| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
|
Ab102223-10μl (试用装) 申请此免费试用装（?） 作为尊贵的客户，您每年可免费申请三次您选择的不同货号试用装产品，尽享探索与享受！
|
10μl |
期货  |
| |
|
Ab102223-50μl |
50μL |
现货 |
| |
|
Ab102223-100μl |
100μL |
现货 |
| |
|
Ab102223-1ml |
1ml |
期货 |
|
| 产品名称 | Recombinant ERK1 Antibody |
|---|---|
| 别名 | ERK1抗体 | ERK1兔抗体 | ERK1单克隆抗体 | 重组ERK1抗体 | 兔抗人ERK1抗体 | 兔抗人ERK1重组抗体 | 重组兔抗人ERK1抗体 | 丝裂原活化蛋白激酶1抗体 | 丝裂原活化蛋白激酶1单克隆抗体 | 细胞外信号调节激酶1(ERK1)单克隆抗体 |
| 规格或纯度 | Recombinant (RR671); Rabbit anti Human ERK1 Antibody; WB, IHC, Flow, IF/ICC, IP; Unconjugated |
| 宿主 | Rabbit |
| 特异性 | MAPK3 |
| 应用 | WB,Flow,IF,ICC,IHC,IP |
| 反应种属 | Human,Mouse?,Rat? |
| 交叉反应 | Cross-reactivity with other species has not been measured. |
| 免疫原 | A synthetic peptide corresponding to the N-term of ERK1 was used as an immunogen. |
| 阳性对照 | WB: HeLa, A431, NIH/3T3, Jurkat and K562 cell lysates. IHC: Cervix cancer tissue. Flow: HeLa cells. ICC/IF: HeLa cells. IP: A375 whole cell lysate. |
| 偶联标记 | Unconjugated |
| 抗体类型 | Primary antibody |
|---|---|
| 克隆 | Recombinant |
| 克隆号 | RR671 |
| Format | Whole IgG |
| 亚型 | Rabbit IgG |
| SDS-PAGE | 150 kDa |
| 纯化方法 | Protein A purified |
| 来源 | CHO supernatant |
| 物理外观 | Liquid |
| 储存缓冲液 | 1*PBS 59%, Sodium azide 0.01%, Glycerol 40%, BSA 0.05%, pH7.3. |
| 防腐剂 | 0.01% Sodium azide |
| 浓度 | 2mg/mL |
| 储存温度 | -20°C储存,避免反复冻融 |
| 运输条件 | 超低温冰袋运输 |
| 稳定性与储存 | Store at -20°C for 2 years. Upon delivery aliquot. Avoid freeze/thaw cycle. |
| Application | Notes |
|---|---|
| WB |
1/2,000-1/10,0000
|
| IHC | 1/100 - 1/200 |
| IF/ICC | 1/50 – 1/200 |
| IP |
1/50
|
| Flow |
1/200 - 1/1000
|
Recombinant ERK1 Antibody (Ab102223) - Western Blot
All lanes: Recombinant ERK1 Antibody (Ab102223) at 1/1000 dilution
Samples: Lysates at 20 μg per lane
Secondary: Goat Anti-Rabbit IgG H&L (HRP) (Ab170144) at 1/30000 dilution
Predicted band size: 43 kDa
Observed band size: 40 kDa
Exposure time: 27.0 s
Recombinant ERK1 Antibody (Ab102223) - IF/ICC
Recombinant ERK1 Antibody (Ab102223) staining ERK1 in HeLa cells by IF/ICC (immunofluorescence/immunocytochemistry). Cells were fixed with paraformaldehyde, permeabilized with 0.1% Triton X-100 and blocked with 10% goat serum for half an hour at room temperature. Samples were incubated with Recombinant ERK1 Antibody (Ab102223) (1/50) at 4°C. An Alexa Fluor? 488-conjugatedGoat Anti-Rabbit IgG polyclonal was used as the secondary antibody (1/500). DAPI (blue) was used as the nuclear counter stain.
Control: PBS and secondary antibody, An Alexa Fluor? 488-conjugatedGoat Anti-Rabbit IgG (1/500).
Recombinant ERK1 Antibody (Ab102223) - Flow Cytometry
Overlay histogram showing HeLa cells stained with Recombinant ERK1 Antibody (Ab102223) (Red). The cells were fixed with 4% paraformaldehyde (10 min) and then permeabilized with 0.1% TritonX-100 for 15 min. The cells were then incubated in the Recombinant ERK1 Antibody (Ab102223) (1/1000 dilution) in 1x PBS/1% BSA for 30 min at room temperature. The secondary antibody was used a Goat Anti-Rabbit Alexa Fluor? 488 (IgG H+L) at 1/2000 dilution for 20 min at room temperature. Unlabeled sample (Black) was used as a control.
Recombinant ERK1 Antibody (Ab102223) - IP
ERK1 was immunoprecipitated from 0.4 mg of A375 whole cell lysate with Recombinant ERK1 Antibody (Ab102223) at 1/50 dilution
2nd Ab: GAR HRP for IP 1/500
Lane 1: Recombinant ERK1 Antibody (Ab102223) IP in A375 whole cell lysate
Lane 2: PBS instead of Recombinant ERK1 Antibody (Ab102223) in A375 whole cell lysate
Lane 3: A375 whole cell lysate, 10 μg (input)
Exposure: 120.0 s.
Recombinant ERK1 Antibody (Ab102223) - IHC
Immunohistochemistry (Formalin/PFA-fixed paraffin-embedded
sections) analysis Cervix cancer tissue labelling ERK1 with Recombinant ERK1 Antibody (Ab102223) at 1:200. Heat mediated antigen retrieval was performed using Tris/EDTA buffer pH 9.0.
| 1. Dumas J, Hatoum-Mokdad H, Sibley RN, Smith RA, Scott WJ, Khire U, Lee W, Wood J, Wolanin D, Cooley J, Bankston D, Redman AM, Schoenleber R, Caringal Y, Gunn D, Romero R, Osterhout M, Paulsen H, Housley TJ, Wilhelm SM, Pirro J, Chien DS, Ranges GE, Shrikhande A, Muzsi A, Bortolon E, Wakefield J, Gianpaolo Ostravage C, Bhargava A, Chau T.. (2002) Synthesis and pharmacological characterization of a potent, orally active p38 kinase inhibitor.. Bioorg Med Chem Lett, 12 (12): (1559-1562). [PMID:12039561] |
| 2. Wang Y, Metcalf CA, Shakespeare WC, Sundaramoorthi R, Keenan TP, Bohacek RS, van Schravendijk MR, Violette SM, Narula SS, Dalgarno DC, Haraldson C, Keats J, Liou S, Mani U, Pradeepan S, Ram M, Adams S, Weigele M, Sawyer TK.. (2003) Bone-targeted 2,6,9-trisubstituted purines: novel inhibitors of Src tyrosine kinase for the treatment of bone diseases.. Bioorg Med Chem Lett, 13 (18): (3067-3070). [PMID:12941335] |
| 3. Trejo A, Arzeno H, Browner M, Chanda S, Cheng S, Comer DD, Dalrymple SA, Dunten P, Lafargue J, Lovejoy B, Freire-Moar J, Lim J, Mcintosh J, Miller J, Papp E, Reuter D, Roberts R, Sanpablo F, Saunders J, Song K, Villasenor A, Warren SD, Welch M, Weller P, Whiteley PE, Zeng L, Goldstein DM.. (2003) Design and synthesis of 4-azaindoles as inhibitors of p38 MAP kinase.. J Med Chem, 46 (22): (4702-4713). [PMID:14561090] |
| 4. Kinoshita T, Yoshida I, Nakae S, Okita K, Gouda M, Matsubara M, Yokota K, Ishiguro H, Tada T. (2008) Crystal structure of human mono-phosphorylated ERK1 at Tyr204.. Biochem Biophys Res Commun, 377 (4): (1123-7). [PMID:18983981] |
| 5. Soth M, Hermann JC, Yee C, Alam M, Barnett JW, Berry P, Browner MF, Frank K, Frauchiger S, Harris S et al.. (2013) 3-Amido pyrrolopyrazine JAK kinase inhibitors: development of a JAK3 vs JAK1 selective inhibitor and evaluation in cellular and in vivo models.. J Med Chem, 56 (1): (345-56). [PMID:23214979] |
| 6. Kubo K, Shimizu T, Ohyama S, Murooka H, Iwai A, Nakamura K, Hasegawa K, Kobayashi Y, Takahashi N, Takahashi K et al.. (2005) Novel potent orally active selective VEGFR-2 tyrosine kinase inhibitors: synthesis, structure-activity relationships, and antitumor activities of N-phenyl-N'-{4-(4-quinolyloxy)phenyl}ureas.. J Med Chem, 48 (5): (1359-66). [PMID:15743179] |
| 7. Greenman C, Stephens P, Smith R, Dalgliesh GL, Hunter C, Bignell G, Davies H, Teague J, Butler A, Stevens C et al.. (2007) Patterns of somatic mutation in human cancer genomes.. Nature, 446 (7132): (153-8). [PMID:17344846] |
| 8. Elkins JM, Wang J, Deng X, Pattison MJ, Arthur JS, Erazo T, Gomez N, Lizcano JM, Gray NS, Knapp S. (2013) X-ray crystal structure of ERK5 (MAPK7) in complex with a specific inhibitor.. J Med Chem, 56 (11): (4413-21). [PMID:23656407] |
