Recombinant; Rabbit anti Human ITK/EMT Antibody; WB; Unconjugated
| SKU | Size | Availability | Price | Qty |
|---|---|---|---|---|
| Ab111383-10μl | 10μl | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $79.90 | |
| Ab111383-50μl | 50μl | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $219.90 | |
| Ab111383-100μl | 100μl | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $329.90 | |
| Ab111383-1ml | 1ml | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $2,899.90 |
Recombinant; Rabbit anti Human ITK/EMT Antibody; WB; Unconjugated
| Product Name | Recombinant ITK/EMT Antibody - Primary antibody, specific to ITK, Rabbit IgG |
|---|---|
| Synonyms | EC 2.7.10.2 | IL-2-inducible T-cell kinase | Interleukin-2-inducible T-cell kinase | Kinase EMT | T-cell-specific kinase | Tyrosine-protein kinase Lyk | EMT antibody | Homolog of mouse T cell itk/tsk antibody | IL 2 inducible T cell kinase antibody | IL2 |
| Specifications & Purity | ExactAb™, Validated, Recombinant, 0.45 mg/mL |
| Host species | Rabbit |
| Specificity | ITK |
| Immunogen | A synthetic peptide derived from human ITK (AA 1-66) |
| Positive Control | WB: Jurkat lysates. |
| Conjugation | Unconjugated |
| Grade | ExactAb™, Recombinant, Validated |
| Product Description |
Rabbit anti Human ITK/EMT Antibody, Recombinant, could be used for WB and so on. |
| Isotype | Rabbit IgG |
|---|---|
| SDS-PAGE | 150 kDa |
| Purification Method | Protein A purified |
| Form | Liquid |
| Concentration | 0.45 mg/mL |
| Storage Temp | Store at -20°C,Avoid repeated freezing and thawing |
| Shipped In | Ice chest + Ice pads |
| Stability And Storage | Store at 4°C short term (1-2 weeks). Store at -20°C long term (24 months). Upon delivery aliquot. Avoid freeze/thaw cycle. |
Recombinant ITK/EMT Antibody (Ab111383) - Western Blot
All lanes: Recombinant ITK/EMT Antibody (Ab111383) at 1/1000 dilution
Samples: Lysates at 20 µg per lane
Secondary: Goat Anti-Rabbit IgG H&L (HRP) (Ab170144) at 1/20000 dilution
Predicted band size: 72 kDa
Observed band size: 71 kDa
Exposure time: 120.0 s
| Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
|---|
| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
|---|
| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
|---|
| Application | Dilution info |
|---|---|
| WB | 1/500-1/1000 |
Enter Lot Number to search for COA:
Find and download the COA for your product by matching the lot number on the packaging.
| Lot Number | Certificate Type | Date | Item |
|---|---|---|---|
 ZJ24F0708731 | Certificate of Analysis | Jul 25, 2024 | Ab111383 |
| ZJ24F0708730 | Certificate of Analysis | Jul 25, 2024 | Ab111383 |
| 1. Zhou W, Ercan D, Chen L, Yun CH, Li D, Capelletti M, Cortot AB, Chirieac L, Iacob RE, Padera R et al.. (2009) Novel mutant-selective EGFR kinase inhibitors against EGFR T790M.. Nature, 462 (7276): (1070-4). [PMID:20033049] |
| 2. 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] |
| 3. 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] |
| 4. 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] |
| 5. 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] |
| 6. Conway JG, McDonald B, Parham J, Keith B, Rusnak DW, Shaw E, Jansen M, Lin P, Payne A, Crosby RM et al.. (2005) Inhibition of colony-stimulating-factor-1 signaling in vivo with the orally bioavailable cFMS kinase inhibitor GW2580.. Proc Natl Acad Sci USA, 102 (44): (16078-83). [PMID:16249345] |
| 7. Misra RN, Xiao HY, Kim KS, Lu S, Han WC, Barbosa SA, Hunt JT, Rawlins DB, Shan W, Ahmed SZ et al.. (2004) N-(cycloalkylamino)acyl-2-aminothiazole inhibitors of cyclin-dependent kinase 2. N-[5-[[[5-(1,1-dimethylethyl)-2-oxazolyl]methyl]thio]-2-thiazolyl]-4- piperidinecarboxamide (BMS-387032), a highly efficacious and selective antitumor agent.. J Med Chem, 47 (7): (1719-28). [PMID:15027863] |
