Click Here for 5% Off Your First Aladdin Purchase!

IMC-EB10 (anti-FLT3) - Primary antibody, specific to FLT3, >95%, high purity, Human IgG1, INHIBITOR of Tyrosine-protein kinase receptor FLT3 inhibitor

  • Azide Free
  • Carrier Free
  • ExactAb™
  • Low Endotoxin
  • Recombinant
  • Validated
  • ≥95%(SDS-PAGE&SEC)
  • Lot by Lot
Features and benefits
  • Short Overview:

    Purity>95% (SDS-PAGE&SEC); Endotoxin Level<1.0EU/mg; Human IgG1; CHO; ELISA, FACS, Functional assay, Animal Model; Unconjugated

  • Species reactivity(Reacts with): Cynomolgus monkey,Human
  • Isotype: Human IgG1
    Application:
  • Animal Model
  • ELISA
  • Flow Cytometry
  • Functional Assay
Item Number
Ab177924
Grouped product items
SKUSizeAvailabilityPrice Qty
Ab177924-100μg
100μg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$109.90
Ab177924-1mg
1mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$519.90
Ab177924-5mg
5mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$1,399.90
Ab177924-10mg
10mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$2,239.90

Purity>95% (SDS-PAGE&SEC); Endotoxin Level<1.0EU/mg; Human IgG1; CHO; ELISA, FACS, Functional assay, Animal Model; Unconjugated

Basic Description

Product NameIMC-EB10 (anti-FLT3) - Primary antibody, specific to FLT3, >95%, high purity, Human IgG1
SynonymsCD 135 antibody; CD135 antibody; CD135 antigen antibody; Fetal liver kinase 2 antibody; FL cytokine receptor antibody; Flk 2 antibody; Flk2 antibody; Flt 3 antibody; FLT-3 antibody; Flt3 antibody; FLT3_HUMAN antibody; FMS like tyrosine kinase 3 antibody;
Specifications & PurityExactAb™, Validated, Carrier Free, Low Endotoxin, Azide Free, Recombinant, ≥95%(SDS-PAGE&SEC), Lot by Lot
SpecificityFLT3
ConjugationUnconjugated
GradeAzide Free, Carrier Free, ExactAb™, Low Endotoxin, Recombinant, Validated
Action TypeINHIBITOR
Mechanism of actionINHIBITOR of Tyrosine-protein kinase receptor FLT3 inhibitor
Product Description

IMC-EB10 (anti-FLT3) is a fully human IgG1 monoclonal antibody, targeting the FLT3 tyrosine kinase receptor (CD135) with potential antineoplastic activity. It binds to FLT3 and blocks FLT3 ligand binding to FLT3 and subsequent FLT3 phosphorylation, which may result in the inhibition of FLT3-mediated signal transduction pathways.

Product Properties

IsotypeHuman IgG1
Light Chain Typekappa
SDS-PAGE26.7 kDa (Light Chain) & 50.9 kDa (Heavy Chain), under reducing conditions; 191.9 kDa, under non-reducing conditions.
Purification MethodProtein A purified
Purity>95%
FormLiquid
ConcentrationLot by Lot
Storage TempStore at -80°C,Avoid repeated freezing and thawing
Shipped InIce chest + Ice pads
Stability And StorageStore at -80℃ for 24 months. Upon delivery aliquot. Avoid freeze/thaw cycle.

Images

IMC-EB10 (anti-FLT3) (Ab177924) - Flow
Human FLT3 HEK293 cells were stained with IMC-EB10 (anti-FLT3) (Ab177924) and negative control protein respectively, washed and then followed by PE and analyzed with FACS, EC ₅₀ for this effect is 110 nM.

IMC-EB10 (anti-FLT3) (Ab177924) - SEC
The purity of IMC-EB10 (anti-FLT3) (Ab177924) is more than 95% verified by HPLC.

Associated Targets

FLT3 Tclin Receptor-type tyrosine-protein kinase FLT3 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

Certificates

Certificate of Analysis(COA)

Enter Lot Number to search for COA:

To view the certificate results,please click on a Lot number.For Lot numbers from past orders,please use our order status section

3 results found

Lot NumberCertificate TypeDateItem
ZJ24F0607184Certificate of AnalysisJun 21, 2024 Ab177924
ZJ24F0607183Certificate of AnalysisJun 21, 2024 Ab177924
ZJ24F0607182Certificate of AnalysisJun 21, 2024 Ab177924

