CDK5 Mouse mAb

    应用:
  • Flow Cytometry
  • IF/ICC
  • IHC
  • WB
功能和特点
  • 宿主种属: 小鼠(Mouse)
  • 种属反应性: 人(Human), 大鼠(Rat), 小鼠(Mouse)
  • 亚型: Mouse IgG1
  • 克隆号: 1552CT262.105.8
  • 偶联: Unconjugated
有货

库存信息

关闭

库存信息

关闭

库存信息

关闭

库存信息

关闭
货号 (SKU) 包装规格 是否现货 价格 数量
Ab095769-10μl
10μl 现货 Stock Image
Ab095769-50μl
50μL 现货 Stock Image
Ab095769-100μl
100μL 现货 Stock Image
Ab095769-1ml
1ml 期货 Stock Image

基本信息

产品名称 CDK5 Mouse mAb
别名 周期素依赖性激酶5单克隆抗体 | CDK5小鼠单克隆抗体 | CDK5小鼠单抗
英文别名 Cdk 5 antibody | Cdk5 antibody | CDK5_HUMAN antibody | Cell division protein kinase 5 antibody | Crk6 antibody | Cyclin dependent kinase 5 antibody | Cyclin-dependent kinase 5 antibody | Protein kinase CDK5 splicing antibody | PSSALRE antibody | Serine th
规格或纯度 ExactAb™, Validated, Carrier Free, 0.5mg/mL
宿主种属 小鼠(Mouse)
特异性 CDK5
种属反应性 人(Human),大鼠(Rat),小鼠(Mouse)
免疫原 A recombinant protein of human CDK5 ( AA 1-292).
阳性对照 WB: A431, K562, HeLa, NIH/3T3, A549, Jurkat, MCF7 and HEK293 cell lysates. IHC: Human skeletal muscle tissue. IF/ICC: A549 cells. Flow: K562 cells.
偶联 Unconjugated

产品属性

克隆类型 单克隆抗体
克隆号 1552CT262.105.8
Format Whole IgG
亚型 Mouse IgG1
轻链亚型 kappa
SDS-PAGE 150 kDa
纯化方法 Protein G purified
物理外观 Liquid
储存缓冲液 10mM PBS, 0.09% Sodium azide, pH7.4.
防腐剂 0.09% Sodium azide.
浓度 0.5mg/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 4°C 短期储存(1-2 周)。-20°C下长期保存(24个月)。收货后建议分装。避免冷冻/解冻循环。
分子类型 抗体

图片

CDK5 Mouse mAb (Ab095769) - Western Blot
All lanes: CDK5 Mouse mAb (Ab095769) at 1/1000 dilution
Samples: Lysates at 20 µg per lane
Secondary: Goat Anti-Mouse IgG H&L (HRP) (Ab138040) at 1/40000 dilution

Predicted band size: 33 kDa
Observed band size: 30 kDa
Exposure time: 11.9 s

CDK5 Mouse mAb (Ab095769) - ICC/IF
Immunofluorescent analysis of 4% paraformaldehyde-fixed, 0.1% Triton X-100 permeabilized A549 (human lung adenocarcinoma epithelial cell line) cells labeling CDK5 with CDK5 Mouse mAb (Ab095769) at 1/25 dilution, followed by Dylight® 488-conjugated goat anti-mouse IgG secondary antibody at 1/200 dilution (green). Immunofluorescence image showing cytoplasm staining on A549 cell line. Cytoplasmic actin is detected with Dylight® 554 Phalloidin at 1/100 dilution (red). The nuclear counter stain is DAPI (blue).

CDK5 Mouse mAb (Ab095769) - IHC
CDK5 Mouse mAb (Ab095769) staining CDK5 in human skeletal muscle sections by Immunohistochemistry (paraformaldehyde - fixed, paraffin - embedded sections). Tissue was fixed with formaldehyde and blocked with 3% BSA for 0.5 hour at room temperature; antigen retrieval was by heat mediation with a citrate buffer (pH 6). Samples were incubated with primary antibody (1/25) for 1 hours at 37°C. A undiluted biotinylated goat polyvalent antibody was used as the secondary antibody.

CDK5 Mouse mAb (Ab095769) - Flow Cytometry
Overlay histogram showing K562 cells stained with CDK5 Mouse mAb (Ab095769) (green line). The cells were fixed with 2% paraformaldehyde (10 min) and then permeabilized with 90% methanol for 10 min. The cells were then incubated in 2% bovine serum albumin to block non-specific protein-protein interactions followed by CDK5 Mouse mAb (Ab095769) (1/25 dilution) for 60 min at 37ºC. The secondary antibody was used Goat-Anti-Mouse IgG, DyLight® 488 Conjugated Highly Cross-Adsorbed at 1/400 dilution for 40 min at 37ºC. Isotype control antibody (blue line) was mouse IgG1 used under the same conditions. Acquisition of >10000 events was performed.

关联靶点(人)

CDK5 Tchem 细胞周期蛋白依赖性类激酶 5(Cyclin-dependent-like kinase 5) (0 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
CDK5 Tchem Cyclin-dependent kinase 5 (3021 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CDK5 Tchem Cyclin-dependent kinase 5/CDK5 activator 1 (3697 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CDK5 Tchem Cyclin-T1/Cyclin-dependent-like kinase 5 (5 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID

作用机制

作用机制 Action Type target ID Target Name Target Type Target Organism Binding Site Name 参考文献

安全和危险性(GHS)

质量标准

应用

应用名称 稀释比例
IHC

1/100-1/500

Flow Cytometry

1/25

WB

1/2000

IF/ICC

1/25

质检证书(CoA,COO,BSE/TSE 和分析图谱)

C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:

通过匹配包装上的批号来查找并下载产品的 COA,每批产品都进行了严格的验证,您可放心使用!

找到3个结果

批号(Lot Number) 证书类型 日期 货号
ZJ24F1011871 分析证书 24-10-12 Ab095769
ZJ23F1001320 分析证书 23-10-18 Ab095769
ZJ23F1001319 分析证书 23-10-18 Ab095769