| 8. Li X, Zuo Y, Tang G, Wang Y, Zhou Y, Wang X, Guo T, Xia M, Ding N, Pan Z. (2014) Discovery of a series of 2,5-diaminopyrimidine covalent irreversible inhibitors of Bruton's tyrosine kinase with in vivo antitumor activity.. J Med Chem, 57 (12): (5112-28). [PMID:24915291] |
| 9. Okuzumi T, Fiedler D, Zhang C, Gray DC, Aizenstein B, Hoffman R, Shokat KM. (2009) Inhibitor hijacking of Akt activation.. Nat Chem Biol, 5 (7): (484-93). [PMID:19465931] |
| 10. Weinberg LR, Albom MS, Angeles TS, Husten J, Lisko JG, McHugh RJ, Milkiewicz KL, Murthy S, Ott GR, Theroff JP et al.. (2011) Fused bicyclic derivatives of 2,4-diaminopyrimidine as c-Met inhibitors.. Bioorg Med Chem Lett, 21 (1): (164-7). [PMID:21123062] |
| 11. 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] |
| 12. Byrd JC, Harrington B, O'Brien S, Jones JA, Schuh A, Devereux S, Chaves J, Wierda WG, Awan FT, Brown JR et al.. (2016) Acalabrutinib (ACP-196) in Relapsed Chronic Lymphocytic Leukemia.. N Engl J Med, 374 (4): (323-32). [PMID:26641137] |
| 13. Zhong Y, Dong S, Strattan E, Ren L, Butchar JP, Thornton K, Mishra A, Porcu P, Bradshaw JM, Bisconte A et al.. (2015) Targeting interleukin-2-inducible T-cell kinase (ITK) and resting lymphocyte kinase (RLK) using a novel covalent inhibitor PRN694.. J Biol Chem, 290 (10): (5960-78). [PMID:25593320] |
| 14. 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] |
| 15. 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] |
| 16. 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] |
| 17. Telliez JB, Dowty ME, Wang L, Jussif J, Lin T, Li L, Moy E, Balbo P, Li W, Zhao Y et al.. (2016) Discovery of a JAK3-Selective Inhibitor: Functional Differentiation of JAK3-Selective Inhibition over pan-JAK or JAK1-Selective Inhibition.. ACS Chem Biol, 11 (12): (3442-3451). [PMID:27791347] |
| 18. Huang Z, Li H, Zhang Q, Lu F, Hong M, Zhang Z, Guo X, Zhu Y, Li S, Liu H. (2017) Discovery of Indolinone-Based Multikinase Inhibitors as Potential Therapeutics for Idiopathic Pulmonary Fibrosis.. ACS Med Chem Lett, 8 (11): (1142-1147). [PMID:29152045] |
| 19. Watterson SH, De Lucca GV, Shi Q, Langevine CM, Liu Q, Batt DG, Beaudoin Bertrand M, Gong H, Dai J, Yip S et al.. (2016) Discovery of 6-Fluoro-5-(R)-(3-(S)-(8-fluoro-1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)-2-methylphenyl)-2-(S)-(2-hydroxypropan-2-yl)-2,3,4,9-tetrahydro-1H-carbazole-8-carboxamide (BMS-986142): A Reversible Inhibitor of Bruton's Tyrosine Kinase (BTK) Conformationally Constrained by Two Locked Atropisomers.. J Med Chem, 59 (19): (9173-9200). [PMID:27583770] |
| 20. 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] |
| 21. Burch JD, Barrett K, Chen Y, DeVoss J, Eigenbrot C, Goldsmith R, Ismaili MH, Lau K, Lin Z, Ortwine DF et al.. (2015) Tetrahydroindazoles as Interleukin-2 Inducible T-Cell Kinase Inhibitors. Part II. Second-Generation Analogues with Enhanced Potency, Selectivity, and Pharmacodynamic Modulation in Vivo.. J Med Chem, 58 (9): (3806-16). [PMID:25844760] |
| 22. Liang C, Tian D, Ren X, Ding S, Jia M, Xin M, Thareja S. (2018) The development of Bruton's tyrosine kinase (BTK) inhibitors from 2012 to 2017: A mini-review.. Eur J Med Chem, 151 (3): (315-326). [PMID:29631132] |
| 23. Li Y, Xiong Y, Zhang G, Zhang L, Yang W, Yang J, Huang L, Qiao Z, Miao Z, Lin G et al.. (2018) Identification of 5-(2,3-Dihydro-1 H-indol-5-yl)-7 H-pyrrolo[2,3- d]pyrimidin-4-amine Derivatives as a New Class of Receptor-Interacting Protein Kinase 1 (RIPK1) Inhibitors, Which Showed Potent Activity in a Tumor Metastasis Model.. J Med Chem, 61 (24): (11398-11414). [PMID:30480444] |