Related Documents

References

1. Huber K, Brault L, Fedorov O, Gasser C, Filippakopoulos P, Bullock AN, Fabbro D, Trappe J, Schwaller J, Knapp S et al..  (2012)  7,8-dichloro-1-oxo-β-carbolines as a versatile scaffold for the development of potent and selective kinase inhibitors with unusual binding modes..  J Med Chem,  55  (1): (403-13).  [PMID:22136433]
2. Verstraete K, Vandriessche G, Januar M, Elegheert J, Shkumatov AV, Desfosses A, Van Craenenbroeck K, Svergun DI, Gutsche I, Vergauwen B et al..  (2011)  Structural insights into the extracellular assembly of the hematopoietic Flt3 signaling complex..  Blood,  118  (1): (60-8).  [PMID:21389326]
3. Griffith J, Black J, Faerman C, Swenson L, Wynn M, Lu F, Lippke J, Saxena K.  (2004)  The structural basis for autoinhibition of FLT3 by the juxtamembrane domain..  Mol Cell,  13  (2): (169-78).  [PMID:14759363]
4. McHardy T, Caldwell JJ, Cheung KM, Hunter LJ, Taylor K, Rowlands M, Ruddle R, Henley A, de Haven Brandon A, Valenti M et al..  (2010)  Discovery of 4-amino-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamides as selective, orally active inhibitors of protein kinase B (Akt)..  J Med Chem,  53  (5): (2239-49).  [PMID:20151677]
5. Huang WS, Metcalf CA, Sundaramoorthi R, Wang Y, Zou D, Thomas RM, Zhu X, Cai L, Wen D, Liu S et al..  (2010)  Discovery of 3-[2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a potent, orally active pan-inhibitor of breakpoint cluster region-abelson (BCR-ABL) kinase including the T315I gatekeeper mutant..  J Med Chem,  53  (12): (4701-19).  [PMID:20513156]
6. Albert DH, Tapang P, Magoc TJ, Pease LJ, Reuter DR, Wei RQ, Li J, Guo J, Bousquet PF, Ghoreishi-Haack NS et al..  (2006)  Preclinical activity of ABT-869, a multitargeted receptor tyrosine kinase inhibitor..  Mol Cancer Ther,  (4): (995-1006).  [PMID:16648571]
7. Galkin AV, Melnick JS, Kim S, Hood TL, Li N, Li L, Xia G, Steensma R, Chopiuk G, Jiang J et al..  (2007)  Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK..  Proc Natl Acad Sci USA,  104  (1): (270-5).  [PMID:17185414]
8. 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]
9. Ballou LM, Selinger ES, Choi JY, Drueckhammer DG, Lin RZ.  (2007)  Inhibition of mammalian target of rapamycin signaling by 2-(morpholin-1-yl)pyrimido[2,1-alpha]isoquinolin-4-one..  J Biol Chem,  282  (33): (24463-70).  [PMID:17562705]
10. Mahboobi S, Uecker A, Sellmer A, Cénac C, Höcher H, Pongratz H, Eichhorn E, Hufsky H, Trümpler A, Sicker M et al..  (2006)  Novel bis(1H-indol-2-yl)methanones as potent inhibitors of FLT3 and platelet-derived growth factor receptor tyrosine kinase..  J Med Chem,  49  (11): (3101-15).  [PMID:16722630]
11. Furet P, Bold G, Meyer T, Roesel J, Guagnano V.  (2006)  Aromatic interactions with phenylalanine 691 and cysteine 828: a concept for FMS-like tyrosine kinase-3 inhibition. Application to the discovery of a new class of potential antileukemia agents..  J Med Chem,  49  (15): (4451-4).  [PMID:16854049]
12. Murata K, Kumagai H, Kawashima T, Tamitsu K, Irie M, Nakajima H, Suzu S, Shibuya M, Kamihira S, Nosaka T et al..  (2003)  Selective cytotoxic mechanism of GTP-14564, a novel tyrosine kinase inhibitor in leukemia cells expressing a constitutively active Fms-like tyrosine kinase 3 (FLT3)..  J Biol Chem,  278  (35): (32892-8).  [PMID:12815052]
13. 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]
14. William AD, Lee AC, Blanchard S, Poulsen A, Teo EL, Nagaraj H, Tan E, Chen D, Williams M, Sun ET et al..  (2011)  Discovery of the macrocycle 11-(2-pyrrolidin-1-yl-ethoxy)-14,19-dioxa-5,7,26-triaza-tetracyclo[19.3.1.1(2,6).1(8,12)]heptacosa-1(25),2(26),3,5,8,10,12(27),16,21,23-decaene (SB1518), a potent Janus kinase 2/fms-like tyrosine kinase-3 (JAK2/FLT3) inhibitor for the treatment of myelofibrosis and lymphoma..  J Med Chem,  54  (13): (4638-58).  [PMID:21604762]
15. Oyarzabal J, Zarich N, Albarran MI, Palacios I, Urbano-Cuadrado M, Mateos G, Reymundo I, Rabal O, Salgado A, Corrionero A et al..  (2010)  Discovery of mitogen-activated protein kinase-interacting kinase 1 inhibitors by a comprehensive fragment-oriented virtual screening approach..  J Med Chem,  53  (18): (6618-28).  [PMID:20722422]
16. Devadas B, Selness SR, Xing L, Madsen HM, Marrufo LD, Shieh H, Messing DM, Yang JZ, Morgan HM, Anderson GD et al..  (2011)  Substituted N-aryl-6-pyrimidinones: a new class of potent, selective, and orally active p38 MAP kinase inhibitors..  Bioorg Med Chem Lett,  21  (13): (3856-60).  [PMID:21620699]
17. Heinrich MC, Griffith D, McKinley A, Patterson J, Presnell A, Ramachandran A, Debiec-Rychter M.  (2012)  Crenolanib inhibits the drug-resistant PDGFRA D842V mutation associated with imatinib-resistant gastrointestinal stromal tumors..  Clin Cancer Res,  18  (16): (4375-84).  [PMID:22745105]
18. Currie KS, Kropf JE, Lee T, Blomgren P, Xu J, Zhao Z, Gallion S, Whitney JA, Maclin D, Lansdon EB et al..  (2014)  Discovery of GS-9973, a selective and orally efficacious inhibitor of spleen tyrosine kinase..  J Med Chem,  57  (9): (3856-73).  [PMID:24779514]
19. Pan BS, Chan GK, Chenard M, Chi A, Davis LJ, Deshmukh SV, Gibbs JB, Gil S, Hang G, Hatch H et al..  (2010)  MK-2461, a novel multitargeted kinase inhibitor, preferentially inhibits the activated c-Met receptor..  Cancer Res,  70  (4): (1524-33).  [PMID:20145145]
20. Eriksson A, Hermanson M, Wickström M, Lindhagen E, Ekholm C, Jenmalm Jensen A, Löthgren A, Lehmann F, Larsson R, Parrow V et al..  (2012)  The novel tyrosine kinase inhibitor AKN-028 has significant antileukemic activity in cell lines and primary cultures of acute myeloid leukemia..  Blood Cancer J,  (3): (e81).  [PMID:22864397]
21. Machrouhi F, Ouhamou N, Laderoute K, Calaoagan J, Bukhtiyarova M, Ehrlich PJ, Klon AE.  (2010)  The rational design of a novel potent analogue of the 5'-AMP-activated protein kinase inhibitor compound C with improved selectivity and cellular activity..  Bioorg Med Chem Lett,  20  (22): (6394-9).  [PMID:20932747]
22. 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]
23. Sampson PB, Liu Y, Patel NK, Feher M, Forrest B, Li SW, Edwards L, Laufer R, Lang Y, Ban F et al..  (2015)  The discovery of Polo-like kinase 4 inhibitors: design and optimization of spiro[cyclopropane-1,3'[3H]indol]-2'(1'H).ones as orally bioavailable antitumor agents..  J Med Chem,  58  (1): (130-46).  [PMID:24867403]
24. Akeno-Stuart N, Croyle M, Knauf JA, Malaguarnera R, Vitagliano D, Santoro M, Stephan C, Grosios K, Wartmann M, Cozens R et al..  (2007)  The RET kinase inhibitor NVP-AST487 blocks growth and calcitonin gene expression through distinct mechanisms in medullary thyroid cancer cells..  Cancer Res,  67  (14): (6956-64).  [PMID:17638907]
25. Manthey CL, Johnson DL, Illig CR, Tuman RW, Zhou Z, Baker JF, Chaikin MA, Donatelli RR, Franks CF, Zeng L et al..  (2009)  JNJ-28312141, a novel orally active colony-stimulating factor-1 receptor/FMS-related receptor tyrosine kinase-3 receptor tyrosine kinase inhibitor with potential utility in solid tumors, bone metastases, and acute myeloid leukemia..  Mol Cancer Ther,  (11): (3151-61).  [PMID:19887542]
26. Weisberg E, Roesel J, Bold G, Furet P, Jiang J, Cools J, Wright RD, Nelson E, Barrett R, Ray A et al..  (2008)  Antileukemic effects of the novel, mutant FLT3 inhibitor NVP-AST487: effects on PKC412-sensitive and -resistant FLT3-expressing cells..  Blood,  112  (13): (5161-70).  [PMID:18820131]
27. Trudel S, Li ZH, Wei E, Wiesmann M, Chang H, Chen C, Reece D, Heise C, Stewart AK.  (2005)  CHIR-258, a novel, multitargeted tyrosine kinase inhibitor for the potential treatment of t(4;14) multiple myeloma..  Blood,  105  (7): (2941-8).  [PMID:15598814]
28. Shiotsu Y, Kiyoi H, Ishikawa Y, Tanizaki R, Shimizu M, Umehara H, Ishii K, Mori Y, Ozeki K, Minami Y et al..  (2009)  KW-2449, a novel multikinase inhibitor, suppresses the growth of leukemia cells with FLT3 mutations or T315I-mutated BCR/ABL translocation..  Blood,  114  (8): (1607-17).  [PMID:19541823]
29. Weisberg E, Boulton C, Kelly LM, Manley P, Fabbro D, Meyer T, Gilliland DG, Griffin JD.  (2002)  Inhibition of mutant FLT3 receptors in leukemia cells by the small molecule tyrosine kinase inhibitor PKC412..  Cancer Cell,  (5): (433-43).  [PMID:12124173]
30. Wilhelm SM, Carter C, Tang L, Wilkie D, McNabola A, Rong H, Chen C, Zhang X, Vincent P, McHugh M et al..  (2004)  BAY 43-9006 exhibits broad spectrum oral antitumor activity and targets the RAF/MEK/ERK pathway and receptor tyrosine kinases involved in tumor progression and angiogenesis..  Cancer Res,  64  (19): (7099-109).  [PMID:15466206]
31. Lee HK, Kim HW, Lee IY, Lee J, Lee J, Jung DS, Lee SY, Park SH, Hwang H, Choi JS et al..  (2014)  G-749, a novel FLT3 kinase inhibitor, can overcome drug resistance for the treatment of acute myeloid leukemia..  Blood,  123  (14): (2209-19).  [PMID:24532805]
32. 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]
33. Pandey A, Volkots DL, Seroogy JM, Rose JW, Yu JC, Lambing JL, Hutchaleelaha A, Hollenbach SJ, Abe K, Giese NA et al..  (2002)  Identification of orally active, potent, and selective 4-piperazinylquinazolines as antagonists of the platelet-derived growth factor receptor tyrosine kinase family..  J Med Chem,  45  (17): (3772-93).  [PMID:12166950]
34. Coombs TC, Tanega C, Shen M, Wang JL, Auld DS, Gerritz SW, Schoenen FJ, Thomas CJ, Aubé J.  (2013)  Small-molecule pyrimidine inhibitors of the cdc2-like (Clk) and dual specificity tyrosine phosphorylation-regulated (Dyrk) kinases: development of chemical probe ML315..  Bioorg Med Chem Lett,  23  (12): (3654-61).  [PMID:23642479]