| 9. Mettey Y, Gompel M, Thomas V, Garnier M, Leost M, Ceballos-Picot I, Noble M, Endicott J, Vierfond JM, Meijer L. (2003) Aloisines, a new family of CDK/GSK-3 inhibitors. SAR study, crystal structure in complex with CDK2, enzyme selectivity, and cellular effects.. J Med Chem, 46 (2): (222-36). [PMID:12519061] |
| 10. Gray NS, Wodicka L, Thunnissen AM, Norman TC, Kwon S, Espinoza FH, Morgan DO, Barnes G, LeClerc S, Meijer L et al.. (1998) Exploiting chemical libraries, structure, and genomics in the search for kinase inhibitors.. Science, 281 (5376): (533-8). [PMID:9677190] |
| 11. Szczepankiewicz BG, Kosogof C, Nelson LT, Liu G, Liu B, Zhao H, Serby MD, Xin Z, Liu M, Gum RJ et al.. (2006) Aminopyridine-based c-Jun N-terminal kinase inhibitors with cellular activity and minimal cross-kinase activity.. J Med Chem, 49 (12): (3563-80). [PMID:16759099] |
| 12. Oyarzabal J, Zarich N, Albarran MI, Palacios I, Urbano-Cuadrado M, Mateos G, Reymundo I, Rabal O, Salgado A, Corrionero A et al.. (2010) Discovery of mitogen-activated protein kinase-interacting kinase 1 inhibitors by a comprehensive fragment-oriented virtual screening approach.. J Med Chem, 53 (18): (6618-28). [PMID:20722422] |
| 13. Chen F, Hancock CN, Macias AT, Joh J, Still K, Zhong S, MacKerell Jr AD, Shapiro P. (2006) Characterization of ATP-independent ERK inhibitors identified through in silico analysis of the active ERK2 structure.. Bioorg Med Chem Lett, 16 (24): (6281-7). [PMID:17000106] |
| 14. Devadas B, Selness SR, Xing L, Madsen HM, Marrufo LD, Shieh H, Messing DM, Yang JZ, Morgan HM, Anderson GD et al.. (2011) Substituted N-aryl-6-pyrimidinones: a new class of potent, selective, and orally active p38 MAP kinase inhibitors.. Bioorg Med Chem Lett, 21 (13): (3856-60). [PMID:21620699] |
| 15. Rowbottom MW, Faraoni R, Chao Q, Campbell BT, Lai AG, Setti E, Ezawa M, Sprankle KG, Abraham S, Tran L et al.. (2012) Identification of 1-(3-(6,7-dimethoxyquinazolin-4-yloxy)phenyl)-3-(5-(1,1,1-trifluoro-2-methylpropan-2-yl)isoxazol-3-yl)urea hydrochloride (CEP-32496), a highly potent and orally efficacious inhibitor of V-RAF murine sarcoma viral oncogene homologue B1 (BRAF) V600E.. J Med Chem, 55 (3): (1082-105). [PMID:22168626] |
| 16. Apsel B, Blair JA, Gonzalez B, Nazif TM, Feldman ME, Aizenstein B, Hoffman R, Williams RL, Shokat KM, Knight ZA. (2008) Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases.. Nat Chem Biol, 4 (11): (691-9). [PMID:18849971] |
| 17. Zarrinkar PP, Gunawardane RN, Cramer MD, Gardner MF, Brigham D, Belli B, Karaman MW, Pratz KW, Pallares G, Chao Q et al.. (2009) AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).. Blood, 114 (14): (2984-92). [PMID:19654408] |
| 18. Goodfellow VS, Loweth CJ, Ravula SB, Wiemann T, Nguyen T, Xu Y, Todd DE, Sheppard D, Pollack S, Polesskaya O et al.. (2013) Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3.. J Med Chem, 56 (20): (8032-48). [PMID:24044867] |
| 19. Hall MD, Salam NK, Hellawell JL, Fales HM, Kensler CB, Ludwig JA, Szakács G, Hibbs DE, Gottesman MM. (2009) Synthesis, activity, and pharmacophore development for isatin-beta-thiosemicarbazones with selective activity toward multidrug-resistant cells.. J Med Chem, 52 (10): (3191-204). [PMID:19397322] |
| 20. Lafleur K, Huang D, Zhou T, Caflisch A, Nevado C. (2009) Structure-based optimization of potent and selective inhibitors of the tyrosine kinase erythropoietin producing human hepatocellular carcinoma receptor B4 (EphB4).. J Med Chem, 52 (20): (6433-46). [PMID:19788238] |
| 21. Li B, Cociorva OM, Nomanbhoy T, Weissig H, Li Q, Nakamura K, Liyanage M, Zhang MC, Shih AY, Aban A et al.. (2013) Hit-to-lead optimization and kinase selectivity of imidazo[1,2-a]quinoxalin-4-amine derived JNK1 inhibitors.. Bioorg Med Chem Lett, 23 (18): (5217-22). [PMID:23916259] |
| 22. Ward RA, Colclough N, Challinor M, Debreczeni JE, Eckersley K, Fairley G, Feron L, Flemington V, Graham MA, Greenwood R et al.. (2015) Structure-Guided Design of Highly Selective and Potent Covalent Inhibitors of ERK1/2.. J Med Chem, 58 (11): (4790-801). [PMID:25977981] |
| 23. Miwatashi S, Arikawa Y, Kotani E, Miyamoto M, Naruo K, Kimura H, Tanaka T, Asahi S, Ohkawa S. (2005) Novel inhibitor of p38 MAP kinase as an anti-TNF-alpha drug: discovery of N-[4-[2-ethyl-4-(3-methylphenyl)-1,3-thiazol-5-yl]-2-pyridyl]benzamide (TAK-715) as a potent and orally active anti-rheumatoid arthritis agent.. J Med Chem, 48 (19): (5966-79). [PMID:16162000] |
| 24. Kim KH, Maderna A, Schnute ME, Hegen M, Mohan S, Miyashiro J, Lin L, Li E, Keegan S, Lussier J et al.. (2011) Imidazo[1,5-a]quinoxalines as irreversible BTK inhibitors for the treatment of rheumatoid arthritis.. Bioorg Med Chem Lett, 21 (21): (6258-63). [PMID:21958547] |
| 25. He X, Da Ros S, Nelson J, Zhu X, Jiang T, Okram B, Jiang S, Michellys PY, Iskandar M, Espinola S et al.. (2017) Identification of Potent and Selective RIPK2 Inhibitors for the Treatment of Inflammatory Diseases.. ACS Med Chem Lett, 8 (10): (1048-1053). [PMID:29057049] |
| 26. Tan L, Gurbani D, Weisberg EL, Jones DS, Rao S, Singer WD, Bernard FM, Mowafy S, Jenney A, Du G et al.. (2017) Studies of TAK1-centered polypharmacology with novel covalent TAK1 inhibitors.. Bioorg Med Chem, 25 (4): (1320-1328). [PMID:28038940] |
| 27. Heightman TD, Berdini V, Braithwaite H, Buck IM, Cassidy M, Castro J, Courtin A, Day JEH, East C, Fazal L et al.. (2018) Fragment-Based Discovery of a Potent, Orally Bioavailable Inhibitor That Modulates the Phosphorylation and Catalytic Activity of ERK1/2.. J Med Chem, 61 (11): (4978-4992). [PMID:29775310] |
| 28. Patel S, Harris SF, Gibbons P, Deshmukh G, Gustafson A, Kellar T, Lin H, Liu X, Liu Y, Liu Y et al.. (2015) Scaffold-Hopping and Structure-Based Discovery of Potent, Selective, And Brain Penetrant N-(1H-Pyrazol-3-yl)pyridin-2-amine Inhibitors of Dual Leucine Zipper Kinase (DLK, MAP3K12).. J Med Chem, 58 (20): (8182-99). [PMID:26431428] |
| 29. Das J, Furch JA, Liu C, Moquin RV, Lin J, Spergel SH, McIntyre KW, Shuster DJ, O'Day KD, Penhallow B et al.. (2006) Discovery and SAR of 2-amino-5-(thioaryl)thiazoles as potent and selective Itk inhibitors.. Bioorg Med Chem Lett, 16 (14): (3706-12). [PMID:16682193] |
| 30. Zhang H, Xu L, Qin X, Chen X, Cong H, Hu L, Chen L, Miao Z, Zhang W, Cai Z et al.. (2019) N-(7-Cyano-6-(4-fluoro-3-(2-(3-(trifluoromethyl)phenyl)acetamido)phenoxy)benzo[d]thiazol-2-yl)cyclopropanecarboxamide (TAK-632) Analogues as Novel Necroptosis Inhibitors by Targeting Receptor-Interacting Protein Kinase 3 (RIPK3): Synthesis, Structure-Activity Relationships, and in Vivo Efficacy.. J Med Chem, 62 (14): (6665-6681). [PMID:31095385] |