| 24. Smith CR, Dougan DR, Komandla M, Kanouni T, Knight B, Lawson JD, Sabat M, Taylor ER, Vu P, Wyrick C. (2015) Fragment-Based Discovery of a Small Molecule Inhibitor of Bruton's Tyrosine Kinase.. J Med Chem, 58 (14): (5437-44). [PMID:26087137] |
| 25. Yao X, Sun X, Jin S, Yang L, Xu H, Rao Y. (2019) Discovery of 4-Aminoquinoline-3-carboxamide Derivatives as Potent Reversible Bruton's Tyrosine Kinase Inhibitors for the Treatment of Rheumatoid Arthritis.. J Med Chem, 62 (14): (6561-6574). [PMID:31260299] |
| 26. Caldwell RD, Qiu H, Askew BC, Bender AT, Brugger N, Camps M, Dhanabal M, Dutt V, Eichhorn T, Gardberg AS et al.. (2019) Discovery of Evobrutinib: An Oral, Potent, and Highly Selective, Covalent Bruton's Tyrosine Kinase (BTK) Inhibitor for the Treatment of Immunological Diseases.. J Med Chem, 62 (17): (7643-7655). [PMID:31368705] |
| 27. Watterson SH, Liu Q, Beaudoin Bertrand M, Batt DG, Li L, Pattoli MA, Skala S, Cheng L, Obermeier MT, Moore R et al.. (2019) Discovery of Branebrutinib (BMS-986195): A Strategy for Identifying a Highly Potent and Selective Covalent Inhibitor Providing Rapid in Vivo Inactivation of Bruton's Tyrosine Kinase (BTK).. J Med Chem, 62 (7): (3228-3250). [PMID:30893553] |
| 28. Angst D, Gessier F, Janser P, Vulpetti A, Wälchli R, Beerli C, Littlewood-Evans A, Dawson J, Nuesslein-Hildesheim B, Wieczorek G et al.. (2020) Discovery of LOU064 (Remibrutinib), a Potent and Highly Selective Covalent Inhibitor of Bruton's Tyrosine Kinase.. J Med Chem, 63 (10): (5102-5118). [PMID:32083858] |
| 29. Yin L, Li H, Liu W, Yao Z, Cheng Z, Zhang H, Zou H. (2018) A highly potent CDK4/6 inhibitor was rationally designed to overcome blood brain barrier in gliobastoma therapy.. Eur J Med Chem, 144 (3): (1-28). [PMID:29247857] |
| 30. Kim KS, Kimball SD, Misra RN, Rawlins DB, Hunt JT, Xiao HY, Lu S, Qian L, Han WC, Shan W, Mitt T, Cai ZW, Poss MA, Zhu H, Sack JS, Tokarski JS, Chang CY, Pavletich N, Kamath A, Humphreys WG, Marathe P, Bursuker I, Kellar KA, Roongta U, Batorsky R, Mulheron JG, Bol D, Fairchild CR, Lee FY, Webster KR.. (2002) Discovery of aminothiazole inhibitors of cyclin-dependent kinase 2: synthesis, X-ray crystallographic analysis, and biological activities.. J Med Chem, 45 (18): (3905-3927). [PMID:12190313] |
| 31. Gellibert F, Woolven J, Fouchet MH, Mathews N, Goodland H, Lovegrove V, Laroze A, Nguyen VL, Sautet S, Wang R, Janson C, Smith W, Krysa G, Boullay V, De Gouville AC, Huet S, Hartley D.. (2004) Identification of 1,5-naphthyridine derivatives as a novel series of potent and selective TGF-beta type I receptor inhibitors.. J Med Chem, 47 (18): (4494-4506). [PMID:15317461] |
| 32. 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] |
| 33. Borzilleri RM, Bhide RS, Barrish JC, D'Arienzo CJ, Derbin GM, Fargnoli J, Hunt JT, Jeyaseelan R, Kamath A, Kukral DW, Marathe P, Mortillo S, Qian L, Tokarski JS, Wautlet BS, Zheng X, Lombardo LJ.. (2006) Discovery and evaluation of N-cyclopropyl- 2,4-difluoro-5-((2-(pyridin-2-ylamino)thiazol-5- ylmethyl)amino)benzamide (BMS-605541), a selective and orally efficacious inhibitor of vascular endothelial growth factor receptor-2.. J Med Chem, 49 (13): (3766-3769). [PMID:16789733] |
| 34. 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] |
| 35. 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] |
| 36. 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] |
| 37. 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] |