35. Hudkins RL, Becknell NC, Zulli AL, Underiner TL, Angeles TS, Aimone LD, Albom MS, Chang H, Miknyoczki SJ, Hunter K et al..  (2012)  Synthesis and biological profile of the pan-vascular endothelial growth factor receptor/tyrosine kinase with immunoglobulin and epidermal growth factor-like homology domains 2 (VEGF-R/TIE-2) inhibitor 11-(2-methylpropyl)-12,13-dihydro-2-methyl-8-(pyrimidin-2-ylamino)-4H-indazolo[5,4-a]pyrrolo[3,4-c]carbazol-4-one (CEP-11981): a novel oncology therapeutic agent..  J Med Chem,  55  (2): (903-13).  [PMID:22148921]
36. Weïwer M, Spoonamore J, Wei J, Guichard B, Ross NT, Masson K, Silkworth W, Dandapani S, Palmer M, Scherer CA et al..  (2012)  A Potent and Selective Quinoxalinone-Based STK33 Inhibitor Does Not Show Synthetic Lethality in KRAS-Dependent Cells..  ACS Med Chem Lett,  (12): (1034-1038).  [PMID:23256033]
37. 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]
38. 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]
39. Papeo G, Posteri H, Borghi D, Busel AA, Caprera F, Casale E, Ciomei M, Cirla A, Corti E, D'Anello M et al..  (2015)  Discovery of 2-[1-(4,4-Difluorocyclohexyl)piperidin-4-yl]-6-fluoro-3-oxo-2,3-dihydro-1H-isoindole-4-carboxamide (NMS-P118): A Potent, Orally Available, and Highly Selective PARP-1 Inhibitor for Cancer Therapy..  J Med Chem,  58  (17): (6875-98).  [PMID:26222319]
40. Khan PM, Correa RG, Divlianska DB, Peddibhotla S, Sessions EH, Magnuson G, Brown B, Suyama E, Yuan H, Mangravita-Novo A et al..  (2011)  Identification of Inhibitors of NOD1-Induced Nuclear Factor-κB Activation..  ACS Med Chem Lett,  (10): (780-785).  [PMID:22003428]
41. Tap WD, Wainberg ZA, Anthony SP, Ibrahim PN, Zhang C, Healey JH, Chmielowski B, Staddon AP, Cohn AL, Shapiro GI et al..  (2015)  Structure-Guided Blockade of CSF1R Kinase in Tenosynovial Giant-Cell Tumor..  N Engl J Med,  373  (5): (428-37).  [PMID:26222558]
42. Genovese MC, Hsia E, Belkowski SM, Chien C, Masterson T, Thurmond RL, Manthey CL, Yan XD, Ge T, Franks C et al..  (2015)  Results from a Phase IIA Parallel Group Study of JNJ-40346527, an Oral CSF-1R Inhibitor, in Patients with Active Rheumatoid Arthritis despite Disease-modifying Antirheumatic Drug Therapy..  J Rheumatol,  42  (10): (1752-60).  [PMID:26233509]
43. William AD, Lee AC, Goh KC, Blanchard S, Poulsen A, Teo EL, Nagaraj H, Lee CP, Wang H, Williams M et al..  (2012)  Discovery of kinase spectrum selective macrocycle (16E)-14-methyl-20-oxa-5,7,14,26-tetraazatetracyclo[19.3.1.1(2,6).1(8,12)]heptacosa-1(25),2(26),3,5,8(27),9,11,16,21,23-decaene (SB1317/TG02), a potent inhibitor of cyclin dependent kinases (CDKs), Janus kinase 2 (JAK2), and fms-like tyrosine kinase-3 (FLT3) for the treatment of cancer..  J Med Chem,  55  (1): (169-96).  [PMID:22148278]
44. 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]
45. Rosnet O, Bühring HJ, Marchetto S, Rappold I, Lavagna C, Sainty D, Arnoulet C, Chabannon C, Kanz L, Hannum C et al..  (1996)  Human FLT3/FLK2 receptor tyrosine kinase is expressed at the surface of normal and malignant hematopoietic cells..  Leukemia,  10  (2): (238-48).  [PMID:8637232]
46. Huang WS, Liu S, Zou D, Thomas M, Wang Y, Zhou T, Romero J, Kohlmann A, Li F, Qi J et al..  (2016)  Discovery of Brigatinib (AP26113), a Phosphine Oxide-Containing, Potent, Orally Active Inhibitor of Anaplastic Lymphoma Kinase..  J Med Chem,  59  (10): (4948-64).  [PMID:27144831]
47. Patel S, Cohen F, Dean BJ, De La Torre K, Deshmukh G, Estrada AA, Ghosh AS, Gibbons P, Gustafson A, Huestis MP et al..  (2015)  Discovery of dual leucine zipper kinase (DLK, MAP3K12) inhibitors with activity in neurodegeneration models..  J Med Chem,  58  (1): (401-18).  [PMID:25341110]
48. 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]
49. 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]
50. Lam B, Arikawa Y, Cramlett J, Dong Q, de Jong R, Feher V, Grimshaw CE, Farrell PJ, Hoffman ID, Jennings A et al..  (2016)  Discovery of TAK-659 an orally available investigational inhibitor of Spleen Tyrosine Kinase (SYK)..  Bioorg Med Chem Lett,  26  (24): (5947-5950).  [PMID:27839918]
51. 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,  (11): (1142-1147).  [PMID:29152045]
52. Jarusiewicz JA, Jeon JY, Connelly MC, Chen Y, Yang L, Baker SD, Guy RK.  (2017)  Discovery of a Diaminopyrimidine FLT3 Inhibitor Active against Acute Myeloid Leukemia..  ACS Omega,  (5): (1985-2009).  [PMID:28580438]
53. Mizuki M, Fenski R, Halfter H, Matsumura I, Schmidt R, Müller C, Grüning W, Kratz-Albers K, Serve S, Steur C et al..  (2000)  Flt3 mutations from patients with acute myeloid leukemia induce transformation of 32D cells mediated by the Ras and STAT5 pathways..  Blood,  96  (12): (3907-14).  [PMID:11090077]
54. Burger MT, Nishiguchi G, Han W, Lan J, Simmons R, Atallah G, Ding Y, Tamez V, Zhang Y, Mathur M et al..  (2015)  Identification of N-(4-((1R,3S,5S)-3-Amino-5-methylcyclohexyl)pyridin-3-yl)-6-(2,6-difluorophenyl)-5-fluoropicolinamide (PIM447), a Potent and Selective Proviral Insertion Site of Moloney Murine Leukemia (PIM) 1, 2, and 3 Kinase Inhibitor in Clinical Trials for Hematological Malignancies..  J Med Chem,  58  (21): (8373-86).  [PMID:26505898]
55. Yan SB, Peek VL, Ajamie R, Buchanan SG, Graff JR, Heidler SA, Hui YH, Huss KL, Konicek BW, Manro JR et al..  (2013)  LY2801653 is an orally bioavailable multi-kinase inhibitor with potent activity against MET, MST1R, and other oncoproteins, and displays anti-tumor activities in mouse xenograft models..  Invest New Drugs,  31  (4): (833-44).  [PMID:23275061]
56. Yin Y, Zheng K, Eid N, Howard S, Jeong JH, Yi F, Guo J, Park CM, Bibian M, Wu W et al..  (2015)  Bis-aryl urea derivatives as potent and selective LIM kinase (Limk) inhibitors..  J Med Chem,  58  (4): (1846-61).  [PMID:25621531]
57. Glaser KB, Li J, Marcotte PA, Magoc TJ, Guo J, Reuter DR, Tapang P, Wei RQ, Pease LJ, Bui MH et al..  (2012)  Preclinical characterization of ABT-348, a kinase inhibitor targeting the aurora, vascular endothelial growth factor receptor/platelet-derived growth factor receptor, and Src kinase families..  J Pharmacol Exp Ther,  343  (3): (617-27).  [PMID:22935731]
58. Patwardhan PP, Ivy KS, Musi E, de Stanchina E, Schwartz GK.  (2016)  Significant blockade of multiple receptor tyrosine kinases by MGCD516 (Sitravatinib), a novel small molecule inhibitor, shows potent anti-tumor activity in preclinical models of sarcoma..  Oncotarget,  (4): (4093-109).  [PMID:26675259]
59. Gucký T, Řezníčková E, Radošová Muchová T, Jorda R, Klejová Z, Malínková V, Berka K, Bazgier V, Ajani H, Lepšík M et al..  (2018)  Discovery of N2-(4-Amino-cyclohexyl)-9-cyclopentyl- N6-(4-morpholin-4-ylmethyl-phenyl)- 9H-purine-2,6-diamine as a Potent FLT3 Kinase Inhibitor for Acute Myeloid Leukemia with FLT3 Mutations..  J Med Chem,  61  (9): (3855-3869).  [PMID:29672049]
60. Patel S, Harris SF, Gibbons P, Deshmukh G, Gustafson A, Kellar T, Lin H, Liu X, Liu Y, Liu Y et al..  (2015)  Scaffold-Hopping and Structure-Based Discovery of Potent, Selective, And Brain Penetrant N-(1H-Pyrazol-3-yl)pyridin-2-amine Inhibitors of Dual Leucine Zipper Kinase (DLK, MAP3K12)..  J Med Chem,  58  (20): (8182-99).  [PMID:26431428]
61. Zhang J, Jiang X, Jiang Y, Guo M, Zhang S, Li J, He J, Liu J, Wang J, Ouyang L.  (2016)  Recent advances in the development of dual VEGFR and c-Met small molecule inhibitors as anticancer drugs..  Eur J Med Chem,  108  (3): (495-504).  [PMID:26717201]
62. Yang T, Hu M, Qi W, Yang Z, Tang M, He J, Chen Y, Bai P, Yuan X, Zhang C et al..  (2019)  Discovery of Potent and Orally Effective Dual Janus Kinase 2/FLT3 Inhibitors for the Treatment of Acute Myelogenous Leukemia and Myeloproliferative Neoplasms..  J Med Chem,  62  (22): (10305-10320).  [PMID:31670517]
63. Ren X, Pan X, Zhang Z, Wang D, Lu X, Li Y, Wen D, Long H, Luo J, Feng Y et al..  (2013)  Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinib..  J Med Chem,  56  (3): (879-94).  [PMID:23301703]
64. Ma H, Nguyen B, Li L, Greenblatt S, Williams A, Zhao M, Levis M, Rudek M, Duffield A, Small D.  (2014)  TTT-3002 is a novel FLT3 tyrosine kinase inhibitor with activity against FLT3-associated leukemias in vitro and in vivo..  Blood,  123  (10): (1525-34).  [PMID:24408321]
65. Yoshida A, Ookura M, Zokumasu K, Ueda T.  (2014)  Gö6976, a FLT3 kinase inhibitor, exerts potent cytotoxic activity against acute leukemia via inhibition of survivin and MCL-1..  Biochem Pharmacol,  90  (1): (16-24).  [PMID:24735609]
66. Ma B, Bohnert T, Otipoby KL, Tien E, Arefayene M, Bai J, Bajrami B, Bame E, Chan TR, Humora M et al..  (2020)  Discovery of BIIB068: A Selective, Potent, Reversible Bruton's Tyrosine Kinase Inhibitor as an Orally Efficacious Agent for Autoimmune Diseases..  J Med Chem,  63  (21): (12526-12541).  [PMID:32696648]
67. 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]
68. Gummadi VR, Boruah A, Ainan BR, Vare BR, Manda S, Gondle HP, Kumar SN, Mukherjee S, Gore ST, Krishnamurthy NR et al..  (2020)  Discovery of CA-4948, an Orally Bioavailable IRAK4 Inhibitor for Treatment of Hematologic Malignancies..  ACS Med Chem Lett,  11  (12): (2374-2381).  [PMID:33335659]
69. Zhang C, Qi W, Li Y, Tang M, Yang T, Liu K, Chen Y, Deng D, Xiang M, Chen L.  (2021)  Discovery of 3-(4-(2-((1 H-Indol-5-yl)amino)-5-fluoropyrimidin-4-yl)-1 H-pyrazol-1-yl)propanenitrile Derivatives as Selective TYK2 Inhibitors for the Treatment of Inflammatory Bowel Disease.  Journal of Medicinal Chemistry,  129  (3): (589-97).  [PMID:33593051]
70. Yang T, Hu M, Chen Y, Xiang M, Tang M, Qi W, Shi M, He J, Yuan X, Zhang C et al..  (2020)  N-(Pyrimidin-2-yl)-1,2,3,4-tetrahydroisoquinolin-6-amine Derivatives as Selective Janus Kinase 2 Inhibitors for the Treatment of Myeloproliferative Neoplasms..  J Med Chem,  63  (23): (14921-14936).  [PMID:33256400]