参考文献

1. 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] [10.1016/s0960-894x(03)00648-6]
2. Tarricone C, Dhavan R, Peng J, Areces LB, Tsai LH, Musacchio A.  (2001)  Structure and regulation of the CDK5-p25(nck5a) complex..  Mol Cell,  (3): (657-69).  [PMID:11583627]
3. 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]
4. Martin MP, Olesen SH, Georg GI, Schönbrunn E.  (2013)  Cyclin-dependent kinase inhibitor dinaciclib interacts with the acetyl-lysine recognition site of bromodomains..  ACS Chem Biol,  (11): (2360-5).  [PMID:24007471]
5. Cirstea D, Hideshima T, Santo L, Eda H, Mishima Y, Nemani N, Hu Y, Mimura N, Cottini F, Gorgun G et al..  (2013)  Small-molecule multi-targeted kinase inhibitor RGB-286638 triggers P53-dependent and -independent anti-multiple myeloma activity through inhibition of transcriptional CDKs..  Leukemia,  27  (12): (2366-75).  [PMID:23807770]
6. 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]
7. Leost M, Schultz C, Link A, Wu YZ, Biernat J, Mandelkow EM, Bibb JA, Snyder GL, Greengard P, Zaharevitz DW et al..  (2000)  Paullones are potent inhibitors of glycogen synthase kinase-3beta and cyclin-dependent kinase 5/p25..  Eur J Biochem,  267  (19): (5983-94).  [PMID:10998059]
8. 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]
9. Polychronopoulos P, Magiatis P, Skaltsounis AL, Myrianthopoulos V, Mikros E, Tarricone A, Musacchio A, Roe SM, Pearl L, Leost M et al..  (2004)  Structural basis for the synthesis of indirubins as potent and selective inhibitors of glycogen synthase kinase-3 and cyclin-dependent kinases..  J Med Chem,  47  (4): (935-46).  [PMID:14761195]
10. 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]
11. Pennati M, Campbell AJ, Curto M, Binda M, Cheng Y, Wang LZ, Curtin N, Golding BT, Griffin RJ, Hardcastle IR et al..  (2005)  Potentiation of paclitaxel-induced apoptosis by the novel cyclin-dependent kinase inhibitor NU6140: a possible role for survivin down-regulation..  Mol Cancer Ther,  (9): (1328-37).  [PMID:16170024]
12. 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,  (11): (691-9).  [PMID:18849971]
13. 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]
14. Changelian PS, Flanagan ME, Ball DJ, Kent CR, Magnuson KS, Martin WH, Rizzuti BJ, Sawyer PS, Perry BD, Brissette WH et al..  (2003)  Prevention of organ allograft rejection by a specific Janus kinase 3 inhibitor..  Science,  302  (5646): (875-8).  [PMID:14593182]
15. Squires MS, Feltell RE, Wallis NG, Lewis EJ, Smith DM, Cross DM, Lyons JF, Thompson NT.  (2009)  Biological characterization of AT7519, a small-molecule inhibitor of cyclin-dependent kinases, in human tumor cell lines..  Mol Cancer Ther,  (2): (324-32).  [PMID:19174555]
16. Lee SL, Hsu EC, Chou CC, Chuang HC, Bai LY, Kulp SK, Chen CS.  (2011)  Identification and characterization of a novel integrin-linked kinase inhibitor..  J Med Chem,  54  (18): (6364-74).  [PMID:21823616]
17. Burgy G, Tahtouh T, Durieu E, Foll-Josselin B, Limanton E, Meijer L, Carreaux F, Bazureau JP.  (2013)  Chemical synthesis and biological validation of immobilized protein kinase inhibitory Leucettines..  Eur J Med Chem,  62  (728-37).  [PMID:23454515]
18. Debdab M, Carreaux F, Renault S, Soundararajan M, Fedorov O, Filippakopoulos P, Lozach O, Babault L, Tahtouh T, Baratte B et al..  (2011)  Leucettines, a class of potent inhibitors of cdc2-like kinases and dual specificity, tyrosine phosphorylation regulated kinases derived from the marine sponge leucettamine B: modulation of alternative pre-RNA splicing..  J Med Chem,  54  (12): (4172-86).  [PMID:21615147]
19. Tahtouh T, Elkins JM, Filippakopoulos P, Soundararajan M, Burgy G, Durieu E, Cochet C, Schmid RS, Lo DC, Delhommel F et al..  (2012)  Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B..  J Med Chem,  55  (21): (9312-30).  [PMID:22998443]
20. Okuzumi T, Fiedler D, Zhang C, Gray DC, Aizenstein B, Hoffman R, Shokat KM.  (2009)  Inhibitor hijacking of Akt activation..  Nat Chem Biol,  (7): (484-93).  [PMID:19465931]
21. Milkiewicz KL, Aimone LD, Albom MS, Angeles TS, Chang H, Grobelny JV, Husten J, Losardo C, Miknyoczki S, Murthy S et al..  (2011)  Improvement in oral bioavailability of 2,4-diaminopyrimidine c-Met inhibitors by incorporation of a 3-amidobenzazepin-2-one group..  Bioorg Med Chem,  19  (21): (6274-84).  [PMID:21967808]
22. Choudhary C, Kumar C, Gnad F, Nielsen ML, Rehman M, Walther TC, Olsen JV, Mann M.  (2009)  Lysine acetylation targets protein complexes and co-regulates major cellular functions..  Science,  325  (5942): (834-40).  [PMID:19608861]
23. 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]
24. Goh KC, Novotny-Diermayr V, Hart S, Ong LC, Loh YK, Cheong A, Tan YC, Hu C, Jayaraman R, William AD et al..  (2012)  TG02, a novel oral multi-kinase inhibitor of CDKs, JAK2 and FLT3 with potent anti-leukemic properties..  Leukemia,  26  (2): (236-43).  [PMID:21860433]
25. Aronov AM, Tang Q, Martinez-Botella G, Bemis GW, Cao J, Chen G, Ewing NP, Ford PJ, Germann UA, Green J et al..  (2009)  Structure-guided design of potent and selective pyrimidylpyrrole inhibitors of extracellular signal-regulated kinase (ERK) using conformational control..  J Med Chem,  52  (20): (6362-8).  [PMID:19827834]
26. Hobson AD, Harris CM, van der Kam EL, Turner SC, Abibi A, Aguirre AL, Bousquet P, Kebede T, Konopacki DB, Gintant G et al..  (2015)  Discovery of A-971432, An Orally Bioavailable Selective Sphingosine-1-Phosphate Receptor 5 (S1P5) Agonist for the Potential Treatment of Neurodegenerative Disorders..  J Med Chem,  58  (23): (9154-70).  [PMID:26509640]
27. Bisi JE, Sorrentino JA, Roberts PJ, Tavares FX, Strum JC.  (2016)  Preclinical Characterization of G1T28: A Novel CDK4/6 Inhibitor for Reduction of Chemotherapy-Induced Myelosuppression..  Mol Cancer Ther,  15  (5): (783-93).  [PMID:26826116]
28. 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]
29. Paiva C, Godbersen JC, Soderquist RS, Rowland T, Kilmarx S, Spurgeon SE, Brown JR, Srinivasa SP, Danilov AV.  (2015)  Cyclin-Dependent Kinase Inhibitor P1446A Induces Apoptosis in a JNK/p38 MAPK-Dependent Manner in Chronic Lymphocytic Leukemia B-Cells..  PLoS ONE,  10  (11): (e0143685).  [PMID:26606677]
30. Jorda R, Havlíček L, Šturc A, Tušková D, Daumová L, Alam M, Škerlová J, Nekardová M, Peřina M, Pospíšil T et al..  (2019)  3,5,7-Substituted Pyrazolo[4,3- d]pyrimidine Inhibitors of Cyclin-Dependent Kinases and Their Evaluation in Lymphoma Models..  J Med Chem,  62  (9): (4606-4623).  [PMID:30943029] [10.1021/acs.jmedchem.9b00189]
31. Pomel V, Klicic J, Covini D, Church DD, Shaw JP, Roulin K, Burgat-Charvillon F, Valognes D, Camps M, Chabert C et al..  (2006)  Furan-2-ylmethylene thiazolidinediones as novel, potent, and selective inhibitors of phosphoinositide 3-kinase gamma..  J Med Chem,  49  (13): (3857-71).  [PMID:16789742]
32. Bettayeb K, Oumata N, Echalier A, Ferandin Y, Endicott JA, Galons H, Meijer L.  (2008)  CR8, a potent and selective, roscovitine-derived inhibitor of cyclin-dependent kinases..  Oncogene,  27  (44): (5797-807).  [PMID:18574471]
33. Xu R, Wang K, Rizzi JP, Huang H, Grina JA, Schlachter ST, Wang B, Wehn PM, Yang H, Dixon DD et al..  (2019)  3-[(1S,2S,3R)-2,3-Difluoro-1-hydroxy-7-methylsulfonylindan-4-yl]oxy-5-fluorobenzonitrile (PT2977), a Hypoxia-Inducible Factor 2α (HIF-2α) Inhibitor for the Treatment of Clear Cell Renal Cell Carcinoma..  J Med Chem,  62  (15): (6876-6893).  [PMID:31282155]