| 38. Hantschel O, Rix U, Schmidt U, Bürckstümmer T, Kneidinger M, Schütze G, Colinge J, Bennett KL, Ellmeier W, Valent P, Superti-Furga G.. (2007) The Btk tyrosine kinase is a major target of the Bcr-Abl inhibitor dasatinib.. Proc Natl Acad Sci U S A, 104 (33): (13283-13288). [PMID:17684099] |
| 39. Liu L, Siegmund A, Xi N, Kaplan-Lefko P, Rex K, Chen A, Lin J, Moriguchi J, Berry L, Huang L, Teffera Y, Yang Y, Zhang Y, Bellon SF, Lee M, Shimanovich R, Bak A, Dominguez C, Norman MH, Harmange JC, Dussault I, Kim TS.. (2008) Discovery of a potent, selective, and orally bioavailable c-Met inhibitor: 1-(2-hydroxy-2-methylpropyl)-N-(5-(7-methoxyquinolin-4-yloxy)pyridin-2-yl)-5-methyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazole-4-carboxamide (AMG 458).. J Med Chem, 51 (13): (3688-3691). [PMID:18553959] |
| 40. 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] |
| 41. Hur W, Velentza A, Kim S, Flatauer L, Jiang X, Valente D, Mason DE, Suzuki M, Larson B, Zhang J, Zagorska A, Didonato M, Nagle A, Warmuth M, Balk SP, Peters EC, Gray NS.. (2008) Clinical stage EGFR inhibitors irreversibly alkylate Bmx kinase.. Bioorg Med Chem Lett, 18 (22): (5916-5919). [PMID:18667312] |
| 42. 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] |
| 43. Velankar AD, Quintini G, Prabhu A, Weber A, Hunaeus G, Voland B, Wuest M, Orjeda C, Harel D, Varghese S, Gore V, Patil M, Gayke D, Herdemann M, Heit I, Zaliani A.. (2010) Synthesis and biological evaluation of novel (4 or 5-aryl)pyrazolyl-indoles as inhibitors of interleukin-2 inducible T-cell kinase (ITK).. Bioorg Med Chem, 18 (12): (4547-4559). [PMID:20472447] |
| 44. 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] |
| 45. 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] |
| 46. 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] |
| 47. Okamoto M, Kojima H, Saito N, Okabe T, Masuda Y, Furuya T, Nagano T.. (2011) Virtual screening and further development of novel ALK inhibitors.. Bioorg Med Chem, 19 (10): (3086-3095). [PMID:21515061] |
| 48. 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] |
| 49. 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] |
| 50. 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] |
| 51. 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] |
| 52. 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] |
| 53. 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] |
| 54. Alder CM, Ambler M, Campbell AJ, Champigny AC, Deakin AM, Harling JD, Harris CA, Longstaff T, Lynn S, Maxwell AC, Mooney CJ, Scullion C, Singh OM, Smith IE, Somers DO, Tame CJ, Wayne G, Wilson C, Woolven JM.. (2013) Identification of a Novel and Selective Series of Itk Inhibitors via a Template-Hopping Strategy.. ACS Med Chem Lett, 4 (10): (948-952). [PMID:24900590] |
| 55. MacKinnon CH, Lau K, Burch JD, Chen Y, Dines J, Ding X, Eigenbrot C, Heifetz A, Jaochico A, Johnson A, Kraemer J, Kruger S, Krülle TM, Liimatta M, Ly J, Maghames R, Montalbetti CA, Ortwine DF, Pérez-Fuertes Y, Shia S, Stein DB, Trani G, Vaidya DG, Wang X, Bromidge SM, Wu LC, Pei Z.. (2013) Structure-based design and synthesis of potent benzothiazole inhibitors of interleukin-2 inducible T cell kinase (ITK).. Bioorg Med Chem Lett, 23 (23): (6331-6335). [PMID:24138940] |
| 56. Shi Q, Tebben A, Dyckman AJ, Li H, Liu C, Lin J, Spergel S, Burke JR, McIntyre KW, Olini GC, Strnad J, Surti N, Muckelbauer JK, Chang C, An Y, Cheng L, Ruan Q, Leftheris K, Carter PH, Tino J, De Lucca GV.. (2014) Purine derivatives as potent Bruton's tyrosine kinase (BTK) inhibitors for autoimmune diseases.. Bioorg Med Chem Lett, 24 (9): (2206-2211). [PMID:24685542] |