71. Reddy MV, Akula B, Cosenza SC, Athuluridivakar S, Mallireddigari MR, Pallela VR, Billa VK, Subbaiah DR, Bharathi EV, Vasquez-Del Carpio R et al..  (2014)  Discovery of 8-cyclopentyl-2-[4-(4-methyl-piperazin-1-yl)-phenylamino]-7-oxo-7,8-dihydro-pyrido[2,3-d]pyrimidine-6-carbonitrile (7x) as a potent inhibitor of cyclin-dependent kinase 4 (CDK4) and AMPK-related kinase 5 (ARK5)..  J Med Chem,  57  (3): (578-99).  [PMID:24417566]
72. Tadesse S, Yu M, Mekonnen LB, Lam F, Islam S, Tomusange K, Rahaman MH, Noll B, Basnet SK, Teo T et al..  (2017)  Highly Potent, Selective, and Orally Bioavailable 4-Thiazol-N-(pyridin-2-yl)pyrimidin-2-amine Cyclin-Dependent Kinases 4 and 6 Inhibitors as Anticancer Drug Candidates: Design, Synthesis, and Evaluation..  J Med Chem,  60  (5): (1892-1915).  [PMID:28156111]
73. Yang H, Chennamaneni LR, Ho MWT, Ang SH, Tan ESW, Jeyaraj DA, Yeap YS, Liu B, Ong EH, Joy JK et al..  (2018)  Optimization of Selective Mitogen-Activated Protein Kinase Interacting Kinases 1 and 2 Inhibitors for the Treatment of Blast Crisis Leukemia..  J Med Chem,  61  (10): (4348-4369).  [PMID:29683667]
74. Seunghee Hong,Jinhee Kim,Sun-Mi Yun,Hyunseung Lee,Yoonsu Park,Soon-Sun Hong,Sungwoo Hong.  (2013-04-23)  Discovery of new benzothiazole-based inhibitors of breakpoint cluster region-Abelson kinase including the T315I mutant..  Journal of medicinal chemistry,  56  ((9)): (3531-3545).  [PMID:23600806]
75. Sung Hee Hwang, Aaron T Wecksler, Guodong Zhang, Christophe Morisseau, Long V Nguyen, Samuel H Fu, Bruce D Hammock,.  (2013-06-04)  Synthesis and biological evaluation of sorafenib- and regorafenib-like sEH inhibitors..  Bioorganic & medicinal chemistry letters,  23  ((13)): ( 3732-3737 ).  [PMID:23726028]
76. Ajit Dhananjay Jagtap,Pei-Teh Chang,Jia-Rong Liu,Hsiao-Chun Wang,Nagendra B Kondekar,Li-Jiuan Shen,Hsiang-Wen Tseng,Grace Shiahuy Chen,Ji-Wang Chern.  (2014-08-05)  Novel acylureidoindolin-2-one derivatives as dual Aurora B/FLT3 inhibitors for the treatment of acute myeloid leukemia..  European journal of medicinal chemistry,  85  (268-288).  [PMID:25089810]
77. Revesz L, Blum E, Di Padova FE, Buhl T, Feifel R, Gram H, Hiestand P, Manning U, Rucklin G..  (2004)  SAR of benzoylpyridines and benzophenones as p38alpha MAP kinase inhibitors with oral activity..  Bioorg Med Chem Lett,  14  (13): (3601-3605).  [PMID:15177483]
78. Aronov AM, Baker C, Bemis GW, Cao J, Chen G, Ford PJ, Germann UA, Green J, Hale MR, Jacobs M, Janetka JW, Maltais F, Martinez-Botella G, Namchuk MN, Straub J, Tang Q, Xie X..  (2007)  Flipped out: structure-guided design of selective pyrazolylpyrrole ERK inhibitors..  J Med Chem,  50  (6): (1280-1287).  [PMID:17300186]
79. Dinges J, Albert DH, Arnold LD, Ashworth KL, Akritopoulou-Zanze I, Bousquet PF, Bouska JJ, Cunha GA, Davidsen SK, Diaz GJ, Djuric SW, Gasiecki AF, Gintant GA, Gracias VJ, Harris CM, Houseman KA, Hutchins CW, Johnson EF, Li H, Marcotte PA, Martin RL, Michaelides MR, Nyein M, Sowin TJ, Su Z, Tapang PH, Xia Z, Zhang HQ..  (2007)  1,4-Dihydroindeno[1,2-c]pyrazoles with acetylenic side chains as novel and potent multitargeted receptor tyrosine kinase inhibitors with low affinity for the hERG ion channel..  J Med Chem,  50  (9): (2011-2029).  [PMID:17425296]
80. Manetti F, Santucci A, Locatelli GA, Maga G, Spreafico A, Serchi T, Orlandini M, Bernardini G, Caradonna NP, Spallarossa A, Brullo C, Schenone S, Bruno O, Ranise A, Bondavalli F, Hoffmann O, Bologna M, Angelucci A, Botta M..  (2007)  Identification of a novel pyrazolo[3,4-d]pyrimidine able to inhibit cell proliferation of a human osteogenic sarcoma in vitro and in a xenograft model in mice..  J Med Chem,  50  (23): (5579-5588).  [PMID:17929792]
81. Ji Z, Ahmed AA, Albert DH, Bouska JJ, Bousquet PF, Cunha GA, Diaz G, Glaser KB, Guo J, Harris CM, Li J, Marcotte PA, Moskey MD, Oie T, Pease L, Soni NB, Stewart KD, Davidsen SK, Michaelides MR..  (2008)  3-amino-benzo[d]isoxazoles as novel multitargeted inhibitors of receptor tyrosine kinases..  J Med Chem,  51  (5): (1231-1241).  [PMID:18260617]
82. Weiss MM, Harmange JC, Polverino AJ, Bauer D, Berry L, Berry V, Borg G, Bready J, Chen D, Choquette D, Coxon A, DeMelfi T, Doerr N, Estrada J, Flynn J, Graceffa RF, Harriman SP, Kaufman S, La DS, Long A, Neervannan S, Patel VF, Potashman M, Regal K, Roveto PM, Schrag ML, Starnes C, Tasker A, Teffera Y, Whittington DA, Zanon R..  (2008)  Evaluation of a series of naphthamides as potent, orally active vascular endothelial growth factor receptor-2 tyrosine kinase inhibitors..  J Med Chem,  51  (6): (1668-1680).  [PMID:18324759]
83. McDermott U, Sharma SV, Dowell L, Greninger P, Montagut C, Lamb J, Archibald H, Raudales R, Tam A, Lee D, Rothenberg SM, Supko JG, Sordella R, Ulkus LE, Iafrate AJ, Maheswaran S, Njauw CN, Tsao H, Drew L, Hanke JH, Ma XJ, Erlander MG, Gray NS, Haber DA, Settleman J..  (2007)  Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling..  Proc Natl Acad Sci U S A,  104  (50): (19936-19941).  [PMID:18077425]
84. 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]
85. Jiang JK, Ghoreschi K, Deflorian F, Chen Z, Perreira M, Pesu M, Smith J, Nguyen DT, Liu EH, Leister W, Costanzi S, O'Shea JJ, Thomas CJ..  (2008)  Examining the chirality, conformation and selective kinase inhibition of 3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)piperidin-1-yl)-3-oxopropanenitrile (CP-690,550)..  J Med Chem,  51  (24): (8012-8018).  [PMID:19053756]
86. Li J, Kaoud TS, Laroche C, Dalby KN, Kerwin SM..  (2009)  Synthesis and biological evaluation of p38alpha kinase-targeting dialkynylimidazoles..  Bioorg Med Chem Lett,  19  (22): (6293-6297).  [PMID:19822424]
87. Ledeboer MW, Pierce AC, Duffy JP, Gao H, Messersmith D, Salituro FG, Nanthakumar S, Come J, Zuccola HJ, Swenson L, Shlyakter D, Mahajan S, Hoock T, Fan B, Tsai WJ, Kolaczkowski E, Carrier S, Hogan JK, Zessis R, Pazhanisamy S, Bennani YL..  (2009)  2-Aminopyrazolo[1,5-a]pyrimidines as potent and selective inhibitors of JAK2..  Bioorg Med Chem Lett,  19  (23): (6529-6533).  [PMID:19857967]
88. 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]
89. Choi HG, Ren P, Adrian F, Sun F, Lee HS, Wang X, Ding Q, Zhang G, Xie Y, Zhang J, Liu Y, Tuntland T, Warmuth M, Manley PW, Mestan J, Gray NS, Sim T..  (2010)  A type-II kinase inhibitor capable of inhibiting the T315I "gatekeeper" mutant of Bcr-Abl..  J Med Chem,  53  (15): (5439-5448).  [PMID:20604564]
90. Kim MH, Kim M, Yu H, Kim H, Yoo KH, Sim T, Hah JM..  (2011)  Structure based design and syntheses of amino-1H-pyrazole amide derivatives as selective Raf kinase inhibitors in melanoma cells..  Bioorg Med Chem,  19  (6): (1915-1923).  [PMID:21353571]
91. Ren X, Duan L, He Q, Zhang Z, Zhou Y, Wu D, Pan J, Pei D, Ding K, Ding K..  (2010)  Identification of Niclosamide as a New Small-Molecule Inhibitor of the STAT3 Signaling Pathway..  ACS Med Chem Lett,  (9): (454-459).  [PMID:24900231]
92. Peterson EA, Andrews PS, Be X, Boezio AA, Bush TL, Cheng AC, Coats JR, Colletti AE, Copeland KW, DuPont M, Graceffa R, Grubinska B, Harmange JC, Kim JL, Mullady EL, Olivieri P, Schenkel LB, Stanton MK, Teffera Y, Whittington DA, Cai T, La DS..  (2011)  Discovery of triazine-benzimidazoles as selective inhibitors of mTOR..  Bioorg Med Chem Lett,  21  (7): (2064-2070).  [PMID:21376583]
93. Shallal HM, Russu WA..  (2011)  Discovery, synthesis, and investigation of the antitumor activity of novel piperazinylpyrimidine derivatives..  Eur J Med Chem,  46  (6): (2043-2057).  [PMID:21429632]
94. Lin WH, Hsieh SY, Yen SC, Chen CT, Yeh TK, Hsu T, Lu CT, Chen CP, Chen CW, Chou LH, Huang YL, Cheng AH, Chang YI, Tseng YJ, Yen KR, Chao YS, Hsu JT, Jiaang WT..  (2011)  Discovery and evaluation of 3-phenyl-1H-5-pyrazolylamine-based derivatives as potent, selective and efficacious inhibitors of FMS-like tyrosine kinase-3 (FLT3)..  Bioorg Med Chem,  19  (14): (4173-4182).  [PMID:21708468]
95. Radi M, Brullo C, Crespan E, Tintori C, Musumeci F, Biava M, Schenone S, Dreassi E, Zamperini C, Maga G, Pagano D, Angelucci A, Bologna M, Botta M..  (2011)  Identification of potent c-Src inhibitors strongly affecting the proliferation of human neuroblastoma cells..  Bioorg Med Chem Lett,  21  (19): (5928-5933).  [PMID:21856155]
96. Davies RJ, Pierce AC, Forster C, Grey R, Xu J, Arnost M, Choquette D, Galullo V, Tian SK, Henkel G, Chen G, Heidary DK, Ma J, Stuver-Moody C, Namchuk M..  (2011)  Design, synthesis, and evaluation of a novel dual FMS-like tyrosine kinase 3/stem cell factor receptor (FLT3/c-KIT) inhibitor for the treatment of acute myelogenous leukemia..  J Med Chem,  54  (20): (7184-7192).  [PMID:21970471]
97. Taldone T, Gomes-DaGama EM, Zong H, Sen S, Alpaugh ML, Zatorska D, Alonso-Sabadell R, Guzman ML, Chiosis G..  (2011)  Synthesis of purine-scaffold fluorescent probes for heat shock protein 90 with use in flow cytometry and fluorescence microscopy..  Bioorg Med Chem Lett,  21  (18): (5347-5352).  [PMID:21802945]
98. Kim H, Kim M, Lee J, Yu H, Hah JM..  (2011)  Syntheses of phenylpyrazolodiazepin-7-ones as conformationally rigid analogs of aminopyrazole amide scaffold and their antiproliferative effects on cancer cells..  Bioorg Med Chem,  19  (22): (6760-6767).  [PMID:22014755]
99. Poulsen A, Blanchard S, Soh CK, Lee C, Williams M, Wang H, Dymock B..  (2012)  Structure-based design of PDK1 inhibitors..  Bioorg Med Chem Lett,  22  (1): (305-307).  [PMID:22119465]
100. Bijian K, Zhang Z, Xu B, Jie S, Chen B, Wan S, Wu J, Jiang T, Alaoui-Jamali MA..  (2012)  Synthesis and biological activity of novel organoselenium derivatives targeting multiple kinases and capable of inhibiting cancer progression to metastases..  Eur J Med Chem,  48  (143-152).  [PMID:22204902]
101. Heidary DK, Huang G, Boucher D, Ma J, Forster C, Grey R, Xu J, Arnost M, Choquette D, Chen G, Zhou JH, Yao YM, Ball ED, Namchuk M, Davies RJ, Henkel G..  (2012)  VX-322: a novel dual receptor tyrosine kinase inhibitor for the treatment of acute myelogenous leukemia..  J Med Chem,  55  (2): (725-734).  [PMID:22221201]