| 31. Czako B, Marszalek JR, Burke JP, Mandal P, Leonard PG, Cross JB, Mseeh F, Jiang Y, Chang EQ, Suzuki E et al.. (2020) Discovery of IACS-9439, a Potent, Exquisitely Selective, and Orally Bioavailable Inhibitor of CSF1R.. J Med Chem, 71 (13): (1755-70). [PMID:32787110] |
| 32. Erik Rytter Ottosen,Morten Dahl S?rensen,Fredrik Bj?rkling,Tine Skak-Nielsen,Marianne Scheel Fjording,Helle Aaes,Lise Binderup. (2003-12-12) Synthesis and structure-activity relationship of aminobenzophenones. A novel class of p38 MAP kinase inhibitors with high antiinflammatory activity.. Journal of medicinal chemistry, 46 ((26)): (5651-5662). [PMID:14667219] |
| 33. Robert M Rzasa,Matthew R Kaller,Gang Liu,Ella Magal,Thomas T Nguyen,Timothy D Osslund,David Powers,Vincent J Santora,Vellarkad N Viswanadhan,Hui-Ling Wang,Xiaoling Xiong,Wenge Zhong,Mark H Norman. (2007-08-19) Structure-activity relationships of 3,4-dihydro-1H-quinazolin-2-one derivatives as potential CDK5 inhibitors.. Bioorganic & medicinal chemistry, 15 ((20)): (6574-6595). [PMID:17697781] |
| 34. Chun Liang,Yan Ding,Huu Tung Nguyen,Jeong-Ah Kim,Hye-Jin Boo,Hee-Kyoung Kang,Mahn Cuong Nguyen,Young Ho Kim. (2010-10-19) Oleanane-type triterpenoids from Panax stipuleanatus and their anticancer activities.. Bioorganic & medicinal chemistry letters, 20 ((23)): (7110-7115). [PMID:20951582] |
| 35. Seunghee Hong,Jinhee Kim,Sun-Mi Yun,Hyunseung Lee,Yoonsu Park,Soon-Sun Hong,Sungwoo Hong. (2013-04-23) Discovery of new benzothiazole-based inhibitors of breakpoint cluster region-Abelson kinase including the T315I mutant.. Journal of medicinal chemistry, 56 ((9)): (3531-3545). [PMID:23600806] |
| 36. Sharon Gauci,Andreas O Helbig,Monique Slijper,Jeroen Krijgsveld,Albert J R Heck,Shabaz Mohammed. (2009-05-06) Lys-N and trypsin cover complementary parts of the phosphoproteome in a refined SCX-based approach.. Analytical chemistry, 81 ((11)): (4493-4501). [PMID:19413330] |
| 37. Bruno O, Brullo C, Bondavalli F, Schenone S, Ranise A, Arduino N, Bertolotto MB, Montecucco F, Ottonello L, Dallegri F, Tognolini M, Ballabeni V, Bertoni S, Barocelli E.. (2007) Synthesis and biological evaluation of N-pyrazolyl-N'-alkyl/benzyl/phenylureas: a new class of potent inhibitors of interleukin 8-induced neutrophil chemotaxis.. J Med Chem, 50 (15): (3618-3626). [PMID:17608466] |
| 38. Hu MK, Liao YF, Chen JF, Wang BJ, Tung YT, Lin HC, Lee KP.. (2008) New 1,2,3,4-tetrahydroisoquinoline derivatives as modulators of proteolytic cleavage of amyloid precursor proteins.. Bioorg Med Chem, 16 (4): (1957-1965). [PMID:18024043] |
| 39. Martin MW, Newcomb J, Nunes JJ, Boucher C, Chai L, Epstein LF, Faust T, Flores S, Gallant P, Gore A, Gu Y, Hsieh F, Huang X, Kim JL, Middleton S, Morgenstern K, Oliveira-dos-Santos A, Patel VF, Powers D, Rose P, Tudor Y, Turci SM, Welcher AA, Zack D, Zhao H, Zhu L, Zhu X, Ghiron C, Ermann M, Johnston D, Saluste CG.. (2008) Structure-based design of novel 2-amino-6-phenyl-pyrimido[5',4':5,6]pyrimido[1,2-a]benzimidazol-5(6H)-ones as potent and orally active inhibitors of lymphocyte specific kinase (Lck): synthesis, SAR, and in vivo anti-inflammatory activity.. J Med Chem, 51 (6): (1637-1648). [PMID:18278858] |
| 40. DiMauro EF, Newcomb J, Nunes JJ, Bemis JE, Boucher C, Chai L, Chaffee SC, Deak HL, Epstein LF, Faust T, Gallant P, Gore A, Gu Y, Henkle B, Hsieh F, Huang X, Kim JL, Lee JH, Martin MW, McGowan DC, Metz D, Mohn D, Morgenstern KA, Oliveira-dos-Santos A, Patel VF, Powers D, Rose PE, Schneider S, Tomlinson SA, Tudor YY, Turci SM, Welcher AA, Zhao H, Zhu L, Zhu X.. (2008) Structure-guided design of aminopyrimidine amides as potent, selective inhibitors of lymphocyte specific kinase: synthesis, structure-activity relationships, and inhibition of in vivo T cell activation.. J Med Chem, 51 (6): (1681-1694). [PMID:18321037] |
| 41. Jang SW, Okada M, Sayeed I, Xiao G, Stein D, Jin P, Ye K.. (2007) Gambogic amide, a selective agonist for TrkA receptor that possesses robust neurotrophic activity, prevents neuronal cell death.. Proc Natl Acad Sci U S A, 104 (41): (16329-16334). [PMID:17911251] |
| 42. Feng Y, Yin Y, Weiser A, Griffin E, Cameron MD, Lin L, Ruiz C, Schürer SC, Inoue T, Rao PV, Schr?ter T, Lograsso P.. (2008) Discovery of substituted 4-(pyrazol-4-yl)-phenylbenzodioxane-2-carboxamides as potent and highly selective Rho kinase (ROCK-II) inhibitors.. J Med Chem, 51 (21): (6642-6645). [PMID:18834107] |
| 43. Hirabayashi A, Mukaiyama H, Kobayashi H, Shiohara H, Nakayama S, Ozawa M, Miyazawa K, Misawa K, Ohnota H, Isaji M.. (2009) Structure-activity relationship studies of 5-benzylaminoimidazo[1,2-c]pyrimidine-8-carboxamide derivatives as potent, highly selective ZAP-70 kinase inhibitors.. Bioorg Med Chem, 17 (1): (284-294). [PMID:19010686] |
| 44. Xia Z, Knaak C, Ma J, Beharry ZM, McInnes C, Wang W, Kraft AS, Smith CD.. (2009) Synthesis and evaluation of novel inhibitors of Pim-1 and Pim-2 protein kinases.. J Med Chem, 52 (1): (74-86). [PMID:19072652] |
| 45. D'Angelo ND, Bellon SF, Booker SK, Cheng Y, Coxon A, Dominguez C, Fellows I, Hoffman D, Hungate R, Kaplan-Lefko P, Lee MR, Li C, Liu L, Rainbeau E, Reider PJ, Rex K, Siegmund A, Sun Y, Tasker AS, Xi N, Xu S, Yang Y, Zhang Y, Burgess TL, Dussault I, Kim TS.. (2008) Design, synthesis, and biological evaluation of potent c-Met inhibitors.. J Med Chem, 51 (18): (5766-5779). [PMID:18763753] |
| 46. Li Q, Al-Ayoubi A, Guo T, Zheng H, Sarkar A, Nguyen T, Eblen ST, Grant S, Kellogg GE, Zhang S.. (2009) Structure-activity relationship (SAR) studies of 3-(2-amino-ethyl)-5-(4-ethoxy-benzylidene)-thiazolidine-2,4-dione: development of potential substrate-specific ERK1/2 inhibitors.. Bioorg Med Chem Lett, 19 (21): (6042-6046). [PMID:19796943] |
| 47. Shomin CD, Meyer SC, Ghosh I.. (2009) Staurosporine tethered peptide ligands that target cAMP-dependent protein kinase (PKA): optimization and selectivity profiling.. Bioorg Med Chem, 17 (17): (6196-6202). [PMID:19674907] |
| 48. Wee XK, Yeo WK, Zhang B, Tan VB, Lim KM, Tay TE, Go ML.. (2009) Synthesis and evaluation of functionalized isoindigos as antiproliferative agents.. Bioorg Med Chem, 17 (21): (7562-7571). [PMID:19783149] |
| 49. Qiao L, Choi S, Case A, Gainer TG, Seyb K, Glicksman MA, Lo DC, Stein RL, Cuny GD.. (2009) Structure-activity relationship study of EphB3 receptor tyrosine kinase inhibitors.. Bioorg Med Chem Lett, 19 (21): (6122-6126). [PMID:19783434] |