| 57. Pastor RM, Burch JD, Magnuson S, Ortwine DF, Chen Y, De La Torre K, Ding X, Eigenbrot C, Johnson A, Liimatta M, Liu Y, Shia S, Wang X, Wu LC, Pei Z.. (2014) Discovery and optimization of indazoles as potent and selective interleukin-2 inducible T cell kinase (ITK) inhibitors.. Bioorg Med Chem Lett, 24 (11): (2448-2452). [PMID:24767842] |
| 58. 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] |
| 59. Burch JD, Lau K, Barker JJ, Brookfield F, Chen Y, Chen Y, Eigenbrot C, Ellebrandt C, Ismaili MH, Johnson A, Kordt D, MacKinnon CH, McEwan PA, Ortwine DF, Stein DB, Wang X, Winkler D, Yuen PW, Zhang Y, Zarrin AA, Pei Z.. (2014) Property- and structure-guided discovery of a tetrahydroindazole series of interleukin-2 inducible T-cell kinase inhibitors.. J Med Chem, 57 (13): (5714-5727). [PMID:24918870] |
| 60. 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] |
| 61. Tan L, Akahane K, McNally R, Reyskens KM, Ficarro SB, Liu S, Herter-Sprie GS, Koyama S, Pattison MJ, Labella K, Johannessen L, Akbay EA, Wong KK, Frank DA, Marto JA, Look TA, Arthur JS, Eck MJ, Gray NS.. (2015) Development of Selective Covalent Janus Kinase 3 Inhibitors.. J Med Chem, 58 (16): (6589-6606). [PMID:26258521] |
| 62. 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] |
| 63. 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] |
| 64. Nakano H, Hasegawa T, Saito N, Furukawa K, Mukaida N, Kojima H, Okabe T, Nagano T.. (2015) Design and synthesis of an in vivo-efficacious PIM3 kinase inhibitor as a candidate anti-pancreatic cancer agent.. Bioorg Med Chem Lett, 25 (24): (5687-5693). [PMID:26547690] |
| 65. 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] |
| 66. 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] |
| 67. 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] |
| 68. 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] |
| 69. Wang Y, Sun Y, Cao R, Liu D, Xie Y, Li L, Qi X, Huang N.. (2017) In Silico Identification of a Novel Hinge-Binding Scaffold for Kinase Inhibitor Discovery.. J Med Chem, 60 (20): (8552-8564). [PMID:28945083] |
| 70. 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] |
| 71. 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] |
| 72. He L, Li D, Zhang C, Bai P, Chen L.. (2017) Discovery of (R)-5-(benzo[d][1,3]dioxol-5-yl)-7-((1-(vinylsulfonyl)pyrrolidin-2-yl)methyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine (B6) as a potent Bmx inhibitor for the treatment of NSCLC.. Bioorg Med Chem Lett, 27 (17): (4171-4175). [PMID:28734581] |
| 73. 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] |
| 74. 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] |
| 75. 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] |
| 76. 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] |
| 77. 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] |
| 78. Liu H, Liang H, Meng H, Deng X, Zhang X, Lai L.. (2018) A novel allosteric inhibitor that prevents IKKβ activation.. Medchemcomm, 9 (2): (239-243). [PMID:30108917] |
| 79. 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] |
| 80. 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] |
| 81. 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] |
| 82. 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] |
| 83. 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] |
| 84. 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] |
| 85. 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] |