102. Liu J, Yang C, Simpson C, Deryckere D, Van Deusen A, Miley MJ, Kireev D, Norris-Drouin J, Sather S, Hunter D, Korboukh VK, Patel HS, Janzen WP, Machius M, Johnson GL, Earp HS, Graham DK, Frye SV, Wang X..  (2012)  Discovery of Novel Small Molecule Mer Kinase Inhibitors for the Treatment of Pediatric Acute Lymphoblastic Leukemia..  ACS Med Chem Lett,  (2): (129-134).  [PMID:22662287]
103. William AD, Lee AC, Poulsen A, Goh KC, Madan B, Hart S, Tan E, Wang H, Nagaraj H, Chen D, Lee CP, Sun ET, Jayaraman R, Pasha MK, Ethirajulu K, Wood JM, Dymock BW..  (2012)  Discovery of the macrocycle (9E)-15-(2-(pyrrolidin-1-yl)ethoxy)-7,12,25-trioxa-19,21,24-triaza-tetracyclo[18.3.1.1(2,5).1(14,18)]hexacosa-1(24),2,4,9,14(26),15,17,20,22-nonaene (SB1578), a potent inhibitor of janus kinase 2/fms-like tyrosine kinase-3 (JAK2/FLT3) for the treatment of rheumatoid arthritis..  J Med Chem,  55  (6): (2623-2640).  [PMID:22339472]
104. Li WW, Wang XY, Zheng RL, Yan HX, Cao ZX, Zhong L, Wang ZR, Ji P, Yang LL, Wang LJ, Xu Y, Liu JJ, Yang J, Zhang CH, Ma S, Feng S, Sun QZ, Wei YQ, Yang SY..  (2012)  Discovery of the novel potent and selective FLT3 inhibitor 1-{5-[7-(3- morpholinopropoxy)quinazolin-4-ylthio]-[1,3,4]thiadiazol-2-yl}-3-p-tolylurea and its anti-acute myeloid leukemia (AML) activities in vitro and in vivo..  J Med Chem,  55  (8): (3852-3866).  [PMID:22452518]
105. 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]
106. Nakano H, Saito N, Parker L, Tada Y, Abe M, Tsuganezawa K, Yokoyama S, Tanaka A, Kojima H, Okabe T, Nagano T..  (2012)  Rational evolution of a novel type of potent and selective proviral integration site in Moloney murine leukemia virus kinase 1 (PIM1) inhibitor from a screening-hit compound..  J Med Chem,  55  (11): (5151-5164).  [PMID:22540945]
107. Leahy JW, Buhr CA, Johnson HW, Kim BG, Baik T, Cannoy J, Forsyth TP, Jeong JW, Lee MS, Ma S, Noson K, Wang L, Williams M, Nuss JM, Brooks E, Foster P, Goon L, Heald N, Holst C, Jaeger C, Lam S, Lougheed J, Nguyen L, Plonowski A, Song J, Stout T, Wu X, Yakes MF, Yu P, Zhang W, Lamb P, Raeber O..  (2012)  Discovery of a novel series of potent and orally bioavailable phosphoinositide 3-kinase γ inhibitors..  J Med Chem,  55  (11): (5467-5482).  [PMID:22548342]
108. Lawrence HR, Martin MP, Luo Y, Pireddu R, Yang H, Gevariya H, Ozcan S, Zhu JY, Kendig R, Rodriguez M, Elias R, Cheng JQ, Sebti SM, Schonbrunn E, Lawrence NJ..  (2012)  Development of o-chlorophenyl substituted pyrimidines as exceptionally potent aurora kinase inhibitors..  J Med Chem,  55  (17): (7392-7416).  [PMID:22803810]
109. Bavetsias V, Crumpler S, Sun C, Avery S, Atrash B, Faisal A, Moore AS, Kosmopoulou M, Brown N, Sheldrake PW, Bush K, Henley A, Box G, Valenti M, de Haven Brandon A, Raynaud FI, Workman P, Eccles SA, Bayliss R, Linardopoulos S, Blagg J..  (2012)  Optimization of imidazo[4,5-b]pyridine-based kinase inhibitors: identification of a dual FLT3/Aurora kinase inhibitor as an orally bioavailable preclinical development candidate for the treatment of acute myeloid leukemia..  J Med Chem,  55  (20): (8721-8734).  [PMID:23043539]
110. Amombo GM, Kramer T, Lo Monte F, Göring S, Fach M, Smith S, Kolb S, Schubenel R, Baumann K, Schmidt B..  (2012)  Modification of a promiscuous inhibitor shifts the inhibition from γ-secretase to FLT-3..  Bioorg Med Chem Lett,  22  (24): (7634-7640).  [PMID:23107479]
111. Duveau DY, Hu X, Walsh MJ, Shukla S, Skoumbourdis AP, Boxer MB, Ambudkar SV, Shen M, Thomas CJ..  (2013)  Synthesis and biological evaluation of analogues of the kinase inhibitor nilotinib as Abl and Kit inhibitors..  Bioorg Med Chem Lett,  23  (3): (682-686).  [PMID:23273517]
112. 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]
113. Yang LL, Li GB, Ma S, Zou C, Zhou S, Sun QZ, Cheng C, Chen X, Wang LJ, Feng S, Li LL, Yang SY..  (2013)  Structure-activity relationship studies of pyrazolo[3,4-d]pyrimidine derivatives leading to the discovery of a novel multikinase inhibitor that potently inhibits FLT3 and VEGFR2 and evaluation of its activity against acute myeloid leukemia in vitro and in vivo..  J Med Chem,  56  (4): (1641-1655).  [PMID:23362959]
114. Chin YW, Kong JY, Han SY..  (2013)  Flavonoids as receptor tyrosine kinase FLT3 inhibitors..  Bioorg Med Chem Lett,  23  (6): (1768-1770).  [PMID:23411073]
115. Brown A, Shi Q, Moore TW, Yoon Y, Prussia A, Maddox C, Liotta DC, Shim H, Snyder JP..  (2013)  Monocarbonyl curcumin analogues: heterocyclic pleiotropic kinase inhibitors that mediate anticancer properties..  J Med Chem,  56  (9): (3456-3466).  [PMID:23550937]
116. 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]
117. 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]
118. Kusakabe K, Ide N, Daigo Y, Tachibana Y, Itoh T, Yamamoto T, Hashizume H, Hato Y, Higashino K, Okano Y, Sato Y, Inoue M, Iguchi M, Kanazawa T, Ishioka Y, Dohi K, Kido Y, Sakamoto S, Yasuo K, Maeda M, Higaki M, Ueda K, Yoshizawa H, Baba Y, Shiota T, Murai H, Nakamura Y..  (2013)  Indazole-based potent and cell-active Mps1 kinase inhibitors: rational design from pan-kinase inhibitor anthrapyrazolone (SP600125)..  J Med Chem,  56  (11): (4343-4356).  [PMID:23634759]
119. Lin WH, Hsu JT, Hsieh SY, Chen CT, Song JS, Yen SC, Hsu T, Lu CT, Chen CH, Chou LH, Yang YN, Chiu CH, Chen CP, Tseng YJ, Yen KJ, Yeh CF, Chao YS, Yeh TK, Jiaang WT..  (2013)  Discovery of 3-phenyl-1H-5-pyrazolylamine derivatives containing a urea pharmacophore as potent and efficacious inhibitors of FMS-like tyrosine kinase-3 (FLT3)..  Bioorg Med Chem,  21  (11): (2856-2867).  [PMID:23618709]
120. Shiao HY, Coumar MS, Chang CW, Ke YY, Chi YH, Chu CY, Sun HY, Chen CH, Lin WH, Fung KS, Kuo PC, Huang CT, Chang KY, Lu CT, Hsu JT, Chen CT, Jiaang WT, Chao YS, Hsieh HP..  (2013)  Optimization of ligand and lipophilic efficiency to identify an in vivo active furano-pyrimidine Aurora kinase inhibitor..  J Med Chem,  56  (13): (5247-5260).  [PMID:23808327]
121. 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]
122. Taldone T, Kang Y, Patel HJ, Patel MR, Patel PD, Rodina A, Patel Y, Gozman A, Maharaj R, Clement CC, Lu A, Young JC, Chiosis G..  (2014)  Heat shock protein 70 inhibitors. 2. 2,5'-thiodipyrimidines, 5-(phenylthio)pyrimidines, 2-(pyridin-3-ylthio)pyrimidines, and 3-(phenylthio)pyridines as reversible binders to an allosteric site on heat shock protein 70..  J Med Chem,  57  (4): (1208-1224).  [PMID:24548239]
123. Szokol B, Gyulavári P, Kurkó I, Baska F, Szántai-Kis C, Greff Z, Orfi Z, Peták I, Pénzes K, Torka R, Ullrich A, Orfi L, Vántus T, Kéri G..  (2014)  Discovery and Biological Evaluation of Novel Dual EGFR/c-Met Inhibitors..  ACS Med Chem Lett,  (4): (298-303).  [PMID:24900830]
124. 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]
125. Park CH, Lee C, Yang JS, Joe BY, Chun K, Kim H, Kim HY, Kang JS, Lee JI, Kim MH, Han G..  (2014)  Discovery of thienopyrimidine-based FLT3 inhibitors from the structural modification of known IKKβ inhibitors..  Bioorg Med Chem Lett,  24  (12): (2655-2660).  [PMID:24813730]
126. 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]
127. Menet CJ, Fletcher SR, Van Lommen G, Geney R, Blanc J, Smits K, Jouannigot N, Deprez P, van der Aar EM, Clement-Lacroix P, Lepescheux L, Galien R, Vayssiere B, Nelles L, Christophe T, Brys R, Uhring M, Ciesielski F, Van Rompaey L..  (2014)  Triazolopyridines as selective JAK1 inhibitors: from hit identification to GLPG0634..  J Med Chem,  57  (22): (9323-9342).  [PMID:25369270]
128. Xu J, Ong EH, Hill J, Chen A, Chai CL..  (2014)  Design, synthesis and biological evaluation of FLT3 covalent inhibitors with a resorcylic acid core..  Bioorg Med Chem,  22  (23): (6625-6637).  [PMID:25456387]
129. Xu Y, Brenning BG, Kultgen SG, Foulks JM, Clifford A, Lai S, Chan A, Merx S, McCullar MV, Kanner SB, Ho KK..  (2015)  Synthesis and Biological Evaluation of Pyrazolo[1,5-a]pyrimidine Compounds as Potent and Selective Pim-1 Inhibitors..  ACS Med Chem Lett,  (1): (63-67).  [PMID:25589932]
130. Park BS, Al-Sanea MM, Abdelazem AZ, Park HM, Roh EJ, Park HM, Yoo KH, Sim T, Tae JS, Lee SH..  (2014)  Structure-based optimization and biological evaluation of trisubstituted pyrazole as a core structure of potent ROS1 kinase inhibitors..  Bioorg Med Chem,  22  (15): (3871-3878).  [PMID:24997577]
131. Zhang W, DeRyckere D, Hunter D, Liu J, Stashko MA, Minson KA, Cummings CT, Lee M, Glaros TG, Newton DL, Sather S, Zhang D, Kireev D, Janzen WP, Earp HS, Graham DK, Frye SV, Wang X..  (2014)  UNC2025, a potent and orally bioavailable MER/FLT3 dual inhibitor..  J Med Chem,  57  (16): (7031-7041).  [PMID:25068800]
132. Yang JS, Park CH, Lee C, Kim H, Oh C, Choi Y, Kang JS, Yun J, Jeong JH, Kim MH, Han G..  (2014)  Synthesis and biological evaluation of novel thieno[2,3-d]pyrimidine-based FLT3 inhibitors as anti-leukemic agents..  Eur J Med Chem,  85  (399-407).  [PMID:25108079]
133. Frett B, McConnell N, Smith CC, Wang Y, Shah NP, Li HY..  (2015)  Computer aided drug discovery of highly ligand efficient, low molecular weight imidazopyridine analogs as FLT3 inhibitors..  Eur J Med Chem,  94  (123-131).  [PMID:25765758]
134. Kovackova S, Chang L, Bekerman E, Neveu G, Barouch-Bentov R, Chaikuad A, Heroven C, Šála M, De Jonghe S, Knapp S, Einav S, Herdewijn P..  (2015)  Selective Inhibitors of Cyclin G Associated Kinase (GAK) as Anti-Hepatitis C Agents..  J Med Chem,  58  (8): (3393-3410).  [PMID:25822739]
135. Xu Y, Wang NY, Song XJ, Lei Q, Ye TH, You XY, Zuo WQ, Xia Y, Zhang LD, Yu LT..  (2015)  Discovery of novel N-(5-(tert-butyl)isoxazol-3-yl)-N'-phenylurea analogs as potent FLT3 inhibitors and evaluation of their activity against acute myeloid leukemia in vitro and in vivo..  Bioorg Med Chem,  23  (15): (4333-4343).  [PMID:26142317]