34. Cabrera DG, Horatscheck A, Wilson CR, Basarab G, Eyermann CJ, Chibale K.  (2018)  Plasmodial Kinase Inhibitors: License to Cure?.  J Med Chem,  61  (18): (8061-8077).  [PMID:29771541]
35. Su S, Yang Z, Gao H, Yang H, Zhu S, An Z, Wang J, Li Q, Chandarlapaty S, Deng H et al..  (2019)  Potent and Preferential Degradation of CDK6 via Proteolysis Targeting Chimera Degraders..  J Med Chem,  62  (16): (7575-7582).  [PMID:31330105]
36. Barlaam B, Casella R, Cidado J, Cook C, De Savi C, Dishington A, Donald CS, Drew L, Ferguson AD, Ferguson D et al..  (2020)  Discovery of AZD4573, a Potent and Selective Inhibitor of CDK9 That Enables Short Duration of Target Engagement for the Treatment of Hematological Malignancies..  J Med Chem,  63  (24): (15564-15590).  [PMID:33306391]
37. 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]
38. 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]
39. Xiao-Guang Bai,Dong-Ke Yu,Ju-Xian Wang,Hao Zhang,Hong-Wei He,Rong-Guang Shao,Xue-Mei Li,Yu-Cheng Wang.  (2012-10-06)  Design, synthesis and anticancer activity of 1-acyl-3-amino-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole derivatives..  Bioorganic & medicinal chemistry letters,  22  ((22)): (6947-6951).  [PMID:23036956]
40. Pevarello P, Brasca MG, Amici R, Orsini P, Traquandi G, Corti L, Piutti C, Sansonna P, Villa M, Pierce BS, Pulici M, Giordano P, Martina K, Fritzen EL, Nugent RA, Casale E, Cameron A, Ciomei M, Roletto F, Isacchi A, Fogliatto G, Pesenti E, Pastori W, Marsiglio A, Leach KL, Clare PM, Fiorentini F, Varasi M, Vulpetti A, Warpehoski MA..  (2004)  3-Aminopyrazole inhibitors of CDK2/cyclin A as antitumor agents. 1. Lead finding..  J Med Chem,  47  (13): (3367-3380).  [PMID:15189033] [10.1021/jm031145u]
41. Helal CJ, Sanner MA, Cooper CB, Gant T, Adam M, Lucas JC, Kang Z, Kupchinsky S, Ahlijanian MK, Tate B, Menniti FS, Kelly K, Peterson M..  (2004)  Discovery and SAR of 2-aminothiazole inhibitors of cyclin-dependent kinase 5/p25 as a potential treatment for Alzheimer's disease..  Bioorg Med Chem Lett,  14  (22): (5521-5525).  [PMID:15482916] [10.1016/j.bmcl.2004.09.006]
42. Mapelli M, Massimiliano L, Crovace C, Seeliger MA, Tsai LH, Meijer L, Musacchio A..  (2005)  Mechanism of CDK5/p25 binding by CDK inhibitors..  J Med Chem,  48  (3): (671-679).  [PMID:15689152] [10.1021/jm049323m]
43. Zhao H, Serby MD, Xin Z, Szczepankiewicz BG, Liu M, Kosogof C, Liu B, Nelson LT, Johnson EF, Wang S, Pederson T, Gum RJ, Clampit JE, Haasch DL, Abad-Zapatero C, Fry EH, Rondinone C, Trevillyan JM, Sham HL, Liu G..  (2006)  Discovery of potent, highly selective, and orally bioavailable pyridine carboxamide c-Jun NH2-terminal kinase inhibitors..  J Med Chem,  49  (15): (4455-4458).  [PMID:16854050] [10.1021/jm060465l]
44. Kim ND, Yoon J, Kim JH, Lee JT, Chon YS, Hwang MK, Ha I, Song WJ..  (2006)  Putative therapeutic agents for the learning and memory deficits of people with Down syndrome..  Bioorg Med Chem Lett,  16  (14): (3772-3776).  [PMID:16698266] [10.1016/j.bmcl.2006.04.042]
45. DiMauro EF, Newcomb J, Nunes JJ, Bemis JE, Boucher C, Buchanan JL, Buckner WH, Cee VJ, Chai L, Deak HL, Epstein LF, Faust T, Gallant P, Geuns-Meyer SD, Gore A, Gu Y, Henkle B, Hodous BL, Hsieh F, Huang X, Kim JL, Lee JH, Martin MW, Masse CE, 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, White RD, Zhao H, Zhu L, Zhu X..  (2006)  Discovery of aminoquinazolines as potent, orally bioavailable inhibitors of Lck: synthesis, SAR, and in vivo anti-inflammatory activity..  J Med Chem,  49  (19): (5671-5686).  [PMID:16970394] [10.1021/jm0605482]
46. Cee VJ, Albrecht BK, Geuns-Meyer S, Hughes P, Bellon S, Bready J, Caenepeel S, Chaffee SC, Coxon A, Emery M, Fretland J, Gallant P, Gu Y, Hodous BL, Hoffman D, Johnson RE, Kendall R, Kim JL, Long AM, McGowan D, Morrison M, Olivieri PR, Patel VF, Polverino A, Powers D, Rose P, Wang L, Zhao H..  (2007)  Alkynylpyrimidine amide derivatives as potent, selective, and orally active inhibitors of Tie-2 kinase..  J Med Chem,  50  (4): (627-640).  [PMID:17253679] [10.1021/jm061112p]
47. Shiradkar MR, Akula KC, Dasari V, Baru V, Chiningiri B, Gandhi S, Kaur R..  (2007)  Clubbed thiazoles by MAOS: a novel approach to cyclin-dependent kinase 5/p25 inhibitors as a potential treatment for Alzheimer's disease..  Bioorg Med Chem,  15  (7): (2601-2610).  [PMID:17291769] [10.1016/j.bmc.2007.01.043]
48. Potashman MH, Bready J, Coxon A, DeMelfi TM, DiPietro L, Doerr N, Elbaum D, Estrada J, Gallant P, Germain J, Gu Y, Harmange JC, Kaufman SA, Kendall R, Kim JL, Kumar GN, Long AM, Neervannan S, Patel VF, Polverino A, Rose P, Plas Sv, Whittington D, Zanon R, Zhao H..  (2007)  Design, synthesis, and evaluation of orally active benzimidazoles and benzoxazoles as vascular endothelial growth factor-2 receptor tyrosine kinase inhibitors..  J Med Chem,  50  (18): (4351-4373).  [PMID:17696416] [10.1021/jm070034i]
49. Conchon E, Anizon F, Aboab B, Prudhomme M..  (2007)  Synthesis and biological activities of new checkpoint kinase 1 inhibitors structurally related to granulatimide..  J Med Chem,  50  (19): (4669-4680).  [PMID:17722905] [10.1021/jm070664k]
50. Shiradkar MR, Padhalingappa MB, Bhetalabhotala S, Akula KC, Tupe DA, Pinninti RR, Thummanagoti S..  (2007)  A novel approach to cyclin-dependent kinase 5/p25 inhibitors: A potential treatment for Alzheimer's disease..  Bioorg Med Chem,  15  (19): (6397-6406).  [PMID:17643991] [10.1016/j.bmc.2007.06.053]
51. Zhong W, Liu H, Kaller MR, Henley C, Magal E, Nguyen T, Osslund TD, Powers D, Rzasa RM, Wang HL, Wang W, Xiong X, Zhang J, Norman MH..  (2007)  Design and synthesis of quinolin-2(1H)-one derivatives as potent CDK5 inhibitors..  Bioorg Med Chem Lett,  17  (19): (5384-5389).  [PMID:17709247] [10.1016/j.bmcl.2007.07.045]
52. Hamann M, Alonso D, Martín-Aparicio E, Fuertes A, Pérez-Puerto MJ, Castro A, Morales S, Navarro ML, Del Monte-Millán M, Medina M, Pennaka H, Balaiah A, Peng J, Cook J, Wahyuono S, Martínez A..  (2007)  Glycogen synthase kinase-3 (GSK-3) inhibitory activity and structure-activity relationship (SAR) studies of the manzamine alkaloids. Potential for Alzheimer's disease..  J Nat Prod,  70  (9): (1397-1405).  [PMID:17708655] [10.1021/np060092r]
53. Echalier A, Bettayeb K, Ferandin Y, Lozach O, Clément M, Valette A, Liger F, Marquet B, Morris JC, Endicott JA, Joseph B, Meijer L..  (2008)  Meriolins (3-(pyrimidin-4-yl)-7-azaindoles): synthesis, kinase inhibitory activity, cellular effects, and structure of a CDK2/cyclin A/meriolin complex..  J Med Chem,  51  (4): (737-751).  [PMID:18232649] [10.1021/jm700940h]
54. 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] [10.1021/jm701095m]
55. 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] [10.1021/jm7010996]
56. Stukenbrock H, Mussmann R, Geese M, Ferandin Y, Lozach O, Lemcke T, Kegel S, Lomow A, Burk U, Dohrmann C, Meijer L, Austen M, Kunick C..  (2008)  9-cyano-1-azapaullone (cazpaullone), a glycogen synthase kinase-3 (GSK-3) inhibitor activating pancreatic beta cell protection and replication..  J Med Chem,  51  (7): (2196-2207).  [PMID:18345612] [10.1021/jm701582f]
57. Wyatt PG, Woodhead AJ, Berdini V, Boulstridge JA, Carr MG, Cross DM, Davis DJ, Devine LA, Early TR, Feltell RE, Lewis EJ, McMenamin RL, Navarro EF, O'Brien MA, O'Reilly M, Reule M, Saxty G, Seavers LC, Smith DM, Squires MS, Trewartha G, Walker MT, Woolford AJ..  (2008)  Identification of N-(4-piperidinyl)-4-(2,6-dichlorobenzoylamino)-1H-pyrazole-3-carboxamide (AT7519), a novel cyclin dependent kinase inhibitor using fragment-based X-ray crystallography and structure based drug design..  J Med Chem,  51  (16): (4986-4999).  [PMID:18656911] [10.1021/jm800382h]
