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Recombinant Human FGFR1 Protein, ＞95% (SDS-PAGE), high purity

  • ActiBioPure™
  • Animal Free
  • Azide Free
  • Bioactive
  • Carrier Free
  • High performance
  • ≥95%(SDS-PAGE)
Features and benefits
  • Expression System: HEK293
  • Accession #: P11362.1
  • Protein Tag: C-Fc & His
  • Bioactivity: Measured by its ability to inhibit FGF1 dependent proliferation of Balb/c-3T3 cells. The ED50 for this effect is typically 0.5-5 ng/mL.
  • Endotoxin Concentration: < 0.1 EU/μg
Item Number
rp145988
Grouped product items
SKUSizeAvailabilityPrice Qty
rp145988-10μg
10μg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$79.90
rp145988-50μg
50μg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$199.90
rp145988-100μg
100μg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$309.90
rp145988-1mg
1mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$2,259.90
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Animal Free, >95% (SDS-PAGE), Active, 293F, C-Fc&His tag, 22-376 aa

View related series
Accession#:P11362 FGFR1 Gene ID:2260

Basic Description

Product NameRecombinant Human FGFR1 Protein, ＞95% (SDS-PAGE), high purity
SynonymsBasic fibroblast growth factor receptor 1; bFGF-R-1; BFGFR; CD331; CEK; FGFBR; FGFR 1; FGFR-1; FGFR1; FGFR1/PLAG1 fusion; FGFR1_HUMAN; fibroblast growth factor receptor 1; FLG; FLT-2; FLT2; Fms-like gene; Fms-like tyrosine kinase 2; fms-related tyrosine k
GradeActiBioPure™, Animal Free, Azide Free, Bioactive, Carrier Free, High performance
Product Description

Purity
＞95% SDS-PAGE.
Additional sequence information
C-terminal Fc&His tag
Function
Receptor for basic fibroblast growth factor. Receptor for FGF23 in the presence of KL (By similarity). A shorter form of the receptor could be a receptor for FGF1 (aFGF).

Specifications & PurityActiBioPure™, Bioactive, Animal Free, Carrier Free, Azide Free, High performance, ≥95%(SDS-PAGE)
Purity＞95% (SDS-PAGE)
BioactivityMeasured by its ability to inhibit FGF1 dependent proliferation of Balb/c-3T3 cells. The ED50 for this effect is typically 0.5-5 ng/mL.
Endotoxin Concentration< 0.1 EU/μg
Expression SystemHEK293
SpeciesHuman
Amino Acids22-376 aa
SequenceRPSPTLPEQAQPWGAPVEVESFLVHPGDLLQLRCRLRDDVQSINWLRDGVQLAESNRTRITGEEVEVQDSVPADSGLYACVTSSPSGSDTTYFSVNVSDALPSSEDDDDDDDSSSEEKETDNTKPNRMPVAPYWTSPEKMEKKLHAVPAAKTVKFKCPSSGTPNPTLRWLKNGKEFKPDHRIGGYKVRYATWSIIMDSVVPSDKGNYTCIVENEYGSINHTYQLDVVERSPHRPILQAGLPANKTVALGSNVEFM
Protein TagC-Fc & His
Accession #P11362.1
Predicted molecular weight67 kDa
SDS-PAGE100-110 kDa, under reducing conditions.

Images

Recombinant Human FGFR1 Protein (rp145988) - Protein Bioactivity
Measured by its ability to inhibit FGF1 dependent proliferation of Balb/c-3T3 cells. The ED₅₀ for this effect is typically 1.2 ng/mL.

Recombinant Human FGFR1 Protein (rp145988) - SDS-PAGE
3 μg/lane of Recombinant Human FGFR1 Protein was resolved with SDS-PAGE under reducing (R) and non-reducing (N) conditions and visualized by Coomassie® Blue staining, showing the band at 90.0 - 120.0 kDa under reducing conditions and 90.0 - 120.0 & 180.0 - 240.0 kDa under non-reducing conditions.

Product Specifications

FormLyophilized
ReconstitutionReconstitute to a concentration of 0.1-0.5 mg/mL in sterile distilled water.
Storage TempStore at -20°C,Avoid repeated freezing and thawing
Shipped InWet ice
Stability And StorageStore at -20~-80℃ for more than 1 year. Upon delivery aliquot. Avoid freeze/thaw cycle.

Certificates

Certificate of Analysis(COA)

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3 results found

Lot NumberCertificate TypeDateItem
ZJ24F0404966Certificate of AnalysisApr 30, 2024 rp145988
ZJ24F0404965Certificate of AnalysisApr 30, 2024 rp145988
ZJ24F0404964Certificate of AnalysisApr 30, 2024 rp145988

