potent, selective and orally active glycogen synthase kinase-3β inhibitors.
Fukunaga K; Uehara F; Aritomo K; Shoda A; Hiki S; Okuyama M; Usui Y; Watanabe K; Yamakoshi K; Kohara T; Hanano T; Tanaka H; Tsuchiya S; Sunada S; Saito K; Eguchi J; Yuki S; Asano S; Tanaka S; Mori A; Yamagami K; Baba H; Horikawa T; Fujimura M
Bioorg Med Chem Lett; 2013 Dec; 23(24):6933-7. PubMed ID: 24176395
[TBL] [Abstract][Full Text] [Related]
10. Potent and selective Bruton's tyrosine kinase inhibitors: discovery of GDC-0834.
Young WB; Barbosa J; Blomgren P; Bremer MC; Crawford JJ; Dambach D; Gallion S; Hymowitz SG; Kropf JE; Lee SH; Liu L; Lubach JW; Macaluso J; Maciejewski P; Maurer B; Mitchell SA; Ortwine DF; Di Paolo J; Reif K; Scheerens H; Schmitt A; Sowell CG; Wang X; Wong H; Xiong JM; Xu J; Zhao Z; Currie KS
Bioorg Med Chem Lett; 2015 Mar; 25(6):1333-7. PubMed ID: 25701252
[TBL] [Abstract][Full Text] [Related]
11. Structure-based design and discovery of potent and selective KDM5 inhibitors.
Nie Z; Shi L; Lai C; O'Connell SM; Xu J; Stansfield RK; Hosfield DJ; Veal JM; Stafford JA
Bioorg Med Chem Lett; 2018 May; 28(9):1490-1494. PubMed ID: 29627262
[TBL] [Abstract][Full Text] [Related]
12. The KDM5 family of histone demethylases as targets in oncology drug discovery.
Rasmussen PB; Staller P
Epigenomics; 2014 Jun; 6(3):277-86. PubMed ID: 25111482
[TBL] [Abstract][Full Text] [Related]
13. Design and evaluation of 1,7-naphthyridones as novel KDM5 inhibitors.
Labadie SS; Dragovich PS; Cummings RT; Deshmukh G; Gustafson A; Han N; Harmange JC; Kiefer JR; Li Y; Liang J; Liederer BM; Liu Y; Manieri W; Mao W; Murray L; Ortwine DF; Trojer P; VanderPorten E; Vinogradova M; Wen L
Bioorg Med Chem Lett; 2016 Sep; 26(18):4492-4496. PubMed ID: 27499454
[TBL] [Abstract][Full Text] [Related]
14. Cell Penetrant Inhibitors of the KDM4 and KDM5 Families of Histone Lysine Demethylases. 2. Pyrido[3,4-d]pyrimidin-4(3H)-one Derivatives.
Westaway SM; Preston AG; Barker MD; Brown F; Brown JA; Campbell M; Chung CW; Drewes G; Eagle R; Garton N; Gordon L; Haslam C; Hayhow TG; Humphreys PG; Joberty G; Katso R; Kruidenier L; Leveridge M; Pemberton M; Rioja I; Seal GA; Shipley T; Singh O; Suckling CJ; Taylor J; Thomas P; Wilson DM; Lee K; Prinjha RK
J Med Chem; 2016 Feb; 59(4):1370-87. PubMed ID: 26771203
[TBL] [Abstract][Full Text] [Related]
15. Application of structure-based drug design and parallel chemistry to identify selective, brain penetrant, in vivo active phosphodiesterase 9A inhibitors.
Claffey MM; Helal CJ; Verhoest PR; Kang Z; Fors KS; Jung S; Zhong J; Bundesmann MW; Hou X; Lui S; Kleiman RJ; Vanase-Frawley M; Schmidt AW; Menniti F; Schmidt CJ; Hoffman WE; Hajos M; McDowell L; O'Connor RE; Macdougall-Murphy M; Fonseca KR; Becker SL; Nelson FR; Liras S
J Med Chem; 2012 Nov; 55(21):9055-68. PubMed ID: 23025719
[TBL] [Abstract][Full Text] [Related]
16. Lead optimization of a 4-aminopyridine benzamide scaffold to identify potent, selective, and orally bioavailable TYK2 inhibitors.