58. Feng Y, Yin Y, Weiser A, Griffin E, Cameron MD, Lin L, Ruiz C, Schürer SC, Inoue T, Rao PV, Schröter 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] [10.1021/jm800986w]
59. 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] [10.1021/jm8006189]
60. Popowycz F, Fournet G, Schneider C, Bettayeb K, Ferandin Y, Lamigeon C, Tirado OM, Mateo-Lozano S, Notario V, Colas P, Bernard P, Meijer L, Joseph B..  (2009)  Pyrazolo[1,5-a]-1,3,5-triazine as a purine bioisostere: access to potent cyclin-dependent kinase inhibitor (R)-roscovitine analogue..  J Med Chem,  52  (3): (655-663).  [PMID:19128055] [10.1021/jm801340z]
61. Koo KA, Kim ND, Chon YS, Jung MS, Lee BJ, Kim JH, Song WJ..  (2009)  QSAR analysis of pyrazolidine-3,5-diones derivatives as Dyrk1A inhibitors..  Bioorg Med Chem Lett,  19  (8): (2324-2328).  [PMID:19282176] [10.1016/j.bmcl.2009.02.062]
62. Bouchikhi F, Anizon F, Moreau P..  (2009)  Synthesis, kinase inhibitory potencies and in vitro antiproliferative activity of isoindigo and 7'-azaisoindigo derivatives substituted by Sonogashira cross-coupling..  Eur J Med Chem,  44  (6): (2705-2710).  [PMID:19232788] [10.1016/j.ejmech.2009.01.027]
63. Helal CJ, Kang Z, Lucas JC, Gant T, Ahlijanian MK, Schachter JB, Richter KE, Cook JM, Menniti FS, Kelly K, Mente S, Pandit J, Hosea N..  (2009)  Potent and cellularly active 4-aminoimidazole inhibitors of cyclin-dependent kinase 5/p25 for the treatment of Alzheimer's disease..  Bioorg Med Chem Lett,  19  (19): (5703-5707).  [PMID:19700321] [10.1016/j.bmcl.2009.08.019]
64. Beauchard A, Laborie H, Rouillard H, Lozach O, Ferandin Y, Le Guével R, Guguen-Guillouzo C, Meijer L, Besson T, Thiéry V..  (2009)  Synthesis and kinase inhibitory activity of novel substituted indigoids..  Bioorg Med Chem,  17  (17): (6257-6263).  [PMID:19665384] [10.1016/j.bmc.2009.07.051]
65. 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] [10.1016/j.bmcl.2009.09.010]
66. Almeida C, Eguereva E, Kehraus S, Siering C, König GM..  (2010)  Hydroxylated sclerosporin derivatives from the marine-derived fungus Cadophora malorum..  J Nat Prod,  73  (3): (476-478).  [PMID:20052971] [10.1021/np900608d]
67. Yu H, Jung Y, Kim H, Lee J, Oh CH, Yoo KH, Sim T, Hah JM..  (2010)  1,4-dihydropyrazolo[4,3-d]imidazole phenyl derivatives: a novel type II Raf kinase inhibitors..  Bioorg Med Chem Lett,  20  (12): (3805-3808).  [PMID:20466542] [10.1016/j.bmcl.2010.04.039]
68. 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] [10.1016/j.bmcl.2010.05.043]
69. Meijer L, Flajolet M, Greengard P..  (2004)  Pharmacological inhibitors of glycogen synthase kinase 3..  Trends Pharmacol Sci,  25  (9): (471-480).  [PMID:15559249] [10.1016/j.tips.2004.07.006]
70. Sridhar J, Akula N, Pattabiraman N..  (2006)  Selectivity and potency of cyclin-dependent kinase inhibitors..  AAPS J,  (1): (E204-E221).  [PMID:16584130] [10.1208/aapsj080125]
71. Barile E, De SK, Carlson CB, Chen V, Knutzen C, Riel-Mehan M, Yang L, Dahl R, Chiang G, Pellecchia M..  (2010)  Design, synthesis, and structure-activity relationships of 3-ethynyl-1H-indazoles as inhibitors of the phosphatidylinositol 3-kinase signaling pathway..  J Med Chem,  53  (23): (8368-8375).  [PMID:21062009] [10.1021/jm100825h]
72. Probst GD, Bowers S, Sealy JM, Truong AP, Hom RK, Galemmo RA, Konradi AW, Sham HL, Quincy DA, Pan H, Yao N, Lin M, Tóth G, Artis DR, Zmolek W, Wong K, Qin A, Lorentzen C, Nakamura DF, Quinn KP, Sauer JM, Powell K, Ruslim L, Wright S, Chereau D, Ren Z, Anderson JP, Bard F, Yednock TA, Griswold-Prenner I..  (2011)  Highly selective c-Jun N-terminal kinase (JNK) 2 and 3 inhibitors with in vitro CNS-like pharmacokinetic properties prevent neurodegeneration..  Bioorg Med Chem Lett,  21  (1): (315-319).  [PMID:21112785] [10.1016/j.bmcl.2010.11.010]
73. Jain P, Flaherty PT, Yi S, Chopra I, Bleasdell G, Lipay J, Ferandin Y, Meijer L, Madura JD..  (2011)  Design, synthesis, and testing of an 6-O-linked series of benzimidazole based inhibitors of CDK5/p25..  Bioorg Med Chem,  19  (1): (359-373).  [PMID:21144757] [10.1016/j.bmc.2010.11.022]
74. Laha JK, Zhang X, Qiao L, Liu M, Chatterjee S, Robinson S, Kosik KS, Cuny GD..  (2011)  Structure-activity relationship study of 2,4-diaminothiazoles as Cdk5/p25 kinase inhibitors..  Bioorg Med Chem Lett,  21  (7): (2098-2101).  [PMID:21353545] [10.1016/j.bmcl.2011.01.140]
75. Jorda R, Havlícek L, McNae IW, Walkinshaw MD, Voller J, Sturc A, Navrátilová J, Kuzma M, Mistrík M, Bártek J, Strnad M, Krystof V..  (2011)  Pyrazolo[4,3-d]pyrimidine bioisostere of roscovitine: evaluation of a novel selective inhibitor of cyclin-dependent kinases with antiproliferative activity..  J Med Chem,  54  (8): (2980-2993).  [PMID:21417417] [10.1021/jm200064p]
76. Yun H, Heo HY, Kim HH, DooKim N, Seol W..  (2011)  Identification of chemicals to inhibit the kinase activity of leucine-rich repeat kinase 2 (LRRK2), a Parkinson's disease-associated protein..  Bioorg Med Chem Lett,  21  (10): (2953-2957).  [PMID:21474311] [10.1016/j.bmcl.2011.03.061]
77. Shiradkar M, Thomas J, Kanase V, Dighe R..  (2011)  Studying synergism of methyl linked cyclohexyl thiophenes with triazole: synthesis and their cdk5/p25 inhibition activity..  Eur J Med Chem,  46  (6): (2066-2074).  [PMID:21420204] [10.1016/j.ejmech.2011.02.059]
78. Lebar MD, Hahn KN, Mutka T, Maignan P, McClintock JB, Amsler CD, van Olphen A, Kyle DE, Baker BJ..  (2011)  CNS and antimalarial activity of synthetic meridianin and psammopemmin analogs..  Bioorg Med Chem,  19  (19): (5756-5762).  [PMID:21907583] [10.1016/j.bmc.2011.08.033]
79. 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] [10.1016/j.bmcl.2012.01.028]
80. Nguyen TB, Lozach O, Surpateanu G, Wang Q, Retailleau P, Iorga BI, Meijer L, Guéritte F..  (2012)  Synthesis, biological evaluation, and molecular modeling of natural and unnatural flavonoidal alkaloids, inhibitors of kinases..  J Med Chem,  55  (6): (2811-2819).  [PMID:22352892] [10.1021/jm201727w]
81. Lo Monte F, Kramer T, Gu J, Anumala UR, Marinelli L, La Pietra V, Novellino E, Franco B, Demedts D, Van Leuven F, Fuertes A, Dominguez JM, Plotkin B, Eldar-Finkelman H, Schmidt B..  (2012)  Identification of glycogen synthase kinase-3 inhibitors with a selective sting for glycogen synthase kinase-3α..  J Med Chem,  55  (9): (4407-4424).  [PMID:22533818] [10.1021/jm300309a]
82. Malmström J, Viklund J, Slivo C, Costa A, Maudet M, Sandelin C, Hiller G, Olsson LL, Aagaard A, Geschwindner S, Xue Y, Vasänge M..  (2012)  Synthesis and structure-activity relationship of 4-(1,3-benzothiazol-2-yl)-thiophene-2-sulfonamides as cyclin-dependent kinase 5 (cdk5)/p25 inhibitors..  Bioorg Med Chem Lett,  22  (18): (5919-5923).  [PMID:22889803] [10.1016/j.bmcl.2012.07.068]
83. N'gompaza-Diarra J, Bettayeb K, Gresh N, Meijer L, Oumata N..  (2012)  Synthesis and biological evaluation of selective and potent cyclin-dependent kinase inhibitors..  Eur J Med Chem,  56  (210-216).  [PMID:22982525] [10.1016/j.ejmech.2012.08.033]
84. 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] [10.1021/jm200900q]