| 86. Zhang C, Pei H, He J, Zhu J, Li W, Niu T, Xiang M, Chen L.. (2019) Design, synthesis and evaluation of novel 7H-pyrrolo[2,3-d]pyrimidin-4-amine derivatives as potent, selective and reversible Bruton's tyrosine kinase (BTK) inhibitors for the treatment of rheumatoid arthritis.. Eur J Med Chem, 169 (121-143). [PMID:30875504] |
| 87. 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] |
| 88. 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] |
| 89. 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] |
| 90. 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] |
| 91. 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] |
| 92. Guo Y, Liu Y, Hu N, Yu D, Zhou C, Shi G, Zhang B, Wei M, Liu J, Luo L, Tang Z, Song H, Guo Y, Liu X, Su D, Zhang S, Song X, Zhou X, Hong Y, Chen S, Cheng Z, Young S, Wei Q, Wang H, Wang Q, Lv L, Wang F, Xu H, Sun H, Xing H, Li N, Zhang W, Wang Z, Liu G, Sun Z, Zhou D, Li W, Liu L, Wang L, Wang Z.. (2019) Discovery of Zanubrutinib (BGB-3111), a Novel, Potent, and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase.. J Med Chem, 62 (17): (7923-7940). [PMID:31381333] |
| 93. De Lucca GV, Shi Q, Liu Q, Batt DG, Beaudoin Bertrand M, Rampulla R, Mathur A, Discenza L, D'Arienzo C, Dai J, Obermeier M, Vickery R, Zhang Y, Yang Z, Marathe P, Tebben AJ, Muckelbauer JK, Chang CJ, Zhang H, Gillooly K, Taylor T, Pattoli MA, Skala S, Kukral DW, McIntyre KW, Salter-Cid L, Fura A, Burke JR, Barrish JC, Carter PH, Tino JA.. (2016) Small Molecule Reversible Inhibitors of Bruton's Tyrosine Kinase (BTK): Structure-Activity Relationships Leading to the Identification of 7-(2-Hydroxypropan-2-yl)-4-[2-methyl-3-(4-oxo-3,4-dihydroquinazolin-3-yl)phenyl]-9H-carbazole-1-carboxamide (BMS-935177).. J Med Chem, 59 (17): (7915-7935). [PMID:27531604] |
| 94. 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] |
| 95. Srivastava AS,Ko S,Watterson SH,Pattoli MA,Skala S,Cheng L,Obermeier MT,Vickery R,Discenza LN,D'Arienzo CJ,Gillooly KM,Taylor TL,Pulicicchio C,McIntyre KW,Yip S,Li P,Sun D,Wu DR,Dai J,Wang C,Zhang Y,Wang B,Pawluczyk J,Kempson J,Zhao R,Hou X,Rampulla R,Mathur A,Galella MA,Salter-Cid L,Barrish JC,Carter PH,Fura A,Burke JR,Tino JA. (2020) Driving Potency with Rotationally Stable Atropisomers: Discovery of Pyridopyrimidinedione-Carbazole Inhibitors of BTK.. ACS Med Chem Lett, 11 (11.0): (2195-2203). [PMID:33214829] |
| 96. Shu L,Chen C,Huan X,Huang H,Wang M,Zhang J,Yan Y,Liu J,Zhang T,Zhang D. (2020) Design, synthesis, and pharmacological evaluation of 4- or 6-phenyl-pyrimidine derivatives as novel and selective Janus kinase 3 inhibitors.. Eur J Med Chem, 191 (112148-112148). [PMID:32097841] |
| 97. Liu J,Guiadeen D,Krikorian A,Gao X,Wang J,Boga SB,Alhassan AB,Yu Y,Vaccaro H,Liu S,Yang C,Wu H,Cooper A,de Man J,Kaptein A,Maloney K,Hornak V,Gao YD,Fischmann TO,Raaijmakers H,Vu-Pham D,Presland J,Mansueto M,Xu Z,Leccese E,Zhang-Hoover J,Knemeyer I,Garlisi CG,Bays N,Stivers P,Brandish PE,Hicks A,Kim R,Kozlowski JA. (2016) Discovery of 8-Amino-imidazo[1,5-a]pyrazines as Reversible BTK Inhibitors for the Treatment of Rheumatoid Arthritis.. ACS Med Chem Lett, 7 (2.0): (198-203). [PMID:26985298] |
| 98. He L,Pei H,Zhang C,Shao M,Li D,Tang M,Wang T,Chen X,Xiang M,Chen L. (2018) Design, synthesis and biological evaluation of 7H-pyrrolo[2,3-d]pyrimidin-4-amine derivatives as selective Btk inhibitors with improved pharmacokinetic properties for the treatment of rheumatoid arthritis.. Eur J Med Chem, 145 (96-112). [PMID:29324347] |
| 99. 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] |
| 100. 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] |
| 101. Teng Y,Lu X,Xiao M,Li Z,Zou Y,Ren S,Cheng Y,Luo G,Xiang H. (2020) Discovery of potent and highly selective covalent inhibitors of Bruton's tyrosine kinase bearing triazine scaffold.. Eur J Med Chem, 199 (112339-112339). [PMID:32402933] |