| 50. Deng X, Lim SM, Zhang J, Gray NS.. (2010) Broad spectrum alkynyl inhibitors of T315I Bcr-Abl.. Bioorg Med Chem Lett, 20 (14): (4196-4200). [PMID:20541934] |
| 51. Andreani A, Bellini S, Burnelli S, Granaiola M, Leoni A, Locatelli A, Morigi R, Rambaldi M, Varoli L, Calonghi N, Cappadone C, Zini M, Stefanelli C, Masotti L, Shoemaker RH.. (2010) Substituted E-3-(3-indolylmethylene)-1,3-dihydroindol-2-ones with antitumor activity. In depth study of the effect on growth of breast cancer cells.. J Med Chem, 53 (15): (5567-5575). [PMID:20684599] |
| 52. Samadi AK, Tong X, Mukerji R, Zhang H, Timmermann BN, Cohen MS.. (2010) Withaferin A, a cytotoxic steroid from Vassobia breviflora, induces apoptosis in human head and neck squamous cell carcinoma.. J Nat Prod, 73 (9): (1476-1481). [PMID:20726569] |
| 53. Charrier JD, Miller A, Kay DP, Brenchley G, Twin HC, Collier PN, Ramaya S, Keily SB, Durrant SJ, Knegtel RM, Tanner AJ, Brown K, Curnock AP, Jimenez JM.. (2011) Discovery and structure-activity relationship of 3-aminopyrid-2-ones as potent and selective interleukin-2 inducible T-cell kinase (Itk) inhibitors.. J Med Chem, 54 (7): (2341-2350). [PMID:21391610] |
| 54. De SK, Barile E, Chen V, Stebbins JL, Cellitti JF, Machleidt T, Carlson CB, Yang L, Dahl R, Pellecchia M.. (2011) Design, synthesis, and structure-activity relationship studies of thiophene-3-carboxamide derivatives as dual inhibitors of the c-Jun N-terminal kinase.. Bioorg Med Chem, 19 (8): (2582-2588). [PMID:21458276] |
| 55. Ishikawa T, Seto M, Banno H, Kawakita Y, Oorui M, Taniguchi T, Ohta Y, Tamura T, Nakayama A, Miki H, Kamiguchi H, Tanaka T, Habuka N, Sogabe S, Yano J, Aertgeerts K, Kamiyama K.. (2011) Design and synthesis of novel human epidermal growth factor receptor 2 (HER2)/epidermal growth factor receptor (EGFR) dual inhibitors bearing a pyrrolo[3,2-d]pyrimidine scaffold.. J Med Chem, 54 (23): (8030-8050). [PMID:22003817] |
| 56. Festa M, Capasso A, D'Acunto CW, Masullo M, Rossi AG, Pizza C, Piacente S.. (2011) Xanthohumol induces apoptosis in human malignant glioblastoma cells by increasing reactive oxygen species and activating MAPK pathways.. J Nat Prod, 74 (12): (2505-2513). [PMID:22111577] |
| 57. Yang T, Lu Z, Meng L, Wei S, Hong K, Zhu W, Huang C.. (2012) The novel agent ophiobolin O induces apoptosis and cell cycle arrest of MCF-7 cells through activation of MAPK signaling pathways.. Bioorg Med Chem Lett, 22 (1): (579-585). [PMID:22130129] |
| 58. Cuny GD, Ulyanova NP, Patnaik D, Liu JF, Lin X, Auerbach K, Ray SS, Xian J, Glicksman MA, Stein RL, Higgins JM.. (2012) Structure-activity relationship study of beta-carboline derivatives as haspin kinase inhibitors.. Bioorg Med Chem Lett, 22 (5): (2015-2019). [PMID:22335895] |
| 59. Zhang J, Deng X, Choi HG, Alessi DR, Gray NS.. (2012) Characterization of TAE684 as a potent LRRK2 kinase inhibitor.. Bioorg Med Chem Lett, 22 (5): (1864-1869). [PMID:22335897] |
| 60. Wei X, Du ZY, Zheng X, Cui XX, Conney AH, Zhang K.. (2012) Synthesis and evaluation of curcumin-related compounds for anticancer activity.. Eur J Med Chem, 53 (): (235-245). [PMID:22551677] |
| 61. Innocenti P, Cheung KM, Solanki S, Mas-Droux C, Rowan F, Yeoh S, Boxall K, Westlake M, Pickard L, Hardy T, Baxter JE, Aherne GW, Bayliss R, Fry AM, Hoelder S.. (2012) Design of potent and selective hybrid inhibitors of the mitotic kinase Nek2: structure-activity relationship, structural biology, and cellular activity.. J Med Chem, 55 (7): (3228-3241). [PMID:22404346] |
| 62. Andreani A, Granaiola M, Locatelli A, Morigi R, Rambaldi M, Varoli L, Calonghi N, Cappadone C, Farruggia G, Stefanelli C, Masotti L, Nguyen TL, Hamel E, Shoemaker RH.. (2012) Substituted 3-(5-imidazo[2,1-b]thiazolylmethylene)-2-indolinones and analogues: synthesis, cytotoxic activity, and study of the mechanism of action.. J Med Chem, 55 (5): (2078-2088). [PMID:22283430] |
| 63. Illig CR, Manthey CL, Wall MJ, Meegalla SK, Chen J, Wilson KJ, Ballentine SK, Desjarlais RL, Schubert C, Crysler CS, Chen Y, Molloy CJ, Chaikin MA, Donatelli RR, Yurkow E, Zhou Z, Player MR, Tomczuk BE.. (2011) Optimization of a potent class of arylamide colony-stimulating factor-1 receptor inhibitors leading to anti-inflammatory clinical candidate 4-cyano-N-[2-(1-cyclohexen-1-yl)-4-[1-[(dimethylamino)acetyl]-4-piperidinyl]phenyl]-1H-imidazole-2-carboxamide (JNJ-28312141).. J Med Chem, 54 (22): (7860-7883). [PMID:22039836] |
| 64. Huh JE, Kang JW, Nam D, Baek YH, Choi DY, Park DS, Lee JD.. (2012) Melittin suppresses VEGF-A-induced tumor growth by blocking VEGFR-2 and the COX-2-mediated MAPK signaling pathway.. J Nat Prod, 75 (11): (1922-1929). [PMID:23110475] |
| 65. Sunose M, Bell K, Ellard K, Bergamini G, Neubauer G, Werner T, Ramsden N.. (2012) Discovery of 5-(2-amino-[1,2,4]triazolo[1,5-a]pyridin-7-yl)-N-(tert-butyl)pyridine-3-sulfonamide (CZC24758), as a potent, orally bioavailable and selective inhibitor of PI3K for the treatment of inflammatory disease.. Bioorg Med Chem Lett, 22 (14): (4613-4618). [PMID:22726925] |
| 66. Reith AD, Bamborough P, Jandu K, Andreotti D, Mensah L, Dossang P, Choi HG, Deng X, Zhang J, Alessi DR, Gray NS.. (2012) GSK2578215A; a potent and highly selective 2-arylmethyloxy-5-substitutent-N-arylbenzamide LRRK2 kinase inhibitor.. Bioorg Med Chem Lett, 22 (17): (5625-5629). [PMID:22863203] |
| 67. Jimenez JM, Boyall D, Brenchley G, Collier PN, Davis CJ, Fraysse D, Keily SB, Henderson J, Miller A, Pierard F, Settimo L, Twin HC, Bolton CM, Curnock AP, Chiu P, Tanner AJ, Young S.. (2013) Design and optimization of selective protein kinase C θ (PKCθ) inhibitors for the treatment of autoimmune diseases.. J Med Chem, 56 (5): (1799-1810). [PMID:23398373] |
| 68. Dole?ková I, Cesnek M, Dra?insky M, Brynda J, Voller J, Janeba Z, Kry?tof V.. (2013) Synthesis and biological evaluation of guanidino analogues of roscovitine.. Eur J Med Chem, 62 (): (443-452). [PMID:23399722] |
| 69. Mortensen DS, Sapienza J, Lee BG, Perrin-Ninkovic SM, Harris R, Shevlin G, Parnes JS, Whitefield B, Hickman M, Khambatta G, Bisonette RR, Peng S, Gamez JC, Leisten J, Narla RK, Fultz KE, Sankar S.. (2013) Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.. Bioorg Med Chem Lett, 23 (6): (1588-1591). [PMID:23414803] |
| 70. Bowers S, Truong AP, Ye M, Aubele DL, Sealy JM, Neitz RJ, Hom RK, Chan W, Dappen MS, Galemmo RA, Konradi AW, Sham HL, Zhu YL, Beroza P, Tonn G, Zhang H, Hoffman J, Motter R, Fauss D, Tanaka P, Bova MP, Ren Z, Tam D, Ruslim L, Baker J, Pandya D, Diep L, Fitzgerald K, Artis DR, Anderson JP, Bergeron M.. (2013) Design and synthesis of highly selective, orally active Polo-like kinase-2 (Plk-2) inhibitors.. Bioorg Med Chem Lett, 23 (9): (2743-2749). [PMID:23522834] |