85. Tell V, Holzer M, Herrmann L, Mahmoud KA, Schächtele C, Totzke F, Hilgeroth A..  (2012)  Multitargeted drug development: Discovery and profiling of dihydroxy substituted 1-aza-9-oxafluorenes as lead compounds targeting Alzheimer disease relevant kinases..  Bioorg Med Chem Lett,  22  (22): (6914-6918).  [PMID:23039927] [10.1016/j.bmcl.2012.09.006]
86. 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] [10.1016/j.bmcl.2012.05.090]
87. 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] [10.1016/j.bmcl.2012.06.104]
88. Demange L, Abdellah FN, Lozach O, Ferandin Y, Gresh N, Meijer L, Galons H..  (2013)  Potent inhibitors of CDK5 derived from roscovitine: synthesis, biological evaluation and molecular modelling..  Bioorg Med Chem Lett,  23  (1): (125-131).  [PMID:23218601] [10.1016/j.bmcl.2012.10.141]
89. Myrianthopoulos V, Kritsanida M, Gaboriaud-Kolar N, Magiatis P, Ferandin Y, Durieu E, Lozach O, Cappel D, Soundararajan M, Filippakopoulos P, Sherman W, Knapp S, Meijer L, Mikros E, Skaltsounis AL..  (2013)  Novel Inverse Binding Mode of Indirubin Derivatives Yields Improved Selectivity for DYRK Kinases..  ACS Med Chem Lett,  (1): (22-26).  [PMID:23336033] [10.1021/ml300207a]
90. Garofalo AW, Adler M, Aubele DL, Bowers S, Franzini M, Goldbach E, Lorentzen C, Neitz RJ, Probst GD, Quinn KP, Santiago P, Sham HL, Tam D, Truong AP, Ye XM, Ren Z..  (2013)  Novel cinnoline-based inhibitors of LRRK2 kinase activity..  Bioorg Med Chem Lett,  23  (1): (71-74).  [PMID:23219325] [10.1016/j.bmcl.2012.11.021]
91. 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] [10.1016/j.bmcl.2013.01.110]
92. Garofalo AW, Adler M, Aubele DL, Brigham EF, Chian D, Franzini M, Goldbach E, Kwong GT, Motter R, Probst GD, Quinn KP, Ruslim L, Sham HL, Tam D, Tanaka P, Truong AP, Ye XM, Ren Z..  (2013)  Discovery of 4-alkylamino-7-aryl-3-cyanoquinoline LRRK2 kinase inhibitors..  Bioorg Med Chem Lett,  23  (7): (1974-1977).  [PMID:23453068] [10.1016/j.bmcl.2013.02.041]
93. Franzini M, Ye XM, Adler M, Aubele DL, Garofalo AW, Gauby S, Goldbach E, Probst GD, Quinn KP, Santiago P, Sham HL, Tam D, Truong A, Ren Z..  (2013)  Triazolopyridazine LRRK2 kinase inhibitors..  Bioorg Med Chem Lett,  23  (7): (1967-1973).  [PMID:23454015] [10.1016/j.bmcl.2013.02.043]
94. Schonbrunn E, Betzi S, Alam R, Martin MP, Becker A, Han H, Francis R, Chakrasali R, Jakkaraj S, Kazi A, Sebti SM, Cubitt CL, Gebhard AW, Hazlehurst LA, Tash JS, Georg GI..  (2013)  Development of highly potent and selective diaminothiazole inhibitors of cyclin-dependent kinases..  J Med Chem,  56  (10): (3768-3782).  [PMID:23600925] [10.1021/jm301234k]
95. 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] [10.1016/j.bmcl.2013.02.065]
96. Shrestha S, Natarajan S, Park JH, Lee DY, Cho JG, Kim GS, Jeon YJ, Yeon SW, Yang DC, Baek NI..  (2013)  Potential neuroprotective flavonoid-based inhibitors of CDK5/p25 from Rhus parviflora..  Bioorg Med Chem Lett,  23  (18): (5150-5154).  [PMID:23927974] [10.1016/j.bmcl.2013.07.020]
97. Yoshida K, Itoyama R, Yamahira M, Tanaka J, Loaëc N, Lozach O, Durieu E, Fukuda T, Ishibashi F, Meijer L, Iwao M..  (2013)  Synthesis, resolution, and biological evaluation of atropisomeric (aR)- and (aS)-16-methyllamellarins N: unique effects of the axial chirality on the selectivity of protein kinases inhibition..  J Med Chem,  56  (18): (7289-7301).  [PMID:23981088] [10.1021/jm400719y]
98. Blake JF, Gaudino JJ, De Meese J, Mohr P, Chicarelli M, Tian H, Garrey R, Thomas A, Siedem CS, Welch MB, Kolakowski G, Kaus R, Burkard M, Martinson M, Chen H, Dean B, Dudley DA, Gould SE, Pacheco P, Shahidi-Latham S, Wang W, West K, Yin J, Moffat J, Schwarz JB..  (2014)  Discovery of 5,6,7,8-tetrahydropyrido[3,4-d]pyrimidine inhibitors of Erk2..  Bioorg Med Chem Lett,  24  (12): (2635-2639).  [PMID:24813737] [10.1016/j.bmcl.2014.04.068]
99. Horbert R, Pinchuk B, Johannes E, Schlosser J, Schmidt D, Cappel D, Totzke F, Schächtele C, Peifer C..  (2015)  Optimization of potent DFG-in inhibitors of platelet derived growth factor receptorβ (PDGF-Rβ) guided by water thermodynamics..  J Med Chem,  58  (1): (170-182).  [PMID:25007344] [10.1021/jm500373x]
100. Tintori C, La Sala G, Vignaroli G, Botta L, Fallacara AL, Falchi F, Radi M, Zamperini C, Dreassi E, Dello Iacono L, Orioli D, Biamonti G, Garbelli M, Lossani A, Gasparrini F, Tuccinardi T, Laurenzana I, Angelucci A, Maga G, Schenone S, Brullo C, Musumeci F, Desogus A, Crespan E, Botta M..  (2015)  Studies on the ATP Binding Site of Fyn Kinase for the Identification of New Inhibitors and Their Evaluation as Potential Agents against Tauopathies and Tumors..  J Med Chem,  58  (11): (4590-4609).  [PMID:25923950] [10.1021/acs.jmedchem.5b00140]
101. Falke H, Chaikuad A, Becker A, Loaëc N, Lozach O, Abu Jhaisha S, Becker W, Jones PG, Preu L, Baumann K, Knapp S, Meijer L, Kunick C..  (2015)  10-iodo-11H-indolo[3,2-c]quinoline-6-carboxylic acids are selective inhibitors of DYRK1A..  J Med Chem,  58  (7): (3131-3143).  [PMID:25730262] [10.1021/jm501994d]
102. 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] [10.1016/j.bmc.2015.09.038]
103. 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] [10.1016/j.ejmech.2015.10.020]
104. Schiemann K, Mallinger A, Wienke D, Esdar C, Poeschke O, Busch M, Rohdich F, Eccles SA, Schneider R, Raynaud FI, Czodrowski P, Musil D, Schwarz D, Urbahns K, Blagg J..  (2016)  Discovery of potent and selective CDK8 inhibitors from an HSP90 pharmacophore..  Bioorg Med Chem Lett,  26  (5): (1443-1451).  [PMID:26852363] [10.1016/j.bmcl.2016.01.062]
105. Mariano M, Hartmann RW, Engel M..  (2016)  Systematic diversification of benzylidene heterocycles yields novel inhibitor scaffolds selective for Dyrk1A, Clk1 and CK2..  Eur J Med Chem,  112  (209-216).  [PMID:26896709] [10.1016/j.ejmech.2016.02.017]
106. Daydé-Cazals B, Fauvel B, Singer M, Feneyrolles C, Bestgen B, Gassiot F, Spenlinhauer A, Warnault P, Van Hijfte N, Borjini N, Chevé G, Yasri A..  (2016)  Rational Design, Synthesis, and Biological Evaluation of 7-Azaindole Derivatives as Potent Focused Multi-Targeted Kinase Inhibitors..  J Med Chem,  59  (8): (3886-3905).  [PMID:27010810] [10.1021/acs.jmedchem.6b00087]
107. 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] [10.1016/j.bmcl.2016.04.079]
108. Laufer R, Li SW, Liu Y, Ng G, Lang Y, Feher M, Brokx R, Beletskaya I, Hodgson R, Mao G, Plotnikova O, Awrey DE, Mason JM, Wei X, Lin DC, Che Y, Kiarash R, Madeira B, Fletcher GC, Mak TW, Bray MR, Pauls HW..  (2016)  Discovery of 4-(4-aminopyrazolo[1,5-a][1,3,5]triazin-8-yl)benzamides as novel, highly potent and selective, orally bioavailable inhibitors of Tyrosine Threonine Kinase, TTK..  Bioorg Med Chem Lett,  26  (15): (3562-3566).  [PMID:27335255] [10.1016/j.bmcl.2016.06.021]
109. Sonawane YA, Taylor MA, Napoleon JV, Rana S, Contreras JI, Natarajan A..  (2016)  Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy..  J Med Chem,  59  (19): (8667-8684).  [PMID:27171036] [10.1021/acs.jmedchem.6b00150]
110. Rye CS, Chessum NE, Lamont S, Pike KG, Faulder P, Demeritt J, Kemmitt P, Tucker J, Zani L, Cheeseman MD, Isaac R, Goodwin L, Boros J, Raynaud F, Hayes A, Henley AT, de Billy E, Lynch CJ, Sharp SY, Te Poele R, Fee LO, Foote KM, Green S, Workman P, Jones K..  (2016)  Discovery of 4,6-disubstituted pyrimidines as potent inhibitors of the heat shock factor 1 (HSF1) stress pathway and CDK9..  Medchemcomm,  (8): (1580-1586).  [PMID:27746890] [10.1039/C6MD00159A]