| 102. Gibson, S S and 7 more authors.. (1993) Identification, cloning, and characterization of a novel human T-cell-specific tyrosine kinase located at the hematopoietin complex on chromosome 5q.. Blood, (1): [PMID:8364206] |
| 103. Tanaka, N N, Asao, H H, Ohtani, K K, Nakamura, M M and Sugamura, K K.. (1993) A novel human tyrosine kinase gene inducible in T cells by interleukin 2.. FEBS letters, (7): [PMID:8504851] |
| 104. Heyeck, S D SD, Wilcox, H M HM, Bunnell, S C SC and Berg, L J LJ.. (1997) Lck phosphorylates the activation loop tyrosine of the Itk kinase domain and activates Itk kinase activity.. The Journal of biological chemistry, (3): [PMID:9312162] |
| 105. Yang, W C WC, Collette, Y Y, Nunès, J A JA and Olive, D D.. (2000) Tec kinases: a family with multiple roles in immunity.. Immunity, [PMID:10795735] |
| 106. Perez-Villar, Juan J JJ and 8 more authors.. (2002) Phosphorylation of the linker for activation of T-cells by Itk promotes recruitment of Vav.. Biochemistry, (27): [PMID:12186560] |
| 107. Nore, Beston F BF and 9 more authors.. (2003) Identification of phosphorylation sites within the SH3 domains of Tec family tyrosine kinases.. Biochimica et biophysica acta, (21): [PMID:12573241] |
| 108. Brill, Laurence M LM and 5 more authors.. (2004) Robust phosphoproteomic profiling of tyrosine phosphorylation sites from human T cells using immobilized metal affinity chromatography and tandem mass spectrometry.. Analytical chemistry, (15): [PMID:15144186] |
| 109. Colgan, John J and 8 more authors.. (2004) Cyclophilin A regulates TCR signal strength in CD4+ T cells via a proline-directed conformational switch in Itk.. Immunity, [PMID:15308100] |
| 110. Qi, Qian Q, Sahu, Nisebita N and August, Avery A.. (2006) Tec kinase Itk forms membrane clusters specifically in the vicinity of recruiting receptors.. The Journal of biological chemistry, (15): [PMID:17060314] |
| 111. Huck, Kirsten K and 11 more authors.. (2009) Girls homozygous for an IL-2-inducible T cell kinase mutation that leads to protein deficiency develop fatal EBV-associated lymphoproliferation.. The Journal of clinical investigation, [PMID:19425169] |
| 112. Joseph, Raji E RE, Severin, Andrew A, Min, Lie L, Fulton, D Bruce DB and Andreotti, Amy H AH.. (2009) SH2-dependent autophosphorylation within the Tec family kinase Itk.. Journal of molecular biology, (7): [PMID:19523959] |
| 113. Mayya, Viveka V and 7 more authors.. (2009) Quantitative phosphoproteomic analysis of T cell receptor signaling reveals system-wide modulation of protein-protein interactions.. Science signaling, (18): [PMID:19690332] |
| 114. Voss, Matthias M, Lettau, Marcus M and Janssen, Ottmar O.. (2009) Identification of SH3 domain interaction partners of human FasL (CD178) by phage display screening.. BMC immunology, (6): [PMID:19807924] |
| 115. Del Rincón, Sonia V and 5 more authors.. (2010) Development and validation of a method for profiling post-translational modification activities using protein microarrays.. PloS one, (28): [PMID:20596523] |
| 116. Sela, Meirav M and 15 more authors.. (2011) Sequential phosphorylation of SLP-76 at tyrosine 173 is required for activation of T and mast cells.. The EMBO journal, (1): [PMID:21725281] |
| 117. Tam, Constantine Si Lun CSL and 20 more authors.. (2019) Phase 1 study of selective BTK inhibitor zanubrutinib in B-cell malignancies and safety and efficacy evaluation in CLL.. Blood, (24): [PMID:31340982] |
| 118. 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] |