| 71. Kamal A, Faazil S, Ramaiah MJ, Ashraf M, Balakrishna M, Pushpavalli SN, Patel N, Pal-Bhadra M.. (2013) Synthesis and study of benzothiazole conjugates in the control of cell proliferation by modulating Ras/MEK/ERK-dependent pathway in MCF-7 cells.. Bioorg Med Chem Lett, 23 (20): (5733-5739). [PMID:23999041] |
| 72. Akama T, Dong C, Virtucio C, Freund YR, Chen D, Orr MD, Jacobs RT, Zhang YK, Hernandez V, Liu Y, Wu A, Bu W, Liu L, Jarnagin K, Plattner JJ.. (2013) Discovery and structure-activity relationships of 6-(benzoylamino)benzoxaboroles as orally active anti-inflammatory agents.. Bioorg Med Chem Lett, 23 (21): (5870-5873). [PMID:24075731] |
| 73. Haftchenary S, Luchman HA, Jouk AO, Veloso AJ, Page BD, Cheng XR, Dawson SS, Grinshtein N, Shahani VM, Kerman K, Kaplan DR, Griffin C, Aman AM, Al-Awar R, Weiss S, Gunning PT.. (2013) Potent Targeting of the STAT3 Protein in Brain Cancer Stem Cells: A Promising Route for Treating Glioblastoma.. ACS Med Chem Lett, 4 (11): (1102-1107). [PMID:24900612] |
| 74. Carrasco E, álvarez PJ, Melguizo C, Prados J, álvarez-Manzaneda E, Chahboun R, Messouri I, Vázquez-Vázquez MI, Aránega A, Rodríguez-Serrano F.. (2014) Novel merosesquiterpene exerts a potent antitumor activity against breast cancer cells in vitro and in vivo.. Eur J Med Chem, 79 (): (1-12). [PMID:24704691] |
| 75. Rechfeld F, Gruber P, Kirchmair J, Boehler M, Hauser N, Hechenberger G, Garczarczyk D, Lapa GB, Preobrazhenskaya MN, Goekjian P, Langer T, Hofmann J.. (2014) Thienoquinolines as novel disruptors of the PKCε/RACK2 protein-protein interaction.. J Med Chem, 57 (8): (3235-3246). [PMID:24712764] |
| 76. Hasumi K, Sato S, Saito T, Kato JY, Shirota K, Sato J, Suzuki H, Ohta S.. (2014) Design and synthesis of 5-[(2-chloro-6-fluorophenyl)acetylamino]-3-(4-fluorophenyl)-4-(4-pyrimidinyl)isoxazole (AKP-001), a novel inhibitor of p38 MAP kinase with reduced side effects based on the antedrug concept.. Bioorg Med Chem, 22 (15): (4162-4176). [PMID:24938496] |
| 77. Avdieiev S, Gera L, Havrylyuk D, Hodges RS, Lesyk R, Ribrag V, Vassetzky Y, Kavsan V.. (2014) Bradykinin antagonists and thiazolidinone derivatives as new potential anti-cancer compounds.. Bioorg Med Chem, 22 (15): (3815-3823). [PMID:25012567] |
| 78. Lawrence HR, Mahajan K, Luo Y, Zhang D, Tindall N, Huseyin M, Gevariya H, Kazi S, Ozcan S, Mahajan NP, Lawrence NJ.. (2015) Development of novel ACK1/TNK2 inhibitors using a fragment-based approach.. J Med Chem, 58 (6): (2746-2763). [PMID:25699576] |
| 79. Zhou X, Wang Y, Lee WY, Or PM, Wan DC, Kwan YW, Yeung JH.. (2015) Miltirone Is a Dual Inhibitor of P-Glycoprotein and Cell Growth in Doxorubicin-Resistant HepG2 Cells.. J Nat Prod, 78 (9): (2266-2275). [PMID:26339922] |
| 80. Uehling DE, Harris PA.. (2015) Recent progress on MAP kinase pathway inhibitors.. Bioorg Med Chem Lett, 25 (19): (4047-4056). [PMID:26298497] |
| 81. Miklossy G, Youn UJ, Yue P, Zhang M, Chen CH, Hilliard TS, Paladino D, Li Y, Choi J, Sarkaria JN, Kawakami JK, Wongwiwatthananukit S, Chen Y, Sun D, Chang LC, Turkson J.. (2015) Hirsutinolide Series Inhibit Stat3 Activity, Alter GCN1, MAP1B, Hsp105, G6PD, Vimentin, TrxR1, and Importin α-2 Expression, and Induce Antitumor Effects against Human Glioma.. J Med Chem, 58 (19): (7734-7748). [PMID:26331426] |
| 82. Charnley AK, Convery MA, Lakdawala Shah A, Jones E, Hardwicke P, Bridges A, Ouellette M, Totoritis R, Schwartz B, King BW, Wisnoski DD, Kang J, Eidam PM, Votta BJ, Gough PJ, Marquis RW, Bertin J, Casillas L.. (2015) Crystal structures of human RIP2 kinase catalytic domain complexed with ATP-competitive inhibitors: Foundations for understanding inhibitor selectivity.. Bioorg Med Chem, 23 (21): (7000-7006). [PMID:26455654] |
| 83. Sestito S, Nesi G, Daniele S, Martelli A, Digiacomo M, Borghini A, Pietra D, Calderone V, Lapucci A, Falasca M, Parrella P, Notarangelo A, Breschi MC, Macchia M, Martini C, Rapposelli S.. (2015) Design and synthesis of 2-oxindole based multi-targeted inhibitors of PDK1/Akt signaling pathway for the treatment of glioblastoma multiforme.. Eur J Med Chem, 105 (): (274-288). [PMID:26498573] |
| 84. Simon-Szabó L, Kokas M, Greff Z, Boros S, Bánhegyi P, Zsákai L, Szántai-Kis C, Vantus T, Mandl J, Bánhegyi G, Vályi-Nagy I, ?rfi L, Ullrich A, Csala M, Kéri G.. (2016) Novel compounds reducing IRS-1 serine phosphorylation for treatment of diabetes.. Bioorg Med Chem Lett, 26 (2): (424-428). [PMID:26704265] |
| 85. Aman W, Lee J, Kim M, Yang S, Jung H, Hah JM.. (2016) Discovery of highly selective CRAF inhibitors, 3-carboxamido-2H-indazole-6-arylamide: In silico FBLD design, synthesis and evaluation.. Bioorg Med Chem Lett, 26 (4): (1188-1192). [PMID:26810260] |
| 86. Juszczak M, Walczak K, Matysiak J, Lemieszek MK, Langner E, Karpińska MM, Po?arowski P, Niewiadomy A, Rzeski W.. (2016) New derivative of 2-(2,4-dihydroxyphenyl)thieno-1,3-thiazin-4-one (BChTT) elicits antiproliferative effect via p38-mediated cell cycle arrest in cancer cells.. Bioorg Med Chem, 24 (6): (1356-1361). [PMID:26897091] |
| 87. Schroeder RL, Goyal N, Bratton M, Townley I, Pham NA, Tram P, Stone T, Geathers J, Nguyen K, Sridhar J.. (2016) Identification of quinones as novel PIM1 kinase inhibitors.. Bioorg Med Chem Lett, 26 (13): (3187-3191). [PMID:27173800] |
| 88. Kumar V, Guru SK, Jain SK, Joshi P, Gandhi SG, Bharate SB, Bhushan S, Bharate SS, Vishwakarma RA.. (2016) A chromatography-free isolation of rohitukine from leaves of Dysoxylum binectariferum: Evaluation for in vitro cytotoxicity, Cdk inhibition and physicochemical properties.. Bioorg Med Chem Lett, 26 (15): (3457-3463). [PMID:27363938] |
| 89. Ravishankar D, Corona G, Hogan SM, Spencer JPE, Greco F, Osborn HMI.. (2016) Thioflavones as novel neuroprotective agents.. Bioorg Med Chem, 24 (21): (5513-5520). [PMID:27663547] |
| 90. Klaeger S, Heinzlmeir S and Wilhelm M et al. (2017) The target landscape of clinical kinase drugs.. Science, 358 (6367): (). [PMID:29191878] |
| 91. Kim YJ, Jeon Y, Kim T, Lim WC, Ham J, Park YN, Kim TJ, Ko H.. (2017) Combined treatment with zingerone and its novel derivative synergistically inhibits TGF-β1 induced epithelial-mesenchymal transition, migration and invasion of human hepatocellular carcinoma cells.. Bioorg Med Chem Lett, 27 (4): (1081-1088). [PMID:28110870] |