111. Labrière C, Lozach O, Blairvacq M, Meijer L, Guillou C..  (2016)  Further investigation of Paprotrain: Towards the conception of selective and multi-targeted CNS kinase inhibitors..  Eur J Med Chem,  124  (920-934).  [PMID:27676471] [10.1016/j.ejmech.2016.08.069]
112. Klaeger S, Heinzlmeir S and Wilhelm M et al.  (2017)  The target landscape of clinical kinase drugs..  Science,  358  (6367): [PMID:29191878] [10.1126/science.aan4368]
113. 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] [10.1016/j.ejmech.2016.12.025]
114. Coxon CR, Anscombe E, Harnor SJ, Martin MP, Carbain B, Golding BT, Hardcastle IR, Harlow LK, Korolchuk S, Matheson CJ, Newell DR, Noble ME, Sivaprakasam M, Tudhope SJ, Turner DM, Wang LZ, Wedge SR, Wong C, Griffin RJ, Endicott JA, Cano C..  (2017)  Cyclin-Dependent Kinase (CDK) Inhibitors: Structure-Activity Relationships and Insights into the CDK-2 Selectivity of 6-Substituted 2-Arylaminopurines..  J Med Chem,  60  (5): (1746-1767).  [PMID:28005359] [10.1021/acs.jmedchem.6b01254]
115. 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] [10.1016/j.ejmech.2017.02.048]
116. Yu J, Ahn S, Kim HJ, Lee M, Ahn S, Kim J, Jin SH, Lee E, Kim G, Cheong JH, Jacobson KA, Jeong LS, Noh M..  (2017)  Polypharmacology of N6-(3-Iodobenzyl)adenosine-5'-N-methyluronamide (IB-MECA) and Related A3 Adenosine Receptor Ligands: Peroxisome Proliferator Activated Receptor (PPAR) γ Partial Agonist and PPARδ Antagonist Activity Suggests Their Antidiabetic Potential..  J Med Chem,  60  (17): (7459-7475).  [PMID:28799755] [10.1021/acs.jmedchem.7b00805]
117. Karthikeyan C, Jharia P, Waiker DK, Nusbaum AC, Amawi H, Kirwen EM, Christman R, Arudra SKC, Meijer L, Tiwari AK, Trivedi P..  (2017)  N-(1H-Pyrazol-3-yl)quinazolin-4-amines as a novel class of casein kinase 1δ/ε inhibitors: Synthesis, biological evaluation and molecular modeling studies..  Bioorg Med Chem Lett,  27  (12): (2663-2667).  [PMID:28487075] [10.1016/j.bmcl.2017.04.080]
118. Li Y, Luo X, Guo Q, Nie Y, Wang T, Zhang C, Huang Z, Wang X, Liu Y, Chen Y, Zheng J, Yang S, Fan Y, Xiang R..  (2018)  Discovery of N1-(4-((7-Cyclopentyl-6-(dimethylcarbamoyl)-7 H-pyrrolo[2,3- d]pyrimidin-2-yl)amino)phenyl)- N8-hydroxyoctanediamide as a Novel Inhibitor Targeting Cyclin-dependent Kinase 4/9 (CDK4/9) and Histone Deacetlyase1 (HDAC1) against Malignant Cancer..  J Med Chem,  61  (7): (3166-3192).  [PMID:29518312] [10.1021/acs.jmedchem.8b00209]
119. 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] [10.1016/j.bmcl.2017.07.072]
120. Park SJ, Kim E, Yoo M, Lee JY, Park CH, Hwang JY, Ha JD..  (2017)  Synthesis and biological evaluation of N9-cis-cyclobutylpurine derivatives for use as cyclin-dependent kinase (CDK) inhibitors..  Bioorg Med Chem Lett,  27  (18): (4399-4404).  [PMID:28827110] [10.1016/j.bmcl.2017.08.018]
121. Toviwek B, Suphakun P, Choowongkomon K, Hannongbua S, Gleeson MP..  (2017)  Synthesis and evaluation of the NSCLC anti-cancer activity and physical properties of 4-aryl-N-phenylpyrimidin-2-amines..  Bioorg Med Chem Lett,  27  (20): (4749-4754).  [PMID:28927795] [10.1016/j.bmcl.2017.08.063]
122. Bharate SB, Kumar V, Jain SK, Mintoo MJ, Guru SK, Nuthakki VK, Sharma M, Bharate SS, Gandhi SG, Mondhe DM, Bhushan S, Vishwakarma RA..  (2018)  Discovery and Preclinical Development of IIIM-290, an Orally Active Potent Cyclin-Dependent Kinase Inhibitor..  J Med Chem,  61  (4): (1664-1687).  [PMID:29370702] [10.1021/acs.jmedchem.7b01765]
123. Zhang H, Wu W, Feng C, Liu Z, Bai E, Wang X, Lei M, Cheng H, Feng H, Shi J, Wang J, Zhang Z, Jin T, Chen S, Hu S, Zhu Y..  (2017)  Design, synthesis, SAR discussion, in vitro and in vivo evaluation of novel selective EGFR modulator to inhibit L858R/T790M double mutants..  Eur J Med Chem,  135  (12-23).  [PMID:28426996] [10.1016/j.ejmech.2017.04.036]
124. Li Y, Guo Q, Zhang C, Huang Z, Wang T, Wang X, Wang X, Xu G, Liu Y, Yang S, Fan Y, Xiang R..  (2017)  Discovery of a highly potent, selective and novel CDK9 inhibitor as an anticancer drug candidate..  Bioorg Med Chem Lett,  27  (15): (3231-3237).  [PMID:28651979] [10.1016/j.bmcl.2017.06.041]
125. 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] [10.1016/j.bmcl.2017.07.004]
126. Patel S, Meilandt WJ, Erickson RI, Chen J, Deshmukh G, Estrada AA, Fuji RN, Gibbons P, Gustafson A, Harris SF, Imperio J, Liu W, Liu X, Liu Y, Lyssikatos JP, Ma C, Yin J, Lewcock JW, Siu M..  (2017)  Selective Inhibitors of Dual Leucine Zipper Kinase (DLK, MAP3K12) with Activity in a Model of Alzheimer's Disease..  J Med Chem,  60  (19): (8083-8102).  [PMID:28929759] [10.1021/acs.jmedchem.7b00843]
127. 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] [10.1016/j.bmcl.2017.10.031]
128. 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] [10.1016/j.bmcl.2018.03.093]
129. Wang Y, Chen Y, Cheng X, Zhang K, Wang H, Liu B, Wang J..  (2018)  Design, synthesis and biological evaluation of pyrimidine derivatives as novel CDK2 inhibitors that induce apoptosis and cell cycle arrest in breast cancer cells..  Bioorg Med Chem,  26  (12): (3491-3501).  [PMID:29853338] [10.1016/j.bmc.2018.05.024]
130. 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] [10.1016/j.ejmech.2018.01.053]
131. 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] [10.1016/j.ejmech.2018.03.003]
132. Darwish SS, Abdel-Halim M, Salah M, Abadi AH, Becker W, Engel M..  (2018)  Development of novel 2,4-bispyridyl thiophene-based compounds as highly potent and selective Dyrk1A inhibitors. Part I: Benzamide and benzylamide derivatives..  Eur J Med Chem,  157  (1031-1050).  [PMID:30193214] [10.1016/j.ejmech.2018.07.050]
133. 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] [10.1016/j.bmcl.2018.09.006]
134. 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] [10.1016/j.ejmech.2018.09.025]
135. Hu X, Zhao H, Wang Y, Liu Z, Feng B, Tang C..  (2018)  Synthesis and biological evaluation of novel 5,6-dihydropyrimido[4,5-f]quinazoline derivatives as potent CDK2 inhibitors..  Bioorg Med Chem Lett,  28  (20): (3385-3390).  [PMID:30197029] [10.1016/j.bmcl.2018.08.035]
136. Darwish SS, Abdel-Halim M, ElHady AK, Salah M, Abadi AH, Becker W, Engel M..  (2018)  Development of novel amide-derivatized 2,4-bispyridyl thiophenes as highly potent and selective Dyrk1A inhibitors. Part II: Identification of the cyclopropylamide moiety as a key modification..  Eur J Med Chem,  158  (270-285).  [PMID:30223116] [10.1016/j.ejmech.2018.08.097]
137. 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] [10.1021/acsmedchemlett.9b00142]
138. Zhang Q, Hu X, Wan G, Wang J, Li L, Wu X, Liu Z, Yu L..  (2019)  Discovery of 3-(((9H-purin-6-yl)amino)methyl)-4,6-dimethylpyridin-2(1H)-one derivatives as novel tubulin polymerization inhibitors for treatment of cancer..  Eur J Med Chem,  184  (111728-111728).  [PMID:31610375] [10.1016/j.ejmech.2019.111728]
139. Rana S, Sonawane YA, Taylor MA, Kizhake S, Zahid M, Natarajan A..  (2018)  Synthesis of aminopyrazole analogs and their evaluation as CDK inhibitors for cancer therapy..  Bioorg Med Chem Lett,  28  (23-24): (3736-3740).  [PMID:30343954] [10.1016/j.bmcl.2018.10.020]
140. 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] [10.1016/j.ejmech.2018.10.052]
141. Wang Y, Dou X, Jiang L, Jin H, Zhang L, Zhang L, Liu Z..  (2019)  Discovery of novel glycogen synthase kinase-3α inhibitors: Structure-based virtual screening, preliminary SAR and biological evaluation for treatment of acute myeloid leukemia..  Eur J Med Chem,  171  (221-234).  [PMID:30925338] [10.1016/j.ejmech.2019.03.039]