Related Documents

 SDS

 Specification Sheet

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. Mohammadi M, Schlessinger J, Hubbard SR.  (1996)  Structure of the FGF receptor tyrosine kinase domain reveals a novel autoinhibitory mechanism..  Cell,  86  (4): (577-87).  [PMID:8752212]
3. Soth M, Hermann JC, Yee C, Alam M, Barnett JW, Berry P, Browner MF, Frank K, Frauchiger S, Harris S et al..  (2013)  3-Amido pyrrolopyrazine JAK kinase inhibitors: development of a JAK3 vs JAK1 selective inhibitor and evaluation in cellular and in vivo models..  J Med Chem,  56  (1): (345-56).  [PMID:23214979]
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. Gerhard DS, Wagner L, Feingold EA, Shenmen CM, Grouse LH, Schuler G, Klein SL, Old S, Rasooly R, Good P et al..  (2004)  The status, quality, and expansion of the NIH full-length cDNA project: the Mammalian Gene Collection (MGC)..  Genome Res,  14  (10B): (2121-7).  [PMID:15489334]
6. Ota T, Suzuki Y, Nishikawa T, Otsuki T, Sugiyama T, Irie R, Wakamatsu A, Hayashi K, Sato H, Nagai K et al..  (2004)  Complete sequencing and characterization of 21,243 full-length human cDNAs..  Nat Genet,  36  (1): (40-5).  [PMID:14702039]
7. Zhou W, Hur W, McDermott U, Dutt A, Xian W, Ficarro SB, Zhang J, Sharma SV, Brugge J, Meyerson M et al..  (2010)  A structure-guided approach to creating covalent FGFR inhibitors..  Chem Biol,  17  (3): (285-95).  [PMID:20338520]
8. Adrián FJ, Ding Q, Sim T, Velentza A, Sloan C, Liu Y, Zhang G, Hur W, Ding S, Manley P et al..  (2006)  Allosteric inhibitors of Bcr-abl-dependent cell proliferation..  Nat Chem Biol,  2  (2): (95-102).  [PMID:16415863]
9. 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]
10. Sun L, Liang C, Shirazian S, Zhou Y, Miller T, Cui J, Fukuda JY, Chu JY, Nematalla A, Wang X et al..  (2003)  Discovery of 5-[5-fluoro-2-oxo-1,2- dihydroindol-(3Z)-ylidenemethyl]-2,4- dimethyl-1H-pyrrole-3-carboxylic acid (2-diethylaminoethyl)amide, a novel tyrosine kinase inhibitor targeting vascular endothelial and platelet-derived growth factor receptor tyrosine kinase..  J Med Chem,  46  (7): (1116-9).  [PMID:12646019]
11. Lombardo LJ, Lee FY, Chen P, Norris D, Barrish JC, Behnia K, Castaneda S, Cornelius LA, Das J, Doweyko AM et al..  (2004)  Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays..  J Med Chem,  47  (27): (6658-61).  [PMID:15615512]
12. Manley PW, Furet P, Bold G, Brüggen J, Mestan J, Meyer T, Schnell CR, Wood J, Haberey M, Huth A et al..  (2002)  Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors..  J Med Chem,  45  (26): (5687-93).  [PMID:12477352]
13. Zhou Y, Chen Y, Tong L, Xie H, Wen W, Zhang J, Xi Y, Shen Y, Geng M, Wang Y et al..  (2012)  AL3810, a multi-tyrosine kinase inhibitor, exhibits potent anti-angiogenic and anti-tumour activity via targeting VEGFR, FGFR and PDGFR..  J Cell Mol Med,  16  (10): (2321-30).  [PMID:22304225]
14. Hennequin LF, Allen J, Breed J, Curwen J, Fennell M, Green TP, Lambert-van der Brempt C, Morgentin R, Norman RA, Olivier A et al..  (2006)  N-(5-chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5- (tetrahydro-2H-pyran-4-yloxy)quinazolin-4-amine, a novel, highly selective, orally available, dual-specific c-Src/Abl kinase inhibitor..  J Med Chem,  49  (22): (6465-88).  [PMID:17064066]
15. 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]
16. 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]
17. Klutchko SR, Zhou H, Winters RT, Tran TP, Bridges AJ, Althaus IW, Amato DM, Elliott WL, Ellis PA, Meade MA et al..  (2006)  Tyrosine kinase inhibitors. 19. 6-Alkynamides of 4-anilinoquinazolines and 4-anilinopyrido[3,4-d]pyrimidines as irreversible inhibitors of the erbB family of tyrosine kinase receptors..  J Med Chem,  49  (4): (1475-85).  [PMID:16480284]
18. 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]
19. 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]
20. Sun L, Tran N, Liang C, Tang F, Rice A, Schreck R, Waltz K, Shawver LK, McMahon G, Tang C.  (1999)  Design, synthesis, and evaluations of substituted 3-[(3- or 4-carboxyethylpyrrol-2-yl)methylidenyl]indolin-2-ones as inhibitors of VEGF, FGF, and PDGF receptor tyrosine kinases..  J Med Chem,  42  (25): (5120-30).  [PMID:10602697]
21. Guagnano V, Furet P, Spanka C, Bordas V, Le Douget M, Stamm C, Brueggen J, Jensen MR, Schnell C, Schmid H et al..  (2011)  Discovery of 3-(2,6-dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea (NVP-BGJ398), a potent and selective inhibitor of the fibroblast growth factor receptor family of receptor tyrosine kinase..  J Med Chem,  54  (20): (7066-83).  [PMID:21936542]
22. Cheng H, Li C, Bailey S, Baxi SM, Goulet L, Guo L, Hoffman J, Jiang Y, Johnson TO, Johnson TW et al..  (2013)  Discovery of the Highly Potent PI3K/mTOR Dual Inhibitor PF-04979064 through Structure-Based Drug Design..  ACS Med Chem Lett,  4  (1): (91-7).  [PMID:24900568]
23. Fancelli D, Moll J, Varasi M, Bravo R, Artico R, Berta D, Bindi S, Cameron A, Candiani I, Cappella P et al..  (2006)  1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazoles: identification of a potent Aurora kinase inhibitor with a favorable antitumor kinase inhibition profile..  J Med Chem,  49  (24): (7247-51).  [PMID:17125279]
24. 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]
25. 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]