136. 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]
137. Lin XD, Yang HW, Ma S, Li WW, Zhang CH, Wang WJ, Xiang R, Li LL, Yang SY..  (2015)  Discovery of 6-phenylimidazo[2,1-b]thiazole derivatives as a new type of FLT3 inhibitors..  Bioorg Med Chem Lett,  25  (20): (4534-4538).  [PMID:26342867]
138. 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]
139. Li X, Wang A, Yu K, Qi Z, Chen C, Wang W, Hu C, Wu H, Wu J, Zhao Z, Liu J, Zou F, Wang L, Wang B, Wang W, Zhang S, Liu J, Liu Q..  (2015)  Discovery of (R)-1-(3-(4-Amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)-2-(dimethylamino)ethanone (CHMFL-FLT3-122) as a Potent and Orally Available FLT3 Kinase Inhibitor for FLT3-ITD Positive Acute Myeloid Leukemia..  J Med Chem,  58  (24): (9625-9638).  [PMID:26630553]
140. Simon-Szabó L, Kokas M, Greff Z, Boros S, Bánhegyi P, Zsákai L, Szántai-Kis C, Vantus T, Mandl J, Bánhegyi G, Vályi-Nagy I, Őrfi L, Ullrich A, Csala M, Kéri G..  (2016)  Novel compounds reducing IRS-1 serine phosphorylation for treatment of diabetes..  Bioorg Med Chem Lett,  26  (2): (424-428).  [PMID:26704265]
141. Simov V, Deshmukh SV, Dinsmore CJ, Elwood F, Fernandez RB, Garcia Y, Gibeau C, Gunaydin H, Jung J, Katz JD, Kraybill B, Lapointe B, Patel SB, Siu T, Su H, Young JR..  (2016)  Structure-based design and development of (benz)imidazole pyridones as JAK1-selective kinase inhibitors..  Bioorg Med Chem Lett,  26  (7): (1803-1808).  [PMID:26927423]
142. Song D, Lee M, Park CH, Ahn S, Yun CS, Lee CO, Kim HR, Hwang JY..  (2016)  Novel 2,4-diaminopyrimidines bearing tetrahydronaphthalenyl moiety against anaplastic lymphoma kinase (ALK): Synthesis, in vitro, ex vivo, and in vivo efficacy studies..  Bioorg Med Chem Lett,  26  (7): (1720-1725).  [PMID:26923695]
143. Getlik M, Smil D, Zepeda-Velázquez C, Bolshan Y, Poda G, Wu H, Dong A, Kuznetsova E, Marcellus R, Senisterra G, Dombrovski L, Hajian T, Kiyota T, Schapira M, Arrowsmith CH, Brown PJ, Vedadi M, Al-Awar R..  (2016)  Structure-Based Optimization of a Small Molecule Antagonist of the Interaction Between WD Repeat-Containing Protein 5 (WDR5) and Mixed-Lineage Leukemia 1 (MLL1)..  J Med Chem,  59  (6): (2478-2496).  [PMID:26958703]
144. Han W, Ding Y, Xu Y, Pfister K, Zhu S, Warne B, Doyle M, Aikawa M, Amiri P, Appleton B, Stuart DD, Fanidi A, Shafer CM..  (2016)  Discovery of a Selective and Potent Inhibitor of Mitogen-Activated Protein Kinase-Interacting Kinases 1 and 2 (MNK1/2) Utilizing Structure-Based Drug Design..  J Med Chem,  59  (7): (3034-3045).  [PMID:27002243]
145. 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]
146. Hatcher JM, Weisberg E, Sim T, Stone RM, Liu S, Griffin JD, Gray NS..  (2016)  Discovery of a Highly Potent and Selective Indenoindolone Type 1 Pan-FLT3 Inhibitor..  ACS Med Chem Lett,  (5): (476-481).  [PMID:27190596]
147. Rudolph J, Murray LJ, Ndubaku CO, O'Brien T, Blackwood E, Wang W, Aliagas I, Gazzard L, Crawford JJ, Drobnick J, Lee W, Zhao X, Hoeflich KP, Favor DA, Dong P, Zhang H, Heise CE, Oh A, Ong CC, La H, Chakravarty P, Chan C, Jakubiak D, Epler J, Ramaswamy S, Vega R, Cain G, Diaz D, Zhong Y..  (2016)  Chemically Diverse Group I p21-Activated Kinase (PAK) Inhibitors Impart Acute Cardiovascular Toxicity with a Narrow Therapeutic Window..  J Med Chem,  59  (11): (5520-5541).  [PMID:27167326]
148. Glatthar R, Stojanovic A, Troxler T, Mattes H, Möbitz H, Beerli R, Blanz J, Gassmann E, Drückes P, Fendrich G, Gutmann S, Martiny-Baron G, Spence F, Hornfeld J, Peel JE, Sparrer H..  (2016)  Discovery of Imidazoquinolines as a Novel Class of Potent, Selective, and in Vivo Efficacious Cancer Osaka Thyroid (COT) Kinase Inhibitors..  J Med Chem,  59  (16): (7544-7560).  [PMID:27502541]
149. 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]
150. Wurz RP, Sastri C, D'Amico DC, Herberich B, Jackson CLM, Pettus LH, Tasker AS, Wu B, Guerrero N, Lipford JR, Winston JT, Yang Y, Wang P, Nguyen Y, Andrews KL, Huang X, Lee MR, Mohr C, Zhang JD, Reid DL, Xu Y, Zhou Y, Wang HL..  (2016)  Discovery of imidazopyridazines as potent Pim-1/2 kinase inhibitors..  Bioorg Med Chem Lett,  26  (22): (5580-5590).  [PMID:27769621]
151. Musumeci F, Fallacara AL, Brullo C, Grossi G, Botta L, Calandro P, Chiariello M, Kissova M, Crespan E, Maga G, Schenone S..  (2017)  Identification of new pyrrolo[2,3-d]pyrimidines as Src tyrosine kinase inhibitors in vitro active against Glioblastoma..  Eur J Med Chem,  127  (369-378).  [PMID:28076826]
152. Ma X, Zhou J, Wang C, Carter-Cooper B, Yang F, Larocque E, Fine J, Tsuji G, Chopra G, Lapidus RG, Sintim HO..  (2017)  Identification of New FLT3 Inhibitors That Potently Inhibit AML Cell Lines via an Azo Click-It/Staple-It Approach..  ACS Med Chem Lett,  (5): (492-497).  [PMID:28523099]
153. Tassini S, Sun L, Lanko K, Crespan E, Langron E, Falchi F, Kissova M, Armijos-Rivera JI, Delang L, Mirabelli C, Neyts J, Pieroni M, Cavalli A, Costantino G, Maga G, Vergani P, Leyssen P, Radi M..  (2017)  Discovery of Multitarget Agents Active as Broad-Spectrum Antivirals and Correctors of Cystic Fibrosis Transmembrane Conductance Regulator for Associated Pulmonary Diseases..  J Med Chem,  60  (4): (1400-1416).  [PMID:28122178]
154. Oh C, Kim H, Kang JS, Yun J, Sim J, Kim HM, Han G..  (2017)  Synthetic strategy for increasing solubility of potential FLT3 inhibitor thieno[2,3-d]pyrimidine derivatives through structural modifications at the C2 and C6 positions..  Bioorg Med Chem Lett,  27  (3): (496-500).  [PMID:28043794]
155. Shi Y, Park J, Lagisetti C, Zhou W, Sambucetti LC, Webb TR..  (2017)  A triple exon-skipping luciferase reporter assay identifies a new CLK inhibitor pharmacophore..  Bioorg Med Chem Lett,  27  (3): (406-412).  [PMID:28049589]
156. Ma F, Liu P, Lei M, Liu J, Wang H, Zhao S, Hu L..  (2017)  Design, synthesis and biological evaluation of indolin-2-one-based derivatives as potent, selective and efficacious inhibitors of FMS-like tyrosine kinase3 (FLT3)..  Eur J Med Chem,  127  (72-86).  [PMID:28038328]
157. Lu Y, Mao F, Li X, Zheng X, Wang M, Xu Q, Zhu J, Li J..  (2017)  Discovery of Potent, Selective Stem Cell Factor Receptor/Platelet Derived Growth Factor Receptor Alpha (c-KIT/PDGFRα) Dual Inhibitor for the Treatment of Imatinib-Resistant Gastrointestinal Stromal Tumors (GISTs)..  J Med Chem,  60  (12): (5099-5119).  [PMID:28541695]
158. Charvin D, Pomel V, Ortiz M, Frauli M, Scheffler S, Steinberg E, Baron L, Deshons L, Rudigier R, Thiarc D, Morice C, Manteau B, Mayer S, Graham D, Giethlen B, Brugger N, Hédou G, Conquet F, Schann S..  (2017)  Discovery, Structure-Activity Relationship, and Antiparkinsonian Effect of a Potent and Brain-Penetrant Chemical Series of Positive Allosteric Modulators of Metabotropic Glutamate Receptor 4..  J Med Chem,  60  (20): (8515-8537).  [PMID:28902994]
159. 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]
160. Patel HM, Pawara R, Ansari A, Noolvi M, Surana S..  (2017)  Design and synthesis of quinazolinones as EGFR inhibitors to overcome EGFR resistance obstacle..  Bioorg Med Chem,  25  (10): (2713-2723).  [PMID:28366268]
161. Mah S, Park JH, Jung HY, Ahn K, Choi S, Tae HS, Jung KH, Rho JK, Lee JC, Hong SS, Hong S..  (2017)  Identification of 4-Phenoxyquinoline Based Inhibitors for L1196M Mutant of Anaplastic Lymphoma Kinase by Structure-Based Design..  J Med Chem,  60  (22): (9205-9221).  [PMID:29091425]
162. Zhang Y, Chen Y, Zhang D, Wang L, Lu T, Jiao Y..  (2018)  Discovery of Novel Potent VEGFR-2 Inhibitors Exerting Significant Antiproliferative Activity against Cancer Cell Lines..  J Med Chem,  61  (1): (140-157).  [PMID:29189002]
163. Bhide RS, Keon A, Weigelt C, Sack JS, Schmidt RJ, Lin S, Xiao HY, Spergel SH, Kempson J, Pitts WJ, Carman J, Poss MA..  (2017)  Discovery and structure-based design of 4,6-diaminonicotinamides as potent and selective IRAK4 inhibitors..  Bioorg Med Chem Lett,  27  (21): (4908-4913).  [PMID:28947151]
164. Wang X, Kolesnikov A, Tay S, Chan G, Chao Q, Do S, Drummond J, Ebens AJ, Liu N, Ly J, Harstad E, Hu H, Moffat J, Munugalavadla V, Murray J, Slaga D, Tsui V, Volgraf M, Wallweber H, Chang JH..  (2017)  Discovery of 5-Azaindazole (GNE-955) as a Potent Pan-Pim Inhibitor with Optimized Bioavailability..  J Med Chem,  60  (10): (4458-4473).  [PMID:28445037]
165. 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]
166. Wang Y, Zhi Y, Jin Q, Lu S, Lin G, Yuan H, Yang T, Wang Z, Yao C, Ling J, Guo H, Li T, Jin J, Li B, Zhang L, Chen Y, Lu T..  (2018)  Discovery of 4-((7H-Pyrrolo[2,3-d]pyrimidin-4-yl)amino)-N-(4-((4-methylpiperazin-1-yl)methyl)phenyl)-1H-pyrazole-3-carboxamide (FN-1501), an FLT3- and CDK-Kinase Inhibitor with Potentially High Efficiency against Acute Myelocytic Leukemia..  J Med Chem,  61  (4): (1499-1518).  [PMID:29357250]
167. 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]
168. 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]
169. Pu SY, Wouters R, Schor S, Rozenski J, Barouch-Bentov R, Prugar LI, O'Brien CM, Brannan JM, Dye JM, Herdewijn P, De Jonghe S, Einav S..  (2018)  Optimization of Isothiazolo[4,3- b]pyridine-Based Inhibitors of Cyclin G Associated Kinase (GAK) with Broad-Spectrum Antiviral Activity..  J Med Chem,  61  (14): (6178-6192).  [PMID:29953812]
170. Malki WH, Gouda AM, Ali HEA, Al-Rousan R, Samaha D, Abdalla AN, Bustamante J, Abd Elmageed ZY, Ali HI..  (2018)  Structural-based design, synthesis, and antitumor activity of novel alloxazine analogues with potential selective kinase inhibition..  Eur J Med Chem,  152  (31-52).  [PMID:29684708]
171. Zhi Y, Li B, Yao C, Li H, Chen P, Bao J, Qin T, Wang Y, Lu T, Lu S..  (2018)  Discovery of the selective and efficacious inhibitors of FLT3 mutations..  Eur J Med Chem,  155  (303-315).  [PMID:29894944]