Liang J; van Abbema A; Balazs M; Barrett K; Berezhkovsky L; Blair W; Chang C; Delarosa D; DeVoss J; Driscoll J; Eigenbrot C; Ghilardi N; Gibbons P; Halladay J; Johnson A; Kohli PB; Lai Y; Liu Y; Lyssikatos J; Mantik P; Menghrajani K; Murray J; Peng I; Sambrone A; Shia S; Shin Y; Smith J; Sohn S; Tsui V; Ultsch M; Wu LC; Xiao Y; Yang W; Young J; Zhang B; Zhu BY; Magnuson S
J Med Chem; 2013 Jun; 56(11):4521-36. PubMed ID: 23668484
[TBL] [Abstract][Full Text] [Related]
17. Potent and Selective KDM5 Inhibitor Stops Cellular Demethylation of H3K4me3 at Transcription Start Sites and Proliferation of MM1S Myeloma Cells.
Tumber A; Nuzzi A; Hookway ES; Hatch SB; Velupillai S; Johansson C; Kawamura A; Savitsky P; Yapp C; Szykowska A; Wu N; Bountra C; Strain-Damerell C; Burgess-Brown NA; Ruda GF; Fedorov O; Munro S; England KS; Nowak RP; Schofield CJ; La Thangue NB; Pawlyn C; Davies F; Morgan G; Athanasou N; Müller S; Oppermann U; Brennan PE
Cell Chem Biol; 2017 Mar; 24(3):371-380. PubMed ID: 28262558
[TBL] [Abstract][Full Text] [Related]
18. The Discovery of in Vivo Active Mitochondrial Branched-Chain Aminotransferase (BCATm) Inhibitors by Hybridizing Fragment and HTS Hits.
Bertrand SM; Ancellin N; Beaufils B; Bingham RP; Borthwick JA; Boullay AB; Boursier E; Carter PS; Chung CW; Churcher I; Dodic N; Fouchet MH; Fournier C; Francis PL; Gummer LA; Herry K; Hobbs A; Hobbs CI; Homes P; Jamieson C; Nicodeme E; Pickett SD; Reid IH; Simpson GL; Sloan LA; Smith SE; Somers DO; Spitzfaden C; Suckling CJ; Valko K; Washio Y; Young RJ
J Med Chem; 2015 Sep; 58(18):7140-63. PubMed ID: 26090771
[TBL] [Abstract][Full Text] [Related]
19. Discovery and optimization of pyrimidone indoline amide PI3Kβ inhibitors for the treatment of phosphatase and tensin homologue (PTEN)-deficient cancers.
Certal V; Carry JC; Halley F; Virone-Oddos A; Thompson F; Filoche-Rommé B; El-Ahmad Y; Karlsson A; Charrier V; Delorme C; Rak A; Abecassis PY; Amara C; Vincent L; Bonnevaux H; Nicolas JP; Mathieu M; Bertrand T; Marquette JP; Michot N; Benard T; Perrin MA; Lemaitre O; Guerif S; Perron S; Monget S; Gruss-Leleu F; Doerflinger G; Guizani H; Brollo M; Delbarre L; Bertin L; Richepin P; Loyau V; Garcia-Echeverria C; Lengauer C; Schio L
J Med Chem; 2014 Feb; 57(3):903-20. PubMed ID: 24387221
[TBL] [Abstract][Full Text] [Related]
20. Discovery of chiral dihydropyridopyrimidinones as potent, selective and orally bioavailable inhibitors of AKT.
Parthasarathy S; Henry K; Pei H; Clayton J; Rempala M; Johns D; De Frutos O; Garcia P; Mateos C; Pleite S; Wang Y; Stout S; Condon B; Ashok S; Lu Z; Ehlhardt W; Raub T; Lai M; Geeganage S; Burkholder TP
Bioorg Med Chem Lett; 2018 Jun; 28(10):1887-1891. PubMed ID: 29655979
[TBL] [Abstract][Full Text] [Related]
[Next] [New Search]