26. 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]
27. Manfredi MG, Ecsedy JA, Meetze KA, Balani SK, Burenkova O, Chen W, Galvin KM, Hoar KM, Huck JJ, LeRoy PJ et al..  (2007)  Antitumor activity of MLN8054, an orally active small-molecule inhibitor of Aurora A kinase..  Proc Natl Acad Sci USA,  104  (10): (4106-11).  [PMID:17360485]
28. Mendel DB, Laird AD, Xin X, Louie SG, Christensen JG, Li G, Schreck RE, Abrams TJ, Ngai TJ, Lee LB et al..  (2003)  In vivo antitumor activity of SU11248, a novel tyrosine kinase inhibitor targeting vascular endothelial growth factor and platelet-derived growth factor receptors: determination of a pharmacokinetic/pharmacodynamic relationship..  Clin Cancer Res,  9  (1): (327-37).  [PMID:12538485]
29. 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]
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. Zhao G, Li WY, Chen D, Henry JR, Li HY, Chen Z, Zia-Ebrahimi M, Bloem L, Zhai Y, Huss K et al..  (2011)  A novel, selective inhibitor of fibroblast growth factor receptors that shows a potent broad spectrum of antitumor activity in several tumor xenograft models..  Mol Cancer Ther,  10  (11): (2200-10).  [PMID:21900693]
32. Hall MD, Salam NK, Hellawell JL, Fales HM, Kensler CB, Ludwig JA, Szakács G, Hibbs DE, Gottesman MM.  (2009)  Synthesis, activity, and pharmacophore development for isatin-beta-thiosemicarbazones with selective activity toward multidrug-resistant cells..  J Med Chem,  52  (10): (3191-204).  [PMID:19397322]
33. Lafleur K, Huang D, Zhou T, Caflisch A, Nevado C.  (2009)  Structure-based optimization of potent and selective inhibitors of the tyrosine kinase erythropoietin producing human hepatocellular carcinoma receptor B4 (EphB4)..  J Med Chem,  52  (20): (6433-46).  [PMID:19788238]
34. 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]
35. Panek RL, Lu GH, Klutchko SR, Batley BL, Dahring TK, Hamby JM, Hallak H, Doherty AM, Keiser JA.  (1997)  In vitro pharmacological characterization of PD 166285, a new nanomolar potent and broadly active protein tyrosine kinase inhibitor..  J Pharmacol Exp Ther,  283  (3): (1433-44).  [PMID:9400019]
36. 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]
37. 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]
38. 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]
39. 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]
40. Hennequin LF, Thomas AP, Johnstone C, Stokes ES, Plé PA, Lohmann JJ, Ogilvie DJ, Dukes M, Wedge SR, Curwen JO et al..  (1999)  Design and structure-activity relationship of a new class of potent VEGF receptor tyrosine kinase inhibitors..  J Med Chem,  42  (26): (5369-89).  [PMID:10639280]
41. Adams ND, Adams JL, Burgess JL, Chaudhari AM, Copeland RA, Donatelli CA, Drewry DH, Fisher KE, Hamajima T, Hardwicke MA et al..  (2010)  Discovery of GSK1070916, a potent and selective inhibitor of Aurora B/C kinase..  J Med Chem,  53  (10): (3973-4001).  [PMID:20420387]
42. 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]
43. Hagel M, Miduturu C, Sheets M, Rubin N, Weng W, Stransky N, Bifulco N, Kim JL, Hodous B, Brooijmans N et al..  (2015)  First Selective Small Molecule Inhibitor of FGFR4 for the Treatment of Hepatocellular Carcinomas with an Activated FGFR4 Signaling Pathway..  Cancer Discov,  5  (4): (424-37).  [PMID:25776529]
44. 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]
45. 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]
46. 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]
47. Tan L, Gurbani D, Weisberg EL, Jones DS, Rao S, Singer WD, Bernard FM, Mowafy S, Jenney A, Du G et al..  (2017)  Studies of TAK1-centered polypharmacology with novel covalent TAK1 inhibitors..  Bioorg Med Chem,  25  (4): (1320-1328).  [PMID:28038940]
48. Hall TG, Yu Y, Eathiraj S, Wang Y, Savage RE, Lapierre JM, Schwartz B, Abbadessa G.  (2016)  Preclinical Activity of ARQ 087, a Novel Inhibitor Targeting FGFR Dysregulation..  PLoS ONE,  11  (9): (e0162594).  [PMID:27627808]
49. Brameld KA, Owens TD, Verner E, Venetsanakos E, Bradshaw JM, Phan VT, Tam D, Leung K, Shu J, LaStant J et al..  (2017)  Discovery of the Irreversible Covalent FGFR Inhibitor 8-(3-(4-Acryloylpiperazin-1-yl)propyl)-6-(2,6-dichloro-3,5-dimethoxyphenyl)-2-(methylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (PRN1371) for the Treatment of Solid Tumors..  J Med Chem,  60  (15): (6516-6527).  [PMID:28665128]
50. 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]
51. Bachegowda L, Morrone K, Winski SL, Mantzaris I, Bartenstein M, Ramachandra N, Giricz O, Sukrithan V, Nwankwo G, Shahnaz S et al..  (2016)  Pexmetinib: A Novel Dual Inhibitor of Tie2 and p38 MAPK with Efficacy in Preclinical Models of Myelodysplastic Syndromes and Acute Myeloid Leukemia..  Cancer Res,  76  (16): (4841-4849).  [PMID:27287719]
52. Pippione AC, Sainas S, Federico A, Lupino E, Piccinini M, Kubbutat M, Contreras JM, Morice C, Barge A, Ducime A et al..  (2018)  N-Acetyl-3-aminopyrazoles block the non-canonical NF-kB cascade by selectively inhibiting NIK..  Medchemcomm,  9  (6): (963-968).  [PMID:30108985]
53. 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]
54. Heffron TP, Ndubaku CO, Salphati L, Alicke B, Cheong J, Drobnick J, Edgar K, Gould SE, Lee LB, Lesnick JD et al..  (2016)  Discovery of Clinical Development Candidate GDC-0084, a Brain Penetrant Inhibitor of PI3K and mTOR..  ACS Med Chem Lett,  7  (4): (351-6).  [PMID:27096040]