172. 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]
173. Monastyrskyi A, Nilchan N, Quereda V, Noguchi Y, Ruiz C, Grant W, Cameron M, Duckett D, Roush W..  (2018)  Development of dual casein kinase 1δ/1ε (CK1δ/ε) inhibitors for treatment of breast cancer..  Bioorg Med Chem,  26  (3): (590-602).  [PMID:29289448]
174. Myers SH, Temps C, Houston DR, Brunton VG, Unciti-Broceta A..  (2018)  Development of Potent Inhibitors of Receptor Tyrosine Kinases by Ligand-Based Drug Design and Target-Biased Phenotypic Screening..  J Med Chem,  61  (5): (2104-2110).  [PMID:29466002]
175. Salado IG, Zaldivar-Diez J, Sebastián-Pérez V, Li L, Geiger L, González S, Campillo NE, Gil C, Morales AV, Perez DI, Martinez A..  (2017)  Leucine rich repeat kinase 2 (LRRK2) inhibitors based on indolinone scaffold: Potential pro-neurogenic agents..  Eur J Med Chem,  138  (328-342).  [PMID:28688273]
176. Nemes Z, Takács-Novák K, Völgyi G, Valko K, Béni S, Horváth Z, Szokol B, Breza N, Dobos J, Szántai-Kis C, Illyés E, Boros S, Kok RJ, Őrfi L..  (2018)  Synthesis and characterization of amino acid substituted sunitinib analogues for the treatment of AML..  Bioorg Med Chem Lett,  28  (14): (2391-2398).  [PMID:29935772]
177. Philip S, Kumarasiri M, Teo T, Yu M, Wang S..  (2018)  Cyclin-Dependent Kinase 8: A New Hope in Targeted Cancer Therapy?.  J Med Chem,  61  (12): (5073-5092).  [PMID:29266937]
178. Zhang Y, Lv H, Luo L, Xu Y, Pan Y, Wang Y, Lin H, Xiong J, Guo P, Zhang J, Li X, Ye F..  (2018)  Design, synthesis and pharmacological evaluation of N4,N6-disubstituted pyrimidine-4,6-diamine derivatives as potent EGFR inhibitors in non-small cell lung cancer..  Eur J Med Chem,  157  (1300-1325).  [PMID:30195240]
179. Baska F, Sipos A, Őrfi Z, Nemes Z, Dobos J, Szántai-Kis C, Szabó E, Szénási G, Dézsi L, Hamar P, Cserepes MT, Tóvári J, Garamvölgyi R, Krekó M, Őrfi L..  (2019)  Discovery and development of extreme selective inhibitors of the ITD and D835Y mutant FLT3 kinases..  Eur J Med Chem,  184  (111710-111710).  [PMID:31614258]
180. Martínez-González S, Rodríguez-Arístegui S, Gómez de la Oliva CA, Hernández AI, González Cantalapiedra E, Varela C, García AB, Rabal O, Oyarzabal J, Bischoff JR, Klett J, Albarrán MI, Cebriá A, Ajenjo N, García-Serelde B, Gómez-Casero E, Cuadrado-Urbano M, Cebrián D, Blanco-Aparicio C, Pastor J..  (2019)  Discovery of novel triazolo[4,3-b]pyridazin-3-yl-quinoline derivatives as PIM inhibitors..  Eur J Med Chem,  168  (87-109).  [PMID:30802730]
181. 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]
182. 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]
183. 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]
184. Xu Q, Dai B, Li Z, Xu L, Yang D, Gong P, Hou Y, Liu Y..  (2019)  Design, synthesis, and biological evaluation of 4-((6,7-dimethoxyquinoline-4-yl)oxy)aniline derivatives as FLT3 inhibitors for the treatment of acute myeloid leukemia..  Bioorg Med Chem Lett,  29  (19): (126630-126630).  [PMID:31466809]
185. Yuan T, Qi B, Jiang Z, Dong W, Zhong L, Bai L, Tong R, Yu J, Shi J..  (2019)  Dual FLT3 inhibitors: Against the drug resistance of acute myeloid leukemia in recent decade..  Eur J Med Chem,  178  (468-483).  [PMID:31207462]
186. Lin WH, Wu SY, Yeh TK, Chen CT, Song JS, Shiao HY, Kuo CC, Hsu T, Lu CT, Wang PC, Wu TS, Peng YH, Lin HY, Chen CP, Weng YL, Kung FC, Wu MH, Su YC, Huang KW, Chou LH, Hsueh CC, Yen KJ, Kuo PC, Huang CL, Chen LT, Shih C, Tsai HJ, Jiaang WT..  (2019)  Identification of a Multitargeted Tyrosine Kinase Inhibitor for the Treatment of Gastrointestinal Stromal Tumors and Acute Myeloid Leukemia..  J Med Chem,  62  (24): (11135-11150).  [PMID:31721578]
187. Yuan X, Chen Y, Zhang W, He J, Lei L, Tang M, Liu J, Li M, Dou C, Yang T, Yang L, Yang S, Wei Y, Peng A, Niu T, Xiang M, Ye H, Chen L..  (2019)  Identification of Pyrrolo[2,3- d]pyrimidine-Based Derivatives as Potent and Orally Effective Fms-like Tyrosine Receptor Kinase 3 (FLT3) Inhibitors for Treating Acute Myelogenous Leukemia..  J Med Chem,  62  (8): (4158-4173).  [PMID:30939008]
188. Tong L, Song P, Jiang K, Xu L, Jin T, Wang P, Hu X, Fang S, Gao A, Zhou Y, Liu T, Li J, Hu Y..  (2019)  Discovery of (R)-5-((5-(1-methyl-1H-pyrazol-4-yl)-4-(methylamino)pyrimidin-2-yl)amino)-3-(piperidin-3-yloxy)picolinonitrile, a novel CHK1 inhibitor for hematologic malignancies..  Eur J Med Chem,  173  (44-62).  [PMID:30986571]
189. Collier PN, Twin HC, Knegtel RMA, Boyall D, Brenchley G, Davis CJ, Keily S, Mak C, Miller A, Pierard F, Settimo L, Bolton CM, Chiu P, Curnock A, Doyle E, Tanner AJ, Jimenez JM..  (2019)  Discovery of Selective, Orally Bioavailable Pyrazolopyridine Inhibitors of Protein Kinase Cθ (PKCθ) That Ameliorate Symptoms of Experimental Autoimmune Encephalomyelitis..  ACS Med Chem Lett,  10  (8): (1134-1139).  [PMID:31417666]
190. Bensinger D, Stubba D, Cremer A, Kohl V, Waßmer T, Stuckert J, Engemann V, Stegmaier K, Schmitz K, Schmidt B..  (2019)  Virtual Screening Identifies Irreversible FMS-like Tyrosine Kinase 3 Inhibitors with Activity toward Resistance-Conferring Mutations..  J Med Chem,  62  (5): (2428-2446).  [PMID:30742435]
191. 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]
192. Wang Q, Dai Y, Ji Y, Shi H, Guo Z, Chen D, Chen Y, Peng X, Gao Y, Wang X, Chen L, Jiang Y, Geng M, Shen J, Ai J, Xiong B..  (2019)  Discovery and optimization of a series of 3-substituted indazole derivatives as multi-target kinase inhibitors for the treatment of lung squamous cell carcinoma..  Eur J Med Chem,  163  (671-689).  [PMID:30572178]
193. Grimm SH, Gagestein B, Keijzer JF, Liu N, Wijdeven RH, Lenselink EB, Tuin AW, van den Nieuwendijk AMCH, van Westen GJP, van Boeckel CAA, Overkleeft HS, Neefjes J, van der Stelt M..  (2019)  Comprehensive structure-activity-relationship of azaindoles as highly potent FLT3 inhibitors..  Bioorg Med Chem,  27  (5): (692-699).  [PMID:30661740]
194. Ikegashira K, Ikenogami T, Yamasaki T, Oka T, Hase Y, Miyagawa N, Inagaki K, Kawahara I, Koga Y, Hashimoto H..  (2019)  Optimization of an azetidine series as inhibitors of colony stimulating factor-1 receptor (CSF-1R) Type II to lead to the clinical candidate JTE-952..  Bioorg Med Chem Lett,  29  (7): (873-877).  [PMID:30755337]
195. Li GB, Ma S, Yang LL, Ji S, Fang Z, Zhang G, Wang LJ, Zhong JM, Xiong Y, Wang JH, Huang SZ, Li LL, Xiang R, Niu D, Chen YC, Yang SY..  (2016)  Drug Discovery against Psoriasis: Identification of a New Potent FMS-like Tyrosine Kinase 3 (FLT3) Inhibitor, 1-(4-((1H-Pyrazolo[3,4-d]pyrimidin-4-yl)oxy)-3-fluorophenyl)-3-(5-(tert-butyl)isoxazol-3-yl)urea, That Showed Potent Activity in a Psoriatic Animal Model..  J Med Chem,  59  (18): (8293-8305).  [PMID:27535613]
196. Sun D, Yang Y, Lyu J, Zhou W, Song W, Zhao Z, Chen Z, Xu Y, Li H..  (2016)  Discovery and Rational Design of Pteridin-7(8H)-one-Based Inhibitors Targeting FMS-like Tyrosine Kinase 3 (FLT3) and Its Mutants..  J Med Chem,  59  (13): (6187-6200).  [PMID:27266526]
197. Mathison CJN, Chianelli D, Rucker PV, Nelson J, Roland J, Huang Z, Yang Y, Jiang J, Xie YF, Epple R, Bursulaya B, Lee C, Gao MY, Shaffer J, Briones S, Sarkisova Y, Galkin A, Li L, Li N, Li C, Hua S, Kasibhatla S, Kinyamu-Akunda J, Kikkawa R, Molteni V, Tellew JE..  (2020)  Efficacy and Tolerability of Pyrazolo[1,5-a]pyrimidine RET Kinase Inhibitors for the Treatment of Lung Adenocarcinoma..  ACS Med Chem Lett,  11  (4): (558-565).  [PMID:32292564]
198. Yuan X,Wu H,Bu H,Zheng P,Zhou J,Zhang H.  (2019)  Design, synthesis and biological evaluation of pyridone-aminal derivatives as MNK1/2 inhibitors..  Bioorg Med Chem,  27  (7.0): (1211-1225).  [PMID:30824167]
199. Zhang Q,Zhao K,Zhang L,Jiao X,Zhang Y,Tang C.  (2020)  Synthesis and biological evaluation of diaryl urea derivatives as FLT3 inhibitors..  Bioorg Med Chem Lett,  30  (23.0): (127525-127525).  [PMID:32898697]
200. Sun N,Ren C,Kong Y,Zhong H,Chen J,Li Y,Zhang J,Zhou Y,Qiu X,Lin H,Song X,Yang X,Jiang B.  (2020)  Development of a Brigatinib degrader (SIAIS117) as a potential treatment for ALK positive cancer resistance..  Eur J Med Chem,  193  (112190-112190).  [PMID:32179332]
201. Sellmer A,Pilsl B,Beyer M,Pongratz H,Wirth L,Elz S,Dove S,Henninger SJ,Spiekermann K,Polzer H,Klaeger S,Kuster B,Böhmer FD,Fiebig HH,Krämer OH,Mahboobi S.  (2020)  A series of novel aryl-methanone derivatives as inhibitors of FMS-like tyrosine kinase 3 (FLT3) in FLT3-ITD-positive acute myeloid leukemia..  Eur J Med Chem,  193  (112232-112232).  [PMID:32199135]
202. Nan X,Li HJ,Fang SB,Li QY,Wu YC.  (2020)  Structure-based discovery of novel 4-(2-fluorophenoxy)quinoline derivatives as c-Met inhibitors using isocyanide-involved multicomponent reactions..  Eur J Med Chem,  193  (112241-112241).  [PMID:32200199]
203. Malik HS,Bilal A,Ullah R,Iqbal M,Khan S,Ahmed I,Krohn K,Saleem RSZ,Hussain H,Faisal A.  (2020)  Natural and Semisynthetic Chalcones as Dual FLT3 and Microtubule Polymerization Inhibitors..  J Nat Prod,  83  (10): (3111-3121).  [PMID:32975953]
204. Yan G,Zhong X,Pu C,Yue L,Shan H,Lan S,Zhou M,Hou X,Yang J,Li D,Fan S,Li R.  (2021)  Targeting Cysteine Located Outside the Active Site: An Effective Strategy for Covalent ALKi Design..  J Med Chem,  64  (3.0): (1558-1569).  [PMID:33471528]
205. 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]
206. Chen Y,Bai G,Ning Y,Cai S,Zhang T,Song P,Zhou J,Duan W,Ding J,Xie H,Zhang H.  (2020)  Design and synthesis of Imidazo[1,2-b]pyridazine IRAK4 inhibitors for the treatment of mutant MYD88 L265P diffuse large B-cell lymphoma..  Eur J Med Chem,  190  (112092-112092).  [PMID:32014679]
207. 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]