| 92. Chen Y, Zheng Y, Jiang Q, Qin F, Zhang Y, Fu L, He G.. (2017) Integrated bioinformatics, computational and experimental methods to discover novel Raf/extracellular-signal regulated kinase (ERK) dual inhibitors against breast cancer cells.. Eur J Med Chem, 127 (): (997-1011). [PMID:27839788] |
| 93. Argyros O, Lougiakis N, Kouvari E, Papafotika A, Raptopoulou CP, Psycharis V, Christoforidis S, Pouli N, Marakos P, Tamvakopoulos C.. (2017) Design and synthesis of novel 7-aminosubstituted pyrido[2,3-b]pyrazines exhibiting anti-breast cancer activity.. Eur J Med Chem, 126 (): (954-968). [PMID:28006668] |
| 94. Juen L, Brachet-Botineau M, Parmenon C, Bourgeais J, Hérault O, Gouilleux F, Viaud-Massuard MC, Prié G.. (2017) New Inhibitor Targeting Signal Transducer and Activator of Transcription 5 (STAT5) Signaling in Myeloid Leukemias.. J Med Chem, 60 (14): (6119-6136). [PMID:28654259] |
| 95. Wang S, Xu L, Lu YT, Liu YF, Han B, Liu T, Tang J, Li J, Wu J, Li JY, Yu LF, Yang F.. (2017) Discovery of benzofuran-3(2H)-one derivatives as novel DRAK2 inhibitors that protect islet β-cells from apoptosis.. Eur J Med Chem, 130 (): (195-208). [PMID:28249207] |
| 96. Huang H, Liu T, Guo J, Yu L, Wu X, He Y, Li D, Liu J, Zhang K, Zheng X, Goodin S.. (2017) Brefeldin A enhances docetaxel-induced growth inhibition and apoptosis in prostate cancer cells in monolayer and 3D cultures.. Bioorg Med Chem Lett, 27 (11): (2286-2291). [PMID:28462831] |
| 97. Karelia DN, Sk UH, Singh P, Gowda ASP, Pandey MK, Ramisetti SR, Amin S, Sharma AK.. (2017) Design, synthesis, and identification of a novel napthalamide-isoselenocyanate compound NISC-6 as a dual Topoisomerase-IIα and Akt pathway inhibitor, and evaluation of its anti-melanoma activity.. Eur J Med Chem, 135 (): (282-295). [PMID:28458134] |
| 98. Lechtenberg BC, Mace PD, Sessions EH, Williamson R, Stalder R, Wallez Y, Roth GP, Riedl SJ, Pasquale EB.. (2017) Structure-Guided Strategy for the Development of Potent Bivalent ERK Inhibitors.. ACS Med Chem Lett, 8 (7): (726-731). [PMID:28740606] |
| 99. Smith GP, Badolo L, Chell V, Chen IJ, Christensen KV, David L, Daechsel JA, Hentzer M, Herzig MC, Mikkelsen GK, Watson SP, Williamson DS.. (2017) The design and SAR of a novel series of 2-aminopyridine based LRRK2 inhibitors.. Bioorg Med Chem Lett, 27 (18): (4500-4505). [PMID:28802631] |
| 100. Fukuda T, Goto R, Kiho T, Ueda K, Muramatsu S, Hashimoto M, Aki A, Watanabe K, Tanaka N.. (2017) Discovery of DS79182026: A potent orally active hepcidin production inhibitor.. Bioorg Med Chem Lett, 27 (16): (3716-3722). [PMID:28705644] |
| 101. Fukuda T, Goto R, Kiho T, Ueda K, Muramatsu S, Hashimoto M, Aki A, Watanabe K, Tanaka N.. (2017) Discovery of DS28120313 as a potent orally active hepcidin production inhibitor: Design and optimization of novel 4,6-disubstituted indazole derivatives.. Bioorg Med Chem Lett, 27 (23): (5252-5257). [PMID:29079471] |
| 102. Gege C, Cummings MD, Albers M, Kinzel O, Kleymann G, Schlüter T, Steeneck C, Nelen MI, Milligan C, Spurlino J, Xue X, Leonard K, Edwards JP, Fourie A, Goldberg SD, Hoffmann T.. (2018) Identification and biological evaluation of thiazole-based inverse agonists of RORγt.. Bioorg Med Chem Lett, 28 (9): (1446-1455). [PMID:29631962] |
| 103. Yao D, Zhou Y, Zhu L, Ouyang L, Zhang J, Jiang Y, Zhao Y, Sun D, Yang S, Yu Y, Wang J.. (2017) Design, synthesis and structure-activity relationship studies of a focused library of pyrimidine moiety with anti-proliferative and anti-metastasis activities in triple negative breast cancer.. Eur J Med Chem, 140 (): (155-171). [PMID:28923383] |
| 104. Farag AK, Elkamhawy A, Londhe AM, Lee KT, Pae AN, Roh EJ.. (2017) Novel LCK/FMS inhibitors based on phenoxypyrimidine scaffold as potential treatment for inflammatory disorders.. Eur J Med Chem, 141 (): (657-675). [PMID:29107425] |
| 105. Guo J, Yu W, Cai G, Zhang W, Li S, Zhu J, Song D, Kong L.. (2018) Discovery of new benzensulfonamide derivatives as tripedal STAT3 inhibitors.. Eur J Med Chem, 151 (): (752-764). [PMID:29674294] |
| 106. Malki WH, Gouda AM, Ali HEA, Al-Rousan R, Samaha D, Abdalla AN, Bustamante J, Abd Elmageed ZY, Ali HI.. (2018) Structural-based design, synthesis, and antitumor activity of novel alloxazine analogues with potential selective kinase inhibition.. Eur J Med Chem, 152 (): (31-52). [PMID:29684708] |
| 107. Reiers?lmoen AC, Han J, Sundby E, Hoff BH.. (2018) Identification of fused pyrimidines as interleukin 17 secretion inhibitors.. Eur J Med Chem, 155 (): (562-578). [PMID:29909341] |
| 108. Thakkar M, Bhuniya D, Kaduskar R, Mengawade T, Naik K, Salunkhe V, Bhalerao A, Kurhade S, Mavinahalli J, Jain V, Petla R, Avaragolla S, Ray S, Rouduri S, Dhanave A, De S, Pathade V, Tambe A, Raje AA, Madgula V, Joshi S, Nadeem A, Bala M, Umrani D, Hariharan N, Kulkarni B, Mookhtiar KA.. (2017) Discovery and evaluation of 1H-pyrrolo[2,3-b]pyridine based selective and reversible small molecule BTK inhibitors for the treatment of rheumatoid arthritis.. Bioorg Med Chem Lett, 27 (8): (1867-1873). [PMID:28279528] |
| 109. Kim SM, Park YJ, Shin MS, Kim HR, Kim MJ, Lee SH, Yun SP, Kwon SH.. (2017) Acacetin inhibits neuronal cell death induced by 6-hydroxydopamine in cellular Parkinson's disease model.. Bioorg Med Chem Lett, 27 (23): (5207-5212). [PMID:29089232] |
| 110. Monastyrskyi A, Nilchan N, Quereda V, Noguchi Y, Ruiz C, Grant W, Cameron M, Duckett D, Roush W.. (2018) Development of dual casein kinase 1δ/1ε (CK1δ/ε) inhibitors for treatment of breast cancer.. Bioorg Med Chem, 26 (3): (590-602). [PMID:29289448] |
| 111. Assadieskandar A, Yu C, Maisonneuve P, Liu X, Chen YC, Prakash GKS, Kurinov I, Sicheri F, Zhang C.. (2018) Effects of rigidity on the selectivity of protein kinase inhibitors.. Eur J Med Chem, 146 (): (519-528). [PMID:29407977] |
| 112. Wang Q, Liu F, Qi S, Qi Z, Yan XE, Wang B, Wang A, Wang W, Chen C, Liu X, Jiang Z, Hu Z, Wang L, Wang W, Ren T, Zhang S, Yun CH, Liu Q, Liu J.. (2018) Discovery of 4-((N-(2-(dimethylamino)ethyl)acrylamido)methyl)-N-(4-methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)benzamide (CHMFL-PDGFR-159) as a highly selective type II PDGFRα kinase inhibitor for PDGFRα driving chronic eosinophilic leukemia.. Eur J Med Chem, 150 (): (366-384). [PMID:29544149] |
| 113. Luo G, Tang Z, Lao K, Li X, You Q, Xiang H.. (2018) Structure-activity relationships of 2, 4-disubstituted pyrimidines as dual ERα/VEGFR-2 ligands with anti-breast cancer activity.. Eur J Med Chem, 150 (): (783-795). [PMID:29587221] |