55. 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]
56. You WK, Sennino B, Williamson CW, Falcón B, Hashizume H, Yao LC, Aftab DT, McDonald DM.  (2011)  VEGF and c-Met blockade amplify angiogenesis inhibition in pancreatic islet cancer..  Cancer Res,  71  (14): (4758-68).  [PMID:21613405]
57. 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]
58. Cabrera DG, Horatscheck A, Wilson CR, Basarab G, Eyermann CJ, Chibale K.  (2018)  Plasmodial Kinase Inhibitors: License to Cure?.  J Med Chem,  61  (18): (8061-8077).  [PMID:29771541]
59. Liao AT, Chien MB, Shenoy N, Mendel DB, McMahon G, Cherrington JM, London CA.  (2002)  Inhibition of constitutively active forms of mutant kit by multitargeted indolinone tyrosine kinase inhibitors..  Blood,  100  (2): (585-93).  [PMID:12091352]
60. Kurosu H, Choi M, Ogawa Y, Dickson AS, Goetz R, Eliseenkova AV, Mohammadi M, Rosenblatt KP, Kliewer SA, Kuro-O M.  (2007)  Tissue-specific expression of betaKlotho and fibroblast growth factor (FGF) receptor isoforms determines metabolic activity of FGF19 and FGF21..  J Biol Chem,  282  (37): (26687-26695).  [PMID:17623664]
61. 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]
62. 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]
63. 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]
64. 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]
65. Bing Yu,Li-da Tang,Yi-Liang Li,Shu-Hui Song,Xiao-Liang Ji,Mu-Sen Lin,Chun-Fu Wu.  (2011-12-16)  Design, synthesis and antitumor activity of 4-aminoquinazoline derivatives targeting VEGFR-2 tyrosine kinase..  Bioorganic & medicinal chemistry letters,  22  ((1)): (110-114).  [PMID:22169262]
66. 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]
67. Rewcastle GW, Murray DK, Elliott WL, Fry DW, Howard CT, Nelson JM, Roberts BJ, Vincent PW, Showalter HD, Winters RT, Denny WA..  (1998)  Tyrosine kinase inhibitors. 14. Structure-activity relationships for methylamino-substituted derivatives of 4-[(3-bromophenyl)amino]-6-(methylamino)-pyrido[3,4-d]pyrimidine (PD 158780), a potent and specific inhibitor of the tyrosine kinase activity of receptors for the EGF family of growth factors..  J Med Chem,  41  (5): (742-751).  [PMID:9513602]
68. Thompson AM, Connolly CJ, Hamby JM, Boushelle S, Hartl BG, Amar AM, Kraker AJ, Driscoll DL, Steinkampf RW, Patmore SJ, Vincent PW, Roberts BJ, Elliott WL, Klohs W, Leopold WR, Showalter HD, Denny WA..  (2000)  3-(3,5-Dimethoxyphenyl)-1,6-naphthyridine-2,7-diamines and related 2-urea derivatives are potent and selective inhibitors of the FGF receptor-1 tyrosine kinase..  J Med Chem,  43  (22): (4200-4211).  [PMID:11063616]
69. Hennequin LF, Stokes ES, Thomas AP, Johnstone C, Plé PA, Ogilvie DJ, Dukes M, Wedge SR, Kendrew J, Curwen JO..  (2002)  Novel 4-anilinoquinazolines with C-7 basic side chains: design and structure activity relationship of a series of potent, orally active, VEGF receptor tyrosine kinase inhibitors..  J Med Chem,  45  (6): (1300-1312).  [PMID:11881999]
70. Pevarello P, Brasca MG, Amici R, Orsini P, Traquandi G, Corti L, Piutti C, Sansonna P, Villa M, Pierce BS, Pulici M, Giordano P, Martina K, Fritzen EL, Nugent RA, Casale E, Cameron A, Ciomei M, Roletto F, Isacchi A, Fogliatto G, Pesenti E, Pastori W, Marsiglio A, Leach KL, Clare PM, Fiorentini F, Varasi M, Vulpetti A, Warpehoski MA..  (2004)  3-Aminopyrazole inhibitors of CDK2/cyclin A as antitumor agents. 1. Lead finding..  J Med Chem,  47  (13): (3367-3380).  [PMID:15189033]
71. Borzilleri RM, Zheng X, Qian L, Ellis C, Cai ZW, Wautlet BS, Mortillo S, Jeyaseelan R, Kukral DW, Fura A, Kamath A, Vyas V, Tokarski JS, Barrish JC, Hunt JT, Lombardo LJ, Fargnoli J, Bhide RS..  (2005)  Design, synthesis, and evaluation of orally active 4-(2,4-difluoro-5-(methoxycarbamoyl)phenylamino)pyrrolo[2,1-f][1,2,4]triazines as dual vascular endothelial growth factor receptor-2 and fibroblast growth factor receptor-1 inhibitors..  J Med Chem,  48  (12): (3991-4008).  [PMID:15943473]
72. VanderWel SN, Harvey PJ, McNamara DJ, Repine JT, Keller PR, Quin J, Booth RJ, Elliott WL, Dobrusin EM, Fry DW, Toogood PL..  (2005)  Pyrido[2,3-d]pyrimidin-7-ones as specific inhibitors of cyclin-dependent kinase 4..  J Med Chem,  48  (7): (2371-2387).  [PMID:15801830]
73. Revesz L, Blum E, Di Padova FE, Buhl T, Feifel R, Gram H, Hiestand P, Manning U, Neumann U, Rucklin G..  (2006)  Pyrazoloheteroaryls: novel p38alpha MAP kinase inhibiting scaffolds with oral activity..  Bioorg Med Chem Lett,  16  (2): (262-266).  [PMID:16249085]
74. McDermott LA, Higgins B, Simcox M, Luk KC, Nevins T, Kolinsky K, Smith M, Yang H, Li JK, Chen Y, Ke J, Mallalieu N, Egan T, Kolis S, Railkar A, Gerber L, Liu JJ, Konzelmann F, Zhang Z, Flynn T, Morales O, Chen Y..  (2006)  Biological evaluation of a multi-targeted small molecule inhibitor of tumor-induced angiogenesis..  Bioorg Med Chem Lett,  16  (7): (1950-1953).  [PMID:16460940]
75. 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]
76. 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]