142. Abdelaziz AM, Basnet SKC, Islam S, Li M, Tadesse S, Albrecht H, Gerber C, Yu M, Wang S..  (2019)  Synthesis and evaluation of 2'H-spiro[cyclohexane-1,3'-imidazo[1,5-a]pyridine]-1',5'-dione derivatives as Mnk inhibitors..  Bioorg Med Chem Lett,  29  (18): (2650-2654).  [PMID:31362920] [10.1016/j.bmcl.2019.07.043]
143. 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] [10.1021/acs.jmedchem.9b00318]
144. 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] [10.1016/j.ejmech.2019.05.021]
145. Montanari R, Capelli D, Yamamoto K, Awaishima H, Nishikata K, Barendregt A, Heck AJR, Loiodice F, Altieri F, Paiardini A, Grottesi A, Pirone L, Pedone E, Peiretti F, Brunel JM, Itoh T, Pochetti G..  (2020)  Insights into PPARγ Phosphorylation and Its Inhibition Mechanism..  J Med Chem,  63  (9): (4811-4823).  [PMID:32239932] [10.1021/acs.jmedchem.0c00048]
146. 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] [10.1021/acs.jmedchem.9b00353]
147. Wang X, Yu C, Wang C, Ma Y, Wang T, Li Y, Huang Z, Zhou M, Sun P, Zheng J, Yang S, Fan Y, Xiang R..  (2019)  Novel cyclin-dependent kinase 9 (CDK9) inhibitor with suppression of cancer stemness activity against non-small-cell lung cancer..  Eur J Med Chem,  181  (111535-111535).  [PMID:31376566] [10.1016/j.ejmech.2019.07.038]
148. Zhao L, Li Y, Wang Y, Qiao Z, Miao Z, Yang J, Huang L, Tian C, Li L, Chen D, Yang S..  (2019)  Discovery of 4H-Chromen-4-one Derivatives as a New Class of Selective Rho Kinase (ROCK) Inhibitors, which Showed Potent Activity in ex Vivo Diabetic Retinopathy Models..  J Med Chem,  62  (23): (10691-10710).  [PMID:31693351] [10.1021/acs.jmedchem.9b01143]
149. Jang J, Son JB, To C, Bahcall M, Kim SY, Kang SY, Mushajiang M, Lee Y, Jänne 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] [10.1016/j.ejmech.2017.04.079]
150. Bronner SM, Merrick KA, Murray J, Salphati L, Moffat JG, Pang J, Sneeringer CJ, Dompe N, Cyr P, Purkey H, Boenig GL, Li J, Kolesnikov A, Larouche-Gauthier R, Lai KW, Shen X, Aubert-Nicol S, Chen YC, Cheong J, Crawford JJ, Hafner M, Haghshenas P, Jakalian A, Leclerc JP, Lim NK, O'Brien T, Plise EG, Shalan H, Sturino C, Wai J, Xiao Y, Yin J, Zhao L, Gould S, Olivero A, Heffron TP..  (2019)  Design of a brain-penetrant CDK4/6 inhibitor for glioblastoma..  Bioorg Med Chem Lett,  29  (16): (2294-2301).  [PMID:31307887] [10.1016/j.bmcl.2019.06.021]
151. 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] [10.1016/j.ejmech.2018.12.063]
152. Khair NZ, Lenjisa JL, Tadesse S, Kumarasiri M, Basnet SKC, Mekonnen LB, Li M, Diab S, Sykes MJ, Albrecht H, Milne R, Wang S..  (2019)  Discovery of CDK5 Inhibitors through Structure-Guided Approach..  ACS Med Chem Lett,  10  (5): (786-791).  [PMID:31098000] [10.1021/acsmedchemlett.9b00029]
153. Teng Y, Lu K, Zhang Q, Zhao L, Huang Y, Ingarra AM, Galons H, Li T, Cui S, Yu P, Oumata N..  (2019)  Recent advances in the development of cyclin-dependent kinase 7 inhibitors..  Eur J Med Chem,  183  (111641-111641).  [PMID:31514062] [10.1016/j.ejmech.2019.111641]
154. Sánchez-Martínez C, Lallena MJ, Sanfeliciano SG, de Dios A..  (2019)  Cyclin dependent kinase (CDK) inhibitors as anticancer drugs: Recent advances (2015-2019)..  Bioorg Med Chem Lett,  29  (20): (126637-126637).  [PMID:31477350] [10.1016/j.bmcl.2019.126637]
155. 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] [10.1016/j.ejmech.2019.111943]
156. Zeinyeh W, Esvan YJ, Nauton L, Loaëc N, Meijer L, Théry V, Anizon F, Giraud F, Moreau P..  (2016)  Synthesis and preliminary in vitro kinase inhibition evaluation of new diversely substituted pyrido[3,4-g]quinazoline derivatives..  Bioorg Med Chem Lett,  26  (17): (4327-4329).  [PMID:27469128] [10.1016/j.bmcl.2016.07.032]
157. Zhou F, Chen L, Cao C, Yu J, Luo X, Zhou P, Zhao L, Du W, Cheng J, Xie Y, Chen Y..  (2020)  Development of selective mono or dual PROTAC degrader probe of CDK isoforms..  Eur J Med Chem,  187  (111952-111952).  [PMID:31846828] [10.1016/j.ejmech.2019.111952]
158. Tazarki H,Zeinyeh W,Esvan YJ,Knapp S,Chatterjee D,Schröder M,Joerger AC,Khiari J,Josselin B,Baratte B,Bach S,Ruchaud S,Anizon F,Giraud F,Moreau P.  (2019)  New pyrido[3,4-g]quinazoline derivatives as CLK1 and DYRK1A inhibitors: synthesis, biological evaluation and binding mode analysis..  Eur J Med Chem,  166  (304-317).  [PMID:30731399] [10.1016/j.ejmech.2019.01.052]
159. Hamilton GL,Chen H,Deshmukh G,Eigenbrot C,Fong R,Johnson A,Kohli PB,Lupardus PJ,Liederer BM,Ramaswamy S,Wang H,Wang J,Xu Z,Zhu Y,Vucic D,Patel S.  (2019)  Potent and selective inhibitors of receptor-interacting protein kinase 1 that lack an aromatic back pocket group..  Bioorg Med Chem Lett,  29  (12.0): (1497-1501).  [PMID:31000154] [10.1016/j.bmcl.2019.04.014]
160. Shi X,Quan Y,Wang Y,Wang Y,Li Y.  (2021)  Design, synthesis, and biological evaluation of 2,6,7-substituted pyrrolo[2,3-d]pyrimidines as cyclin dependent kinase inhibitor in pancreatic cancer cells..  Bioorg Med Chem Lett,  33  (127725-127725).  [PMID:33316409] [10.1016/j.bmcl.2020.127725]
161. Wu T,Qin Z,Tian Y,Wang J,Xu C,Li Z,Bian J.  (2020)  Recent Developments in the Biology and Medicinal Chemistry of CDK9 Inhibitors: An Update..  J Med Chem,  63  (22): (13228-13257).  [PMID:32866383] [10.1021/acs.jmedchem.0c00744]
162. 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] [10.1016/j.bmcl.2018.03.045]
163. 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] [10.1016/j.ejmech.2020.112968]
164. Yu M,Teo T,Yang Y,Li M,Long Y,Philip S,Noll B,Heinemann GK,Diab S,Eldi P,Mekonnen L,Anshabo AT,Rahaman MH,Milne R,Hayball JD,Wang S.  (2021)  Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation..  Eur J Med Chem,  214  (113248-113248).  [PMID:33571827] [10.1016/j.ejmech.2021.113248]
165. Yang J,Chen K,Zhang G,Yang QY,Li YS,Huang SZ,Wang YL,Yang W,Jiang XJ,Yan HX,Zhu JQ,Xiang R,Luo YF,Li WM,Wei YQ,Li LL,Yang SY.  (2018)  Structural optimization and structure-activity relationship studies of N-phenyl-7,8-dihydro-6H-pyrimido[5,4-b][1,4]oxazin-4-amine derivatives as a new class of inhibitors of RET and its drug resistance mutants..  Eur J Med Chem,  143  (1148-1164).  [PMID:29133048] [10.1016/j.ejmech.2017.09.018]
166. Jeong P,Moon Y,Lee JH,Lee SD,Park J,Lee J,Kim J,Lee HJ,Kim NY,Choi J,Heo JD,Shin JE,Park HW,Kim YG,Han SY,Kim YC.  (2020)  Discovery of orally active indirubin-3'-oxime derivatives as potent type 1 FLT3 inhibitors for acute myeloid leukemia..  Eur J Med Chem,  195  (112205-112205).  [PMID:32272419] [10.1016/j.ejmech.2020.112205]
167. Xu J,Li H,Wang X,Huang J,Li S,Liu C,Dong R,Zhu G,Duan C,Jiang F,Zhang Y,Zhu Y,Zhang T,Chen Y,Tang W,Lu T.  (2020)  Discovery of coumarin derivatives as potent and selective cyclin-dependent kinase 9 (CDK9) inhibitors with high antitumour activity..  Eur J Med Chem,  200  (112424-112424).  [PMID:32447197] [10.1016/j.ejmech.2020.112424]
168. Meyerson, M M and 7 more authors..  (1992)  A family of human cdc2-related protein kinases..  The EMBO journal,  [PMID:1639063]
169. Meijer, L L and 8 more authors..  (1997)  Biochemical and cellular effects of roscovitine, a potent and selective inhibitor of the cyclin-dependent kinases cdc2, cdk2 and cdk5..  European journal of biochemistry,  (15): [PMID:9030781]
170. Sharma, P P, Sharma, M M, Amin, N D ND, Albers, R W RW and Pant, H C HC..  (1999)  Regulation of cyclin-dependent kinase 5 catalytic activity by phosphorylation..  Proceedings of the National Academy of Sciences of the United States of America,  (28): [PMID:10500146]