| 114. He LJ, Yang DL, Li SQ, Zhang YJ, Tang Y, Lei J, Frett B, Lin HK, Li HY, Chen ZZ, Xu ZG.. (2018) Facile construction of fused benzimidazole-isoquinolinones that induce cell-cycle arrest and apoptosis in colorectal cancer cells.. Bioorg Med Chem, 26 (14): (3899-3908). [PMID:29921474] |
| 115. Abbott JR, Patel PA, Howes JE, Akan DT, Kennedy JP, Burns MC, Browning CF, Sun Q, Rossanese OW, Phan J, Waterson AG, Fesik SW.. (2018) Discovery of Quinazolines That Activate SOS1-Mediated Nucleotide Exchange on RAS.. ACS Med Chem Lett, 9 (9): (941-946). [PMID:30258545] |
| 116. Pan Z, Chen Y, Liu J, Jiang Q, Yang S, Guo L, He G.. (2018) Design, synthesis, and biological evaluation of polo-like kinase 1/eukaryotic elongation factor 2 kinase (PLK1/EEF2K) dual inhibitors for regulating breast cancer cells apoptosis and autophagy.. Eur J Med Chem, 144 (): (517-528). [PMID:29288948] |
| 117. Lopez-Tapia F, Brotherton-Pleiss C, Yue P, Murakami H, Costa Araujo AC, Reis Dos Santos B, Ichinotsubo E, Rabkin A, Shah R, Lantz M, Chen S, Tius MA, Turkson J.. (2018) Linker Variation and Structure-Activity Relationship Analyses of Carboxylic Acid-based Small Molecule STAT3 Inhibitors.. ACS Med Chem Lett, 9 (3): (250-255). [PMID:29541369] |
| 118. Fearon D, Westwood IM, van Montfort RLM, Bayliss R, Jones K, Bavetsias V.. (2018) Synthesis and profiling of a 3-aminopyridin-2-one-based kinase targeted fragment library: Identification of 3-amino-5-(pyridin-4-yl)pyridin-2(1H)-one scaffold for monopolar spindle 1 (MPS1) and Aurora kinases inhibition.. Bioorg Med Chem, 26 (11): (3021-3029). [PMID:29764757] |
| 119. Jiang JK, Huang X, Shamim K, Patel PR, Lee A, Wang AQ, Nguyen K, Tawa G, Cuny GD, Yu PB, Zheng W, Xu X, Sanderson P, Huang W.. (2018) Discovery of 3-(4-sulfamoylnaphthyl)pyrazolo[1,5-a]pyrimidines as potent and selective ALK2 inhibitors.. Bioorg Med Chem Lett, 28 (20): (3356-3362). [PMID:30227946] |
| 120. Wang B, Wu J, Wu Y, Chen C, Zou F, Wang A, Wu H, Hu Z, Jiang Z, Liu Q, Wang W, Zhang Y, Liu F, Zhao M, Hu J, Huang T, Ge J, Wang L, Ren T, Wang Y, Liu J, Liu Q.. (2018) Discovery of 4-(((4-(5-chloro-2-(((1s,4s)-4-((2-methoxyethyl)amino)cyclohexyl)amino)pyridin-4-yl)thiazol-2-yl)amino)methyl)tetrahydro-2H-pyran-4-carbonitrile (JSH-150) as a novel highly selective and potent CDK9 kinase inhibitor.. Eur J Med Chem, 158 (): (896-916). [PMID:30253346] |
| 121. Dodo K, Kuboki E, Shimizu T, Imamura R, Magarisawa M, Takahashi M, Tokuhiro T, Yotsumoto S, Asano K, Nakao S, Terayama N, Suda T, Tanaka M, Sodeoka M.. (2019) Development of a Water-Soluble Indolylmaleimide Derivative IM-93 Showing Dual Inhibition of Ferroptosis and NETosis.. ACS Med Chem Lett, 10 (9): (1272-1278). [PMID:31531196] |
| 122. Narayan S, Ramisetti S, Jaiswal AS, Law BK, Singh-Pillay A, Singh P, Amin S, Sharma AK.. (2019) ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells.. Eur J Med Chem, 161 (): (456-467). [PMID:30384048] |
| 123. Osborne J, Birchall K, Tsagris DJ, Lewis SJ, Smiljanic-Hurley E, Taylor DL, Levy A, Alessi DR, McIver EG.. (2019) Discovery of potent and selective 5-azaindazole inhibitors of leucine-rich repeat kinase 2 (LRRK2) - Part 1.. Bioorg Med Chem Lett, 29 (4): (668-673). [PMID:30554956] |
| 124. Michalak B, Piwowarski JP, Granica S, Waltenberger B, Atanasov AG, Khan SY, Breuss JM, Uhrin P, ?y?yńska-Granica B, Stojakowska A, Stuppner H, Kiss AK.. (2019) Eupatoriopicrin Inhibits Pro-inflammatory Functions of Neutrophils via Suppression of IL-8 and TNF-alpha Production and p38 and ERK 1/2 MAP Kinases.. J Nat Prod, 82 (2): (375-385). [PMID:30653318] |
| 125. Zhang M, Jiang L, Tao J, Pan Z, He M, Su D, He G, Jiang Q.. (2019) Design, synthesis and biological evaluation of 4-aniline-thieno[2,3-d]pyrimidine derivatives as MNK1 inhibitors against renal cell carcinoma and nasopharyngeal carcinoma.. Bioorg Med Chem, 27 (11): (2268-2279). [PMID:31014565] |
| 126. Liang X, Zang J, Li X, Tang S, Huang M, Geng M, Chou CJ, Li C, Cao Y, Xu W, Liu H, Zhang Y.. (2019) Discovery of Novel Janus Kinase (JAK) and Histone Deacetylase (HDAC) Dual Inhibitors for the Treatment of Hematological Malignancies.. J Med Chem, 62 (8): (3898-3923). [PMID:30901208] |
| 127. Tang G, Liu L, Wang X, Pan Z.. (2019) Discovery of 7H-pyrrolo[2,3-d]pyrimidine derivatives as selective covalent irreversible inhibitors of interleukin-2-inducible T-cell kinase (Itk).. Eur J Med Chem, 173 (): (167-183). [PMID:30999237] |
| 128. Harris PA, Faucher N, George N, Eidam PM, King BW, White GV, Anderson NA, Bandyopadhyay D, Beal AM, Beneton V, Berger SB, Campobasso N, Campos S, Capriotti CA, Cox JA, Daugan A, Donche F, Fouchet MH, Finger JN, Geddes B, Gough PJ, Grondin P, Hoffman BL, Hoffman SJ, Hutchinson SE, Jeong JU, Jigorel E, Lamoureux P, Leister LK, Lich JD, Mahajan MK, Meslamani J, Mosley JE, Nagilla R, Nassau PM, Ng SL, Ouellette MT, Pasikanti KK, Potvain F, Reilly MA, Rivera EJ, Sautet S, Schaeffer MC, Sehon CA, Sun H, Thorpe JH, Totoritis RD, Ward P, Wellaway N, Wisnoski DD, Woolven JM, Bertin J, Marquis RW.. (2019) Discovery and Lead-Optimization of 4,5-Dihydropyrazoles as Mono-Kinase Selective, Orally Bioavailable and Efficacious Inhibitors of Receptor Interacting Protein 1 (RIP1) Kinase.. J Med Chem, 62 (10): (5096-5110). [PMID:31013427] |
| 129. Heng H, Wang Z, Li H, Huang Y, Lan Q, Guo X, Zhang L, Zhi Y, Cai J, Qin T, Xiang L, Wang S, Chen Y, Lu T, Lu S.. (2019) Combining structure- and property-based optimization to identify selective FLT3-ITD inhibitors with good antitumor efficacy in AML cell inoculated mouse xenograft model.. Eur J Med Chem, 176 (): (248-267). [PMID:31103903] |
| 130. Huang MR, Hsu YL, Lin TC, Cheng TJ, Li LW, Tseng YW, Chou YS, Liu JH, Pan SH, Fang JM, Wong CH.. (2019) Structure-guided development of purine amide, hydroxamate, and amidoxime for the inhibition of non-small cell lung cancer.. Eur J Med Chem, 181 (): (111551-111551). [PMID:31376567] |
| 131. Nagiec MM, Duvall JR, Skepner AP, Howe EA, Bastien J, Comer E, Marie JC, Johnston SE, Negri J, Eichhorn M, Vantourout J, Clish C, Musunuru K, Foley M, Perez JR, Palmer MAJ.. (2018) Novel tricyclic glycal-based TRIB1 inducers that reprogram LDL metabolism in hepatic cells.. Medchemcomm, 9 (11): (1831-1842). [PMID:30542533] |
| 132. Qi B, Zhong L, He J, Zhang H, Li F, Wang T, Zou J, Lin YX, Zhang C, Guo X, Li R, Shi J.. (2019) Discovery of Inhibitors of Aurora/PLK Targets as Anticancer Agents.. J Med Chem, 62 (17): (7697-7707). [PMID:31381325] |