77. Potashman MH, Bready J, Coxon A, DeMelfi TM, DiPietro L, Doerr N, Elbaum D, Estrada J, Gallant P, Germain J, Gu Y, Harmange JC, Kaufman SA, Kendall R, Kim JL, Kumar GN, Long AM, Neervannan S, Patel VF, Polverino A, Rose P, Plas Sv, Whittington D, Zanon R, Zhao H..  (2007)  Design, synthesis, and evaluation of orally active benzimidazoles and benzoxazoles as vascular endothelial growth factor-2 receptor tyrosine kinase inhibitors..  J Med Chem,  50  (18): (4351-4373).  [PMID:17696416]
78. 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]
79. 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]
80. Xia Z, Knaak C, Ma J, Beharry ZM, McInnes C, Wang W, Kraft AS, Smith CD..  (2009)  Synthesis and evaluation of novel inhibitors of Pim-1 and Pim-2 protein kinases..  J Med Chem,  52  (1): (74-86).  [PMID:19072652]
81. Peach ML, Tan N, Choyke SJ, Giubellino A, Athauda G, Burke TR, Nicklaus MC, Bottaro DP..  (2009)  Directed discovery of agents targeting the Met tyrosine kinase domain by virtual screening..  J Med Chem,  52  (4): (943-951).  [PMID:19199650]
82. Mohammadi M, McMahon G, Sun L, Tang C, Hirth P, Yeh BK, Hubbard SR, Schlessinger J..  (1997)  Structures of the tyrosine kinase domain of fibroblast growth factor receptor in complex with inhibitors..  Science,  276  (5314): (955-960).  [PMID:9139660]
83. Park BS, El-Deeb IM, Yoo KH, Oh CH, Cho SJ, Han DK, Lee HS, Lee JY, Lee SH..  (2009)  Design, synthesis and biological evaluation of new potent and highly selective ROS1-tyrosine kinase inhibitor..  Bioorg Med Chem Lett,  19  (16): (4720-4723).  [PMID:19596575]
84. Kraker AJ, Hartl BG, Amar AM, Barvian MR, Showalter HD, Moore CW..  (2000)  Biochemical and cellular effects of c-Src kinase-selective pyrido[2, 3-d]pyrimidine tyrosine kinase inhibitors..  Biochem Pharmacol,  60  (7): (885-898).  [PMID:10974196]
85. Cha MY, Lee KO, Kim JW, Lee CG, Song JY, Kim YH, Lee GS, Park SB, Kim MS..  (2009)  Discovery of a novel Her-1/Her-2 dual tyrosine kinase inhibitor for the treatment of Her-1 selective inhibitor-resistant non-small cell lung cancer..  J Med Chem,  52  (21): (6880-6888).  [PMID:19888761]
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. Ravindranathan KP, Mandiyan V, Ekkati AR, Bae JH, Schlessinger J, Jorgensen WL..  (2010)  Discovery of novel fibroblast growth factor receptor 1 kinase inhibitors by structure-based virtual screening..  J Med Chem,  53  (4): (1662-1672).  [PMID:20121196]
88. 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]
89. Bavetsias V, Large JM, Sun C, Bouloc N, Kosmopoulou M, Matteucci M, Wilsher NE, Martins V, Reynisson J, Atrash B, Faisal A, Urban F, Valenti M, de Haven Brandon A, Box G, Raynaud FI, Workman P, Eccles SA, Bayliss R, Blagg J, Linardopoulos S, McDonald E..  (2010)  Imidazo[4,5-b]pyridine derivatives as inhibitors of Aurora kinases: lead optimization studies toward the identification of an orally bioavailable preclinical development candidate..  J Med Chem,  53  (14): (5213-5228).  [PMID:20565112]
90. 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]
91. 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]
92. Ye P, Kuhn C, Juan M, Sharma R, Connolly B, Alton G, Liu H, Stanton R, Kablaoui NM..  (2011)  Potent and selective thiophene urea-templated inhibitors of S6K..  Bioorg Med Chem Lett,  21  (2): (849-852).  [PMID:21185721]
93. 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]
94. 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,  1  (9): (454-459).  [PMID:24900231]
95. 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]
96. 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]
97. Lumeras W, Vidal L, Vidal B, Balagué C, Orellana A, Maldonado M, Domínguez M, Segarra V, Caturla F..  (2011)  1,7-Naphthyridine 1-oxides as novel potent and selective inhibitors of p38 mitogen activated protein kinase..  J Med Chem,  54  (22): (7899-7910).  [PMID:21999461]
98. Ishikawa T, Seto M, Banno H, Kawakita Y, Oorui M, Taniguchi T, Ohta Y, Tamura T, Nakayama A, Miki H, Kamiguchi H, Tanaka T, Habuka N, Sogabe S, Yano J, Aertgeerts K, Kamiyama K..  (2011)  Design and synthesis of novel human epidermal growth factor receptor 2 (HER2)/epidermal growth factor receptor (EGFR) dual inhibitors bearing a pyrrolo[3,2-d]pyrimidine scaffold..  J Med Chem,  54  (23): (8030-8050).  [PMID:22003817]
99. Powell NA, Kohrt JT, Filipski KJ, Kaufman M, Sheehan D, Edmunds JE, Delaney A, Wang Y, Bourbonais F, Lee DY, Schwende F, Sun F, McConnell P, Catana C, Chen H, Ohren J, Perrin LA..  (2012)  Novel and selective spiroindoline-based inhibitors of Sky kinase..  Bioorg Med Chem Lett,  22  (1): (190-193).  [PMID:22119469]
100. Caruso M, Valsasina B, Ballinari D, Bertrand J, Brasca MG, Caldarelli M, Cappella P, Fiorentini F, Gianellini LM, Scolaro A, Beria I..  (2012)  5-(2-amino-pyrimidin-4-yl)-1H-pyrrole and 2-(2-amino-pyrimidin-4-yl)-1,5,6,7-tetrahydro-pyrrolo[3,2-c]pyridin-4-one derivatives as new classes of selective and orally available Polo-like kinase 1 inhibitors..  Bioorg Med Chem Lett,  22  (1): (96-101).  [PMID:22154349]
101. 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]
102. 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]
103. Zhang J, Deng X, Choi HG, Alessi DR, Gray NS..  (2012)  Characterization of TAE684 as a potent LRRK2 kinase inhibitor..  Bioorg Med Chem Lett,  22  (5): (1864-1869).  [PMID:22335897]
104. 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]