208. Cao DS,Jiang SL,Guan YD,Chen XS,Zhang LX,Zhang Y,Chen AF,Yang JM,Cheng Y.  (2020)  A multi-scale systems pharmacology approach uncovers the anti-cancer molecular mechanism of Ixabepilone..  Eur J Med Chem,  199  (112421-112421).  [PMID:32428794]
209. Lakkaniga NR,Zhang L,Belachew B,Gunaganti N,Frett B,Li HY.  (2020)  Discovery of SP-96, the first non-ATP-competitive Aurora Kinase B inhibitor, for reduced myelosuppression..  Eur J Med Chem,  203  (112589-112589).  [PMID:32717530]
210. El-Damasy AK,Jin H,Seo SH,Bang EK,Keum G.  (2020)  Design, synthesis, and biological evaluations of novel 3-amino-4-ethynyl indazole derivatives as Bcr-Abl kinase inhibitors with potent cellular antileukemic activity..  Eur J Med Chem,  207  (112710-112710).  [PMID:32961435]
211. Yen SC, Chen LC, Huang HL, Ngo ST, Wu YW, Lin TE, Sung TY, Lien ST, Tseng HJ, Pan SL, Huang WJ, Hsu KC..  (2021)  Investigation of Selected Flavonoid Derivatives as Potent FLT3 Inhibitors for the Potential Treatment of Acute Myeloid Leukemia..  J Nat Prod,  84  (1.0): (1-10).  [PMID:33393294]
212. Krajčovičová S, Jorda R, Vanda D, Soural M, Kryštof V..  (2021)  1,4,6-Trisubstituted imidazo[4,5-c]pyridines as inhibitors of Bruton's tyrosine kinase..  Eur J Med Chem,  211  (113094-113094).  [PMID:33340912]
213. Rosnet, O O, Matteï, M G MG, Marchetto, S S and Birnbaum, D D..  (1991)  Isolation and chromosomal localization of a novel FMS-like tyrosine kinase gene..  Genomics,      [PMID:2004790]
214. Small, D D and 9 more authors..  (1994)  STK-1, the human homolog of Flk-2/Flt-3, is selectively expressed in CD34+ human bone marrow cells and is involved in the proliferation of early progenitor/stem cells..  Proceedings of the National Academy of Sciences of the United States of America,    (18):   [PMID:7507245]
215. Rosnet, O O and 7 more authors..  (1993)  Human FLT3/FLK2 gene: cDNA cloning and expression in hematopoietic cells..  Blood,    (15):   [PMID:8394751]
216. Nakao, M M and 8 more authors..  (1996)  Internal tandem duplication of the flt3 gene found in acute myeloid leukemia..  Leukemia,      [PMID:8946930]
217. Kiyoi, H H and 6 more authors..  (1998)  Internal tandem duplication of the FLT3 gene is a novel modality of elongation mutation which causes constitutive activation of the product..  Leukemia,      [PMID:9737679]
218. Zhang, S S, Mantel, C C and Broxmeyer, H E HE..  (1999)  Flt3 signaling involves tyrosyl-phosphorylation of SHP-2 and SHIP and their association with Grb2 and Shc in Baf3/Flt3 cells..  Journal of leukocyte biology,      [PMID:10080542]
219. Yamamoto, Y Y and 19 more authors..  (2001)  Activating mutation of D835 within the activation loop of FLT3 in human hematologic malignancies..  Blood,    (15):   [PMID:11290608]
220. Abu-Duhier, F M FM and 5 more authors..  (2001)  Identification of novel FLT-3 Asp835 mutations in adult acute myeloid leukaemia..  British journal of haematology,      [PMID:11442493]
221. O'Farrell, Anne-Marie AM and 14 more authors..  (2003)  SU11248 is a novel FLT3 tyrosine kinase inhibitor with potent activity in vitro and in vivo..  Blood,    (1):   [PMID:12531805]
222. Stirewalt, Derek L DL and Radich, Jerald P JP..  (2003)  The role of FLT3 in haematopoietic malignancies..  Nature reviews. Cancer,      [PMID:12951584]
223. Taketani, Takeshi T and 9 more authors..  (2004)  FLT3 mutations in the activation loop of tyrosine kinase domain are frequently found in infant ALL with MLL rearrangements and pediatric ALL with hyperdiploidy..  Blood,    (1):   [PMID:14504097]
224. O'Farrell, Anne-Marie AM and 17 more authors..  (2003)  An innovative phase I clinical study demonstrates inhibition of FLT3 phosphorylation by SU11248 in acute myeloid leukemia patients..  Clinical cancer research : an official journal of the American Association for Cancer Research,    (15):   [PMID:14654525]
225. Dunham, A A and 125 more authors..  (2004)  The DNA sequence and analysis of human chromosome 13..  Nature,    (1):   [PMID:15057823]
226. Schmidt-Arras, Dirk D, Schwäble, Joachim J, Böhmer, Frank-D FD and Serve, Hubert H..  (2004)  Flt3 receptor tyrosine kinase as a drug target in leukemia..  Current pharmaceutical design,      [PMID:15180525]
227. Yee, Kevin W H KW and 7 more authors..  (2004)  Synergistic effect of SU11248 with cytarabine or daunorubicin on FLT3 ITD-positive leukemic cells..  Blood,    (15):   [PMID:15304385]
228. Schmidt-Arras, Dirk-E DE and 5 more authors..  (2005)  Tyrosine phosphorylation regulates maturation of receptor tyrosine kinases..  Molecular and cellular biology,      [PMID:15831474]
229. Brandts, Christian H CH and 11 more authors..  (2005)  Constitutive activation of Akt by Flt3 internal tandem duplications is necessary for increased survival, proliferation, and myeloid transformation..  Cancer research,    (1):   [PMID:16266983]
230. Rocnik, Jennifer L JL and 6 more authors..  (2006)  Roles of tyrosine 589 and 591 in STAT5 activation and transformation mediated by FLT3-ITD..  Blood,    (15):   [PMID:16627759]
231. Heiss, Elke E and 6 more authors..  (2006)  Identification of Y589 and Y599 in the juxtamembrane domain of Flt3 as ligand-induced autophosphorylation sites involved in binding of Src family kinases and the protein tyrosine phosphatase SHP2..  Blood,    (1):   [PMID:16684964]
232. Auclair, D D and 17 more authors..  (2007)  Antitumor activity of sorafenib in FLT3-driven leukemic cells..  Leukemia,      [PMID:17205056]
233. Lierman, Els E and 5 more authors..  (2007)  The ability of sorafenib to inhibit oncogenic PDGFRbeta and FLT3 mutants and overcome resistance to other small molecule inhibitors..  Haematologica,      [PMID:17229632]
234. Meshinchi, Soheil S and 8 more authors..  (2008)  Structural and numerical variation of FLT3/ITD in pediatric AML..  Blood,    (15):   [PMID:18305215]
235. Kikushige, Yoshikane Y and 11 more authors..  (2008)  Human Flt3 is expressed at the hematopoietic stem cell and the granulocyte/macrophage progenitor stages to maintain cell survival..  Journal of immunology (Baltimore, Md. : 1950),    (1):   [PMID:18490735]
236. Ley, Timothy J TJ and 47 more authors..  (2008)  DNA sequencing of a cytogenetically normal acute myeloid leukaemia genome..  Nature,    (6):   [PMID:18987736]
237. Razumovskaya, Elena E, Masson, Kristina K, Khan, Rasheed R, Bengtsson, Susanne S and Rönnstrand, Lars L..  (2009)  Oncogenic Flt3 receptors display different specificity and kinetics of autophosphorylation..  Experimental hematology,      [PMID:19477218]
238. Meshinchi, Soheil S and Appelbaum, Frederick R FR..  (2009)  Structural and functional alterations of FLT3 in acute myeloid leukemia..  Clinical cancer research : an official journal of the American Association for Cancer Research,    (1):   [PMID:19549778]
239. Voisset, E E and 7 more authors..  (2010)  FES kinases are required for oncogenic FLT3 signaling..  Leukemia,      [PMID:20111072]
240. Buchwald, M M and 5 more authors..  (2010)  Ubiquitin conjugase UBCH8 targets active FMS-like tyrosine kinase 3 for proteasomal degradation..  Leukemia,      [PMID:20508617]
241. Chen, Weina W and 10 more authors..  (2010)  mTOR signaling is activated by FLT3 kinase and promotes survival of FLT3-mutated acute myeloid leukemia cells..  Molecular cancer,    (10):   [PMID:21067588]
242. Arora, Deepika D and 11 more authors..  (2011)  Protein-tyrosine phosphatase DEP-1 controls receptor tyrosine kinase FLT3 signaling..  The Journal of biological chemistry,    (1):   [PMID:21262971]
243. Zheng, R R and 6 more authors..  (2011)  Further activation of FLT3 mutants by FLT3 ligand..  Oncogene,    (22):   [PMID:21516120]
244. Ceccon, Monica M, Mologni, Luca L, Bisson, William W, Scapozza, Leonardo L and Gambacorti-Passerini, Carlo C..  (2013)  Crizotinib-resistant NPM-ALK mutants confer differential sensitivity to unrelated Alk inhibitors..  Molecular cancer research : MCR,      [PMID:23239810]
245. Smith, Catherine C CC and 7 more authors..  (2013)  Activity of ponatinib against clinically-relevant AC220-resistant kinase domain mutants of FLT3-ITD..  Blood,    (18):   [PMID:23430109]
246. Motzer, Robert J RJ and 20 more authors..  (2013)  Tivozanib versus sorafenib as initial targeted therapy for patients with metastatic renal cell carcinoma: results from a phase III trial..  Journal of clinical oncology : official journal of the American Society of Clinical Oncology,    (20):   [PMID:24019545]
247. and Thom, Claire C..  (2015)  Preliminary data on ASP2215: tolerability and efficacy in acute myeloid leukemia patients..  Future oncology (London, England),      [PMID:26279055]
248. Gallogly, Molly Megan MM and Lazarus, Hillard M HM..  (2016)  Midostaurin: an emerging treatment for acute myeloid leukemia patients..  Journal of blood medicine,      [PMID:27186148]
249. Antar, A A and 7 more authors..  (2017)  Inhibition of FLT3 in AML: a focus on sorafenib..  Bone marrow transplantation,      [PMID:27775694]
250. Mori, Masamichi M and 8 more authors..  (2017)  Gilteritinib, a FLT3/AXL inhibitor, shows antileukemic activity in mouse models of FLT3 mutated acute myeloid leukemia..  Investigational new drugs,      [PMID:28516360]
251. Cannarile, Michael A MA and 5 more authors..  (2017)  Colony-stimulating factor 1 receptor (CSF1R) inhibitors in cancer therapy..  Journal for immunotherapy of cancer,    (18):   [PMID:28716061]
252. Crawford, Lindsey B LB and 8 more authors..  (2018)  Human Cytomegalovirus Encodes a Novel FLT3 Receptor Ligand Necessary for Hematopoietic Cell Differentiation and Viral Reactivation..  mBio,    (24):   [PMID:29691342]
253. Yalcin, Suayib and Lacin, Sahin..  (2019)  Impact of tivozanib on patient outcomes in treatment of advanced renal cell carcinoma..  Cancer management and research,      [PMID:31496820]

Solution Calculators