| 133. Jang J, Son JB, To C, Bahcall M, Kim SY, Kang SY, Mushajiang M, Lee Y, J?nne PA, Choi HG, Gray NS.. (2017) Discovery of a potent dual ALK and EGFR T790M inhibitor.. Eur J Med Chem, 136 (): (497-510). [PMID:28528303] |
| 134. Oukoloff K, Coquelle N, Bartolini M, Naldi M, Le Guevel R, Bach S, Josselin B, Ruchaud S, Catto M, Pisani L, Denora N, Iacobazzi RM, Silman I, Sussman JL, Buron F, Colletier JP, Jean L, Routier S, Renard PY.. (2019) Design, biological evaluation and X-ray crystallography of nanomolar multifunctional ligands targeting simultaneously acetylcholinesterase and glycogen synthase kinase-3.. Eur J Med Chem, 168 (): (58-77). [PMID:30798053] |
| 135. Cai G, Yu W, Song D, Zhang W, Guo J, Zhu J, Ren Y, Kong L.. (2019) Discovery of fluorescent coumarin-benzo[b]thiophene 1, 1-dioxide conjugates as mitochondria-targeting antitumor STAT3 inhibitors.. Eur J Med Chem, 174 (): (236-251). [PMID:31048139] |
| 136. Recagni M, Greco ML, Milelli A, Minarini A, Zaffaroni N, Folini M, Sissi C.. (2019) Distinct biological responses of metastatic castration resistant prostate cancer cells upon exposure to G-quadruplex interacting naphthalenediimide derivatives.. Eur J Med Chem, 177 (): (401-413). [PMID:31158753] |
| 137. Bensinger D, Stubba D, Cremer A, Kohl V, Wa?mer T, Stuckert J, Engemann V, Stegmaier K, Schmitz K, Schmidt B.. (2019) Virtual Screening Identifies Irreversible FMS-like Tyrosine Kinase 3 Inhibitors with Activity toward Resistance-Conferring Mutations.. J Med Chem, 62 (5): (2428-2446). [PMID:30742435] |
| 138. Wang Q, Dai Y, Ji Y, Shi H, Guo Z, Chen D, Chen Y, Peng X, Gao Y, Wang X, Chen L, Jiang Y, Geng M, Shen J, Ai J, Xiong B.. (2019) Discovery and optimization of a series of 3-substituted indazole derivatives as multi-target kinase inhibitors for the treatment of lung squamous cell carcinoma.. Eur J Med Chem, 163 (): (671-689). [PMID:30572178] |
| 139. Xie Z, Wu K, Wang Y, Pan Y, Chen B, Cheng D, Pan S, Guo T, Du X, Fang L, Wang X, Ye F.. (2020) Discovery of 4,6-pyrimidinediamine derivatives as novel dual EGFR/FGFR inhibitors aimed EGFR/FGFR1-positive NSCLC.. Eur J Med Chem, 187 (): (111943-111943). [PMID:31846829] |
| 140. Jung O, Lee J, Lee YJ, Yun JM, Son YJ, Cho JY, Ryou C, Lee SY.. (2016) Timosaponin AIII inhibits migration and invasion of A549 human non-small-cell lung cancer cells via attenuations of MMP-2 and MMP-9 by inhibitions of ERK1/2, Src/FAK and β-catenin signaling pathways.. Bioorg Med Chem Lett, 26 (16): (3963-3967). [PMID:27422337] |
| 141. Jnawali HN, Jeon D, Jeong MC, Lee E, Jin B, Ryoo S, Yoo J, Jung ID, Lee SJ, Park YM, Kim Y.. (2016) Antituberculosis Activity of a Naturally Occurring Flavonoid, Isorhamnetin.. J Nat Prod, 79 (4): (961-969). [PMID:26974691] |
| 142. Zak M,Hanan EJ,Lupardus P,Brown DG,Robinson C,Siu M,Lyssikatos JP,Romero FA,Zhao G,Kellar T,Mendonca R,Ray NC,Goodacre SC,Crackett PH,McLean N,Hurley CA,Yuen PW,Cheng YX,Liu X,Liimatta M,Kohli PB,Nonomiya J,Salmon G,Buckley G,Lloyd J,Gibbons P,Ghilardi N,Kenny JR,Johnson A. (2019) Discovery of a class of highly potent Janus Kinase 1/2 (JAK1/2) inhibitors demonstrating effective cell-based blockade of IL-13 signaling.. Bioorg Med Chem Lett, 29 (12.0): (1522-1531). [PMID:30981576] |
| 143. Grant CV,Cai S,Risinger AL,Liang H,O'Keefe BR,Doench JG,Cichewicz RH,Mooberry SL. (2020) CRISPR-Cas9 Genome-Wide Knockout Screen Identifies Mechanism of Selective Activity of Dehydrofalcarinol in Mesenchymal Stem-like Triple-Negative Breast Cancer Cells.. J Nat Prod, 83 (10.0): (3080-3092). [PMID:33021790] |
| 144. Panknin O,Wagenfeld A,Bone W,Bender E,Nowak-Reppel K,Fernández-Montalván AE,Nubbemeyer R,B?urle S,Ring S,Schmees N,Prien O,Sch?fer M,Friedrich C,Zollner TM,Steinmeyer A,Mueller T,Langer G. (2020) Discovery and Characterization of BAY 1214784, an Orally Available Spiroindoline Derivative Acting as a Potent and Selective Antagonist of the Human Gonadotropin-Releasing Hormone Receptor as Proven in a First-In-Human Study in Postmenopausal Women.. J Med Chem, 63 (20): (11854-11881). [PMID:32960053] |
| 145. Matheson, Christopher J., Coxon, Christopher R., Bayliss, Richard, Boxall, Kathy, Carbain, Benoit, Fry, Andrew M., Hardcastle, Ian R., Harnor, Suzannah J., Mas-Droux, Corine, Newell, David R., Richards, Mark W., Sivaprakasam, Mangaleswaran, Turner, David, Griffin, Roger J., Golding, Bernard T., Cano, Celine. (2020) 2-Arylamino-6-ethynylpurines are cysteine-targeting irreversible inhibitors of Nek2 kinase. RSC Med Chem, 11 (6): (707-731). [PMID:33479670] |
| 146. Jiang X,Zhou J,Wang Y,Chen L,Duan Y,Huang J,Liu C,Chen Y,Liu W,Sun H,Feng F,Qu W. (2020) Rational design and biological evaluation of a new class of thiazolopyridyl tetrahydroacridines as cholinesterase and GSK-3 dual inhibitors for Alzheimer's disease.. Eur J Med Chem, 207 (): (112751-112751). [PMID:32950908] |
| 147. Ding X,Stasi LP,Ho MH,Zhao B,Wang H,Long K,Xu Q,Sang Y,Sun C,Hu H,Yu H,Wan Z,Wang L,Edge C,Liu Q,Li Y,Dong K,Guan X,Tattersall FD,Reith AD,Ren F. (2018) Discovery of 4-ethoxy-7H-pyrrolo[2,3-d]pyrimidin-2-amines as potent, selective and orally bioavailable LRRK2 inhibitors.. Bioorg Med Chem Lett, 28 (9.0): (1615-1620). [PMID:29588215] |
| 148. Kaoud TS,Mohassab AM,Hassan HA,Yan C,Van Ravenstein SX,Abdelhamid D,Dalby KN,Abdel-Aziz M. (2020) NO-releasing STAT3 inhibitors suppress BRAF-mutant melanoma growth.. Eur J Med Chem, 186 (): (111885-111885). [PMID:31784187] |
| 149. Elwaie TA,Abbas SE,Aly EI,George RF,Ali H,Kraiouchkine N,Abdelwahed KS,Fandy TE,El Sayed KA,Abd Elmageed ZY,Ali HI. (2020) HER2 Kinase-Targeted Breast Cancer Therapy: Design, Synthesis, and In Vitro and In Vivo Evaluation of Novel Lapatinib Congeners as Selective and Potent HER2 Inhibitors with Favorable Metabolic Stability.. J Med Chem, 63 (24.0): (15906-15945). [PMID:33314925] |
| 150. Jiang X,Zhou J,Wang Y,Liu X,Xu K,Xu J,Feng F,Sun H. (2021) PROTACs suppression of GSK-3β, a crucial kinase in neurodegenerative diseases.. Eur J Med Chem, 210 (): (112949-112949). [PMID:33097303] |
| 151. Rojas-Prats E,Martinez-Gonzalez L,Gonzalo-Consuegra C,Liachko NF,Perez C,Ramírez D,Kraemer BC,Martin-Requero á,Perez DI,Gil C,de Lago E,Martinez A. (2021) Targeting nuclear protein TDP-43 by cell division cycle kinase 7 inhibitors: A new therapeutic approach for amyotrophic lateral sclerosis.. Eur J Med Chem, 210 (): (112968-112968). [PMID:33139113] |
| 152. Kraj?ovi?ová S, Jorda R, Vanda D, Soural M, Kry?tof V.. (2021) 1,4,6-Trisubstituted imidazo[4,5-c]pyridines as inhibitors of Bruton's tyrosine kinase.. Eur J Med Chem, 211 (): (113094-113094). [PMID:33340912] |
首页
400-620-6333
危险品化学品经营许可证（带存储）