105. Martínez González S, Hernández AI, Varela C, Rodríguez-Arístegui S, Lorenzo M, Rodríguez A, Rivero V, Martín JI, Saluste CG, Ramos-Lima F, Cendón E, Cebrián D, Aguirre E, Gomez-Casero E, Albarrán M, Alfonso P, García-Serelde B, Oyarzabal J, Rabal O, Mulero F, Gonzalez-Granda T, Link W, Fominaya J, Barbacid M, Bischoff JR, Pizcueta P, Pastor J..  (2012)  Identification of ETP-46321, a potent and orally bioavailable PI3K α, δ inhibitor..  Bioorg Med Chem Lett,  22  (10): (3460-3466).  [PMID:22520259]
106. 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]
107. Illig CR, Manthey CL, Wall MJ, Meegalla SK, Chen J, Wilson KJ, Ballentine SK, Desjarlais RL, Schubert C, Crysler CS, Chen Y, Molloy CJ, Chaikin MA, Donatelli RR, Yurkow E, Zhou Z, Player MR, Tomczuk BE..  (2011)  Optimization of a potent class of arylamide colony-stimulating factor-1 receptor inhibitors leading to anti-inflammatory clinical candidate 4-cyano-N-[2-(1-cyclohexen-1-yl)-4-[1-[(dimethylamino)acetyl]-4-piperidinyl]phenyl]-1H-imidazole-2-carboxamide (JNJ-28312141)..  J Med Chem,  54  (22): (7860-7883).  [PMID:22039836]
108. 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]
109. 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]
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. Dolečková I, Cesnek M, Dračinský M, Brynda J, Voller J, Janeba Z, Kryštof V..  (2013)  Synthesis and biological evaluation of guanidino analogues of roscovitine..  Eur J Med Chem,  62  (443-452).  [PMID:23399722]
112. 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]
113. 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]
114. 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]
115. 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]
116. Cheng X, Merz KH, Vatter S, Christ J, Wölfl S, Eisenbrand G..  (2014)  7,7'-Diazaindirubin--a small molecule inhibitor of casein kinase 2 in vitro and in cells..  Bioorg Med Chem,  22  (1): (247-255).  [PMID:24326279]
117. 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]
118. Zhang P, Li S, Gao Y, Lu W, Huang K, Ye D, Li X, Chu Y..  (2014)  Novel benzothiazinones (BTOs) as allosteric modulator or substrate competitive inhibitor of glycogen synthase kinase 3β (GSK-3β) with cellular activity of promoting glucose uptake..  Bioorg Med Chem Lett,  24  (24): (5639-5643).  [PMID:25467150]
119. Song Z, Yang Y, Liu Z, Peng X, Guo J, Yang X, Wu K, Ai J, Ding J, Geng M, Zhang A..  (2015)  Discovery of novel 2,4-diarylaminopyrimidine analogues (DAAPalogues) showing potent inhibitory activities against both wild-type and mutant ALK kinases..  J Med Chem,  58  (1): (197-211).  [PMID:24785465]
120. Muth F, Günther M, Bauer SM, Döring E, Fischer S, Maier J, Drückes P, Köppler J, Trappe J, Rothbauer U, Koch P, Laufer SA..  (2015)  Tetra-substituted pyridinylimidazoles as dual inhibitors of p38α mitogen-activated protein kinase and c-Jun N-terminal kinase 3 for potential treatment of neurodegenerative diseases..  J Med Chem,  58  (1): (443-456).  [PMID:25475894]
121. Starosyla SA, Volynets GP, Lukashov SS, Gorbatiuk OB, Golub AG, Bdzhola VG, Yarmoluk SM..  (2015)  Identification of apoptosis signal-regulating kinase 1 (ASK1) inhibitors among the derivatives of benzothiazol-2-yl-3-hydroxy-5-phenyl-1,5-dihydro-pyrrol-2-one..  Bioorg Med Chem,  23  (10): (2489-2497).  [PMID:25882527]
122. Roth GJ, Binder R, Colbatzky F, Dallinger C, Schlenker-Herceg R, Hilberg F, Wollin SL, Kaiser R..  (2015)  Nintedanib: from discovery to the clinic..  J Med Chem,  58  (3): (1053-1063).  [PMID:25474320]
123. Lawrence HR, Mahajan K, Luo Y, Zhang D, Tindall N, Huseyin M, Gevariya H, Kazi S, Ozcan S, Mahajan NP, Lawrence NJ..  (2015)  Development of novel ACK1/TNK2 inhibitors using a fragment-based approach..  J Med Chem,  58  (6): (2746-2763).  [PMID:25699576]
124. Chen CT, Hsu JT, Lin WH, Lu CT, Yen SC, Hsu T, Huang YL, Song JS, Chen CH, Chou LH, Yen KJ, Chen CP, Kuo PC, Huang CL, Liu HE, Chao YS, Yeh TK, Jiaang WT..  (2015)  Identification of a potent 5-phenyl-thiazol-2-ylamine-based inhibitor of FLT3 with activity against drug resistance-conferring point mutations..  Eur J Med Chem,  100  (151-161).  [PMID:26081023]
125. Elkamhawy A, Farag AK, Viswanath AN, Bedair TM, Leem DG, Lee KT, Pae AN, Roh EJ..  (2015)  Targeting EGFR/HER2 tyrosine kinases with a new potent series of 6-substituted 4-anilinoquinazoline hybrids: Design, synthesis, kinase assay, cell-based assay, and molecular docking..  Bioorg Med Chem Lett,  25  (22): (5147-5154).  [PMID:26475520]
126. 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]
127. Shan Y, Wang C, Zhang L, Wang J, Wang M, Dong Y..  (2016)  Expanding the structural diversity of diarylureas as multi-target tyrosine kinase inhibitors..  Bioorg Med Chem,  24  (4): (750-758).  [PMID:26753815]
128. 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]
129. 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]
130. Fan J, Dai Y, Shao J, Peng X, Wang C, Cao S, Zhao B, Ai J, Geng M, Duan W..  (2016)  Design, synthesis and biological evaluation of pyrazolylaminoquinazoline derivatives as highly potent pan-fibroblast growth factor receptor inhibitors..  Bioorg Med Chem Lett,  26  (11): (2594-2599).  [PMID:27117427]
131. 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]
132. Fu J, Xia A, Qi X..  (2016)  Identification of novel peptoid agonists of fibroblast growth factor receptor using microarray-based screening..  Medchemcomm,  7  (6): (1183-1189).  [PMID:27721968]
133. Laufer R, Li SW, Liu Y, Ng G, Lang Y, Feher M, Brokx R, Beletskaya I, Hodgson R, Mao G, Plotnikova O, Awrey DE, Mason JM, Wei X, Lin DC, Che Y, Kiarash R, Madeira B, Fletcher GC, Mak TW, Bray MR, Pauls HW..  (2016)  Discovery of 4-(4-aminopyrazolo[1,5-a][1,3,5]triazin-8-yl)benzamides as novel, highly potent and selective, orally bioavailable inhibitors of Tyrosine Threonine Kinase, TTK..  Bioorg Med Chem Lett,  26  (15): (3562-3566).  [PMID:27335255]
134. Kumar V, Guru SK, Jain SK, Joshi P, Gandhi SG, Bharate SB, Bhushan S, Bharate SS, Vishwakarma RA..  (2016)  A chromatography-free isolation of rohitukine from leaves of Dysoxylum binectariferum: Evaluation for in vitro cytotoxicity, Cdk inhibition and physicochemical properties..  Bioorg Med Chem Lett,  26  (15): (3457-3463).  [PMID:27363938]
135. Kim H, Lee C, Yang JS, Choi S, Park CH, Kang JS, Oh SJ, Yun J, Kim MH, Han G..  (2016)  Structural modifications at the 6-position of thieno[2,3-d]pyrimidines and their effects on potency at FLT3 for treatment of acute myeloid leukemia..  Eur J Med Chem,  120  (74-85).  [PMID:27187860]
136. Klaeger S, Heinzlmeir S and Wilhelm M et al.  (2017)  The target landscape of clinical kinase drugs..  Science,  358  (6367):   [PMID:29191878]
137. Ying S, Du X, Fu W, Yun D, Chen L, Cai Y, Xu Q, Wu J, Li W, Liang G..  (2017)  Synthesis, biological evaluation, QSAR and molecular dynamics simulation studies of potential fibroblast growth factor receptor 1 inhibitors for the treatment of gastric cancer..  Eur J Med Chem,  127  (885-899).  [PMID:27829519]
138. Chen Y, Zheng Y, Jiang Q, Qin F, Zhang Y, Fu L, He G..  (2017)  Integrated bioinformatics, computational and experimental methods to discover novel Raf/extracellular-signal regulated kinase (ERK) dual inhibitors against breast cancer cells..  Eur J Med Chem,  127  (997-1011).  [PMID:27839788]
139. 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]
140. Hoemann M, Wilson N, Argiriadi M, Banach D, Burchat A, Calderwood D, Clapham B, Cox P, Duignan DB, Konopacki D, Somal G, Vasudevan A..  (2016)  Synthesis and optimization of furano[3,2-d]pyrimidines as selective spleen tyrosine kinase (Syk) inhibitors..  Bioorg Med Chem Lett,  26  (22): (5562-5567).  [PMID:27789138]
141. 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]
142. 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]
143. Zhu W, Chen H, Wang Y, Wang J, Peng X, Chen X, Gao Y, Li C, He Y, Ai J, Geng M, Zheng M, Liu H..  (2017)  Design, Synthesis, and Pharmacological Evaluation of Novel Multisubstituted Pyridin-3-amine Derivatives as Multitargeted Protein Kinase Inhibitors for the Treatment of Non-Small Cell Lung Cancer..  J Med Chem,  60  (14): (6018-6035).  [PMID:28714692]
144. 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]
145. Zhao F, Zhang LD, Hao Y, Chen N, Bai R, Wang YJ, Zhang CC, Li GS, Hao LJ, Shi C, Zhang J, Mao Y, Fan Y, Xia GX, Yu JX, Liu YJ..  (2017)  Identification of 3-substituted-6-(1-(1H-[1,2,3]triazolo[4,5-b]pyrazin-1-yl)ethyl)quinoline derivatives as highly potent and selective mesenchymal-epithelial transition factor (c-Met) inhibitors via metabolite profiling-based structural optimization..  Eur J Med Chem,  134  (147-158).  [PMID:28411455]
146. Wagman AS, Boyce RS, Brown SP, Fang E, Goff D, Jansen JM, Le VP, Levine BH, Ng SC, Ni ZJ, Nuss JM, Pfister KB, Ramurthy S, Renhowe PA, Ring DB, Shu W, Subramanian S, Zhou XA, Shafer CM, Harrison SD, Johnson KW, Bussiere DE..  (2017)  Synthesis, Binding Mode, and Antihyperglycemic Activity of Potent and Selective (5-Imidazol-2-yl-4-phenylpyrimidin-2-yl)[2-(2-pyridylamino)ethyl]amine Inhibitors of Glycogen Synthase Kinase 3..  J Med Chem,  60  (20): (8482-8514).  [PMID:29016121]
147. 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]
148. 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]
149. 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]
150. Zhou D, Springer MZ, Xu D, Liu D, Hudmon A, Macleod KF, Meroueh SO..  (2017)  Small molecules inhibit STAT3 activation, autophagy, and cancer cell anchorage-independent growth..  Bioorg Med Chem,  25  (12): (2995-3005).  [PMID:28438385]
151. 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]
152. 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]
153. 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]
154. 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]
155. 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]
156. 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]
157. Zang J, Liang X, Huang Y, Jia Y, Li X, Xu W, Chou CJ, Zhang Y..  (2018)  Discovery of Novel Pazopanib-Based HDAC and VEGFR Dual Inhibitors Targeting Cancer Epigenetics and Angiogenesis Simultaneously..  J Med Chem,  61  (12): (5304-5322).  [PMID:29787262]
158. Cho H, Shin I, Ju E, Choi S, Hur W, Kim H, Hong E, Kim ND, Choi HG, Gray NS, Sim T..  (2018)  First SAR Study for Overriding NRAS Mutant Driven Acute Myeloid Leukemia..  J Med Chem,  61  (18): (8353-8373).  [PMID:30153003]
159. 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]
160. 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]
161. Pan Z, Chen Y, Liu J, Jiang Q, Yang S, Guo L, He G..  (2018)  Design, synthesis, and biological evaluation of polo-like kinase 1/eukaryotic elongation factor 2 kinase (PLK1/EEF2K) dual inhibitors for regulating breast cancer cells apoptosis and autophagy..  Eur J Med Chem,  144  (517-528).  [PMID:29288948]
162. Lovering F, Morgan P, Allais C, Aulabaugh A, Brodfuehrer J, Chang J, Coe J, Ding W, Dowty H, Fleming M, Frisbie R, Guzova J, Hepworth D, Jasti J, Kortum S, Kurumbail R, Mohan S, Papaioannou N, Strohbach JW, Vincent F, Lee K, Zapf CW..  (2018)  Rational approach to highly potent and selective apoptosis signal-regulating kinase 1 (ASK1) inhibitors..  Eur J Med Chem,  145  (606-621).  [PMID:29348070]
163. 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]
164. 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]
165. Baladi T, Aziz J, Dufour F, Abet V, Stoven V, Radvanyi F, Poyer F, Wu TD, Guerquin-Kern JL, Bernard-Pierrot I, Garrido SM, Piguel S..  (2018)  Design, synthesis, biological evaluation and cellular imaging of imidazo[4,5-b]pyridine derivatives as potent and selective TAM inhibitors..  Bioorg Med Chem,  26  (20): (5510-5530).  [PMID:30309671]
166. 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]
167. 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]
168. 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]
169. 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]
170. Choi MJ, Roh EJ, Hur W, Lee SH, Sim T, Oh CH, Lee SH, Kim JS, Yoo KH..  (2018)  Design, synthesis, and biological evaluation of novel aminopyrimidinylisoindolines as AXL kinase inhibitors..  Bioorg Med Chem Lett,  28  (23-24): (3761-3765).  [PMID:30340900]
171. 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]
172. Osborne J, Birchall K, Tsagris DJ, Lewis SJ, Smiljanic-Hurley E, Taylor DL, Levy A, Alessi DR, McIver EG..  (2019)  Discovery of potent and selective 5-azaindazole inhibitors of leucine-rich repeat kinase 2 (LRRK2) - Part 1..  Bioorg Med Chem Lett,  29  (4): (668-673).  [PMID:30554956]
173. 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]
174. 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]
175. Liang X, Zang J, Li X, Tang S, Huang M, Geng M, Chou CJ, Li C, Cao Y, Xu W, Liu H, Zhang Y..  (2019)  Discovery of Novel Janus Kinase (JAK) and Histone Deacetylase (HDAC) Dual Inhibitors for the Treatment of Hematological Malignancies..  J Med Chem,  62  (8): (3898-3923).  [PMID:30901208]
176. 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]
177. Harris PA, Faucher N, George N, Eidam PM, King BW, White GV, Anderson NA, Bandyopadhyay D, Beal AM, Beneton V, Berger SB, Campobasso N, Campos S, Capriotti CA, Cox JA, Daugan A, Donche F, Fouchet MH, Finger JN, Geddes B, Gough PJ, Grondin P, Hoffman BL, Hoffman SJ, Hutchinson SE, Jeong JU, Jigorel E, Lamoureux P, Leister LK, Lich JD, Mahajan MK, Meslamani J, Mosley JE, Nagilla R, Nassau PM, Ng SL, Ouellette MT, Pasikanti KK, Potvain F, Reilly MA, Rivera EJ, Sautet S, Schaeffer MC, Sehon CA, Sun H, Thorpe JH, Totoritis RD, Ward P, Wellaway N, Wisnoski DD, Woolven JM, Bertin J, Marquis RW..  (2019)  Discovery and Lead-Optimization of 4,5-Dihydropyrazoles as Mono-Kinase Selective, Orally Bioavailable and Efficacious Inhibitors of Receptor Interacting Protein 1 (RIP1) Kinase..  J Med Chem,  62  (10): (5096-5110).  [PMID:31013427]
178. 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]
179. Lin X, Yosaatmadja Y, Kalyukina M, Middleditch MJ, Zhang Z, Lu X, Ding K, Patterson AV, Smaill JB, Squire CJ..  (2019)  Rotational Freedom, Steric Hindrance, and Protein Dynamics Explain BLU554 Selectivity for the Hinge Cysteine of FGFR4..  ACS Med Chem Lett,  10  (8): (1180-1186).  [PMID:31413803]
180. 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]
181. 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]
182. 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]
183. Wang Y, Li L, Fan J, Dai Y, Jiang A, Geng M, Ai J, Duan W..  (2018)  Discovery of Potent Irreversible Pan-Fibroblast Growth Factor Receptor (FGFR) Inhibitors..  J Med Chem,  61  (20): (9085-9104).  [PMID:29522671]
184. Bronner SM, Merrick KA, Murray J, Salphati L, Moffat JG, Pang J, Sneeringer CJ, Dompe N, Cyr P, Purkey H, Boenig GL, Li J, Kolesnikov A, Larouche-Gauthier R, Lai KW, Shen X, Aubert-Nicol S, Chen YC, Cheong J, Crawford JJ, Hafner M, Haghshenas P, Jakalian A, Leclerc JP, Lim NK, O'Brien T, Plise EG, Shalan H, Sturino C, Wai J, Xiao Y, Yin J, Zhao L, Gould S, Olivero A, Heffron TP..  (2019)  Design of a brain-penetrant CDK4/6 inhibitor for glioblastoma..  Bioorg Med Chem Lett,  29  (16): (2294-2301).  [PMID:31307887]
185. Shen FQ, Shi L, Wang ZF, Wang CR, Chen JJ, Liu Y, Qiu HY, Zhu HL..  (2019)  Design, synthesis, biological evaluation of benzoyl amide derivatives containing nitrogen heterocyclic ring as potential VEGFR-2 inhibitors..  Bioorg Med Chem,  27  (17): (3813-3824).  [PMID:31327679]
186. 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]
187. Heider F, Ansideri F, Tesch R, Pantsar T, Haun U, Döring E, Kudolo M, Poso A, Albrecht W, Laufer SA, Koch P..  (2019)  Pyridinylimidazoles as dual glycogen synthase kinase 3β/p38α mitogen-activated protein kinase inhibitors..  Eur J Med Chem,  175  (309-329).  [PMID:31096153]
188. Lu X, Chen H, Patterson AV, Smaill JB, Ding K..  (2019)  Fibroblast Growth Factor Receptor 