171. Dhavan, R R and Tsai, L H LH..  (2001)  A decade of CDK5..  Nature reviews. Molecular cell biology,  [PMID:11584302]
172. Chen, X X, Ji, Z L ZL and Chen, Y Z YZ..  (2002)  TTD: Therapeutic Target Database..  Nucleic acids research,  (1): [PMID:11752352]
173. Gong, Xiaoming X and 8 more authors..  (2003)  Cdk5-mediated inhibition of the protective effects of transcription factor MEF2 in neurotoxicity-induced apoptosis..  Neuron,  (10): [PMID:12691662]
174. Hillier, Ladeana W LW and 106 more authors..  (2003)  The DNA sequence of human chromosome 7..  Nature,  (10): [PMID:12853948]
175. Honma, Naoyuki N and 11 more authors..  (2003)  Apoptosis-associated tyrosine kinase is a Cdk5 activator p35 binding protein..  Biochemical and biophysical research communications,  (17): [PMID:14521924]
176. Tang, Lin L and 13 more authors..  (2005)  Crystal structure of pyridoxal kinase in complex with roscovitine and derivatives..  The Journal of biological chemistry,  (2): [PMID:15985434]
177. Caligiuri, Maureen M and 11 more authors..  (2005)  A proteome-wide CDK/CRK-specific kinase inhibitor promotes tumor cell death in the absence of cell cycle progression..  Chemistry & biology,  [PMID:16242653]
178. Kamei, Hirotsugu H and 8 more authors..  (2007)  Suppression of calpain-dependent cleavage of the CDK5 activator p35 to p25 by site-specific phosphorylation..  The Journal of biological chemistry,  (19): [PMID:17121855]
179. Fu, Wing-Yu WY and 10 more authors..  (2007)  Cdk5 regulates EphA4-mediated dendritic spine retraction through an ephexin1-dependent mechanism..  Nature neuroscience,  [PMID:17143272]
180. Anne, Sandrine L SL, Saudou, Frédéric F and Humbert, Sandrine S..  (2007)  Phosphorylation of huntingtin by cyclin-dependent kinase 5 is induced by DNA damage and regulates wild-type and mutant huntingtin toxicity in neurons..  The Journal of neuroscience : the official journal of the Society for Neuroscience,  (4): [PMID:17611284]
181. Miyamoto, Yuki Y and 6 more authors..  (2007)  Cdk5 regulates differentiation of oligodendrocyte precursor cells through the direct phosphorylation of paxillin..  Journal of cell science,  (15): [PMID:18042622]
182. Daub, Henrik H and 9 more authors..  (2008)  Kinase-selective enrichment enables quantitative phosphoproteomics of the kinome across the cell cycle..  Molecular cell,  (8): [PMID:18691976]
183. Kim, Dohoon D and 16 more authors..  (2008)  Deregulation of HDAC1 by p25/Cdk5 in neurotoxicity..  Neuron,  (10): [PMID:19081376]
184. Malumbres, Marcos M and Barbacid, Mariano M..  (2009)  Cell cycle, CDKs and cancer: a changing paradigm..  Nature reviews. Cancer,  [PMID:19238148]
185. Oppermann, Felix S FS and 7 more authors..  (2009)  Large-scale proteomics analysis of the human kinome..  Molecular & cellular proteomics : MCP,  [PMID:19369195]
186. Li, Qiang Q and 8 more authors..  (2010)  Characterization of a novel human CDK5 splicing variant that inhibits Wnt/beta-catenin signaling..  Molecular biology reports,  [PMID:19693690]
187. Jessberger, Sebastian; Gage, Fred H; Eisch, Amelia J and Lagace, Diane C..  (2009)  Making a neuron: Cdk5 in embryonic and adult neurogenesis..  Trends in neurosciences,  [PMID:19782409]
188. Lee, Chien-Hsing CH and 6 more authors..  (2010)  CDK5 phosphorylates eNOS at Ser-113 and regulates NO production..  Journal of cellular biochemistry,  [PMID:20213743]
189. Liebl, Johanna J and 6 more authors..  (2010)  Cyclin-dependent kinase 5 regulates endothelial cell migration and angiogenesis..  The Journal of biological chemistry,  (12): [PMID:20826806]
190. Hisanaga, Shin-ichi S and Endo, Ryo R..  (2010)  Regulation and role of cyclin-dependent kinase activity in neuronal survival and death..  Journal of neurochemistry,  [PMID:21044075]
191. Gallazzini, Morgan M and 5 more authors..  (2011)  High NaCl-induced activation of CDK5 increases phosphorylation of the osmoprotective transcription factor TonEBP/OREBP at threonine 135, which contributes to its rapid nuclear localization..  Molecular biology of the cell,  (1): [PMID:21209322]
192. Arif, Abul A, Jia, Jie J, Moodt, Robyn A RA, DiCorleto, Paul E PE and Fox, Paul L PL..  (2011)  Phosphorylation of glutamyl-prolyl tRNA synthetase by cyclin-dependent kinase 5 dictates transcript-selective translational control..  Proceedings of the National Academy of Sciences of the United States of America,  (25): [PMID:21220307]
193. Zhang, Jie J and Herrup, Karl K..  (2011)  Nucleocytoplasmic Cdk5 is involved in neuronal cell cycle and death in post-mitotic neurons..  Cell cycle (Georgetown, Tex.),  (15): [PMID:21415596]
194. Lee, Ki-Young KY, Liu, Lijuan L, Jin, Yan Y, Fu, Song-Bin SB and Rosales, Jesusa L JL..  (2012)  Cdk5 mediates vimentin Ser56 phosphorylation during GTP-induced secretion by neutrophils..  Journal of cellular physiology,  [PMID:21465480]
195. Lopes, Joao P JP and Agostinho, Paula P..  (2011)  Cdk5: multitasking between physiological and pathological conditions..  Progress in neurobiology,  [PMID:21473899]
196. Wong, Alan S L AS and 6 more authors..  (2011)  Cdk5-mediated phosphorylation of endophilin B1 is required for induced autophagy in models of Parkinson's disease..  Nature cell biology,  [PMID:21499257]
197. Zhu, Jinqiu J, Li, Wenming W and Mao, Zixu Z..  (2011)  Cdk5: mediator of neuronal development, death and the response to DNA damage..  Mechanisms of ageing and development,  [PMID:21600237]
198. Sun, Kai-Hui KH and 6 more authors..  (2011)  Glutathione-S-transferase P1 is a critical regulator of Cdk5 kinase activity..  Journal of neurochemistry,  [PMID:21668448]
199. Zhou, Houjiang H and 6 more authors..  (2013)  Toward a comprehensive characterization of a human cancer cell phosphoproteome..  Journal of proteome research,  (4): [PMID:23186163]
200. Kwak, Yongdo Y and 11 more authors..  (2013)  Cyclin-dependent kinase 5 (Cdk5) regulates the function of CLOCK protein by direct phosphorylation..  The Journal of biological chemistry,  (27): [PMID:24235147]
201. Magen, Daniella D and 13 more authors..  (2015)  Autosomal recessive lissencephaly with cerebellar hypoplasia is associated with a loss-of-function mutation in CDK5..  Human genetics,  [PMID:25560765]
202. Gaisina IN, Gallier F, Ougolkov AV, Kim KH, Kurome T, Guo S, Holzle D, Luchini DN, Blond SY, Billadeau DD et al..  (2009)  From a natural product lead to the identification of potent and selective benzofuran-3-yl-(indol-3-yl)maleimides as glycogen synthase kinase 3beta inhibitors that suppress proliferation and survival of pancreatic cancer cells..  J Med Chem,  52  (7): (1853-63).  [PMID:19338355]
203. Thomas R Burkard,Melanie Planyavsky,Ines Kaupe,Florian P Breitwieser,Tilmann Bürckstümmer,Keiryn L Bennett,Giulio Superti-Furga,Jacques Colinge.  (2011-01-29)  Initial characterization of the human central proteome..  BMC systems biology,  (17-17).  [PMID:21269460]
204. May-Dracka TL,Arduini R,Bertolotti-Ciarlet A,Bhisetti G,Brickelmaier M,Cahir-McFarland E,Enyedy I,Fontenot JD,Hesson T,Little K,Lyssikatos J,Marcotte D,McKee T,Murugan P,Patterson T,Peng H,Rushe M,Silvian L,Spilker K,Wu P,Xin Z,Burkly LC.  (2018)  Investigating small molecules to inhibit germinal center kinase-like kinase (GLK/MAP4K3) upstream of PKCθ phosphorylation: Potential therapy to modulate T cell dependent immunity..  Bioorg Med Chem Lett,  28  (10): (1964-1971).  [PMID:29636220] [10.1016/j.bmcl.2018.03.032]

溶液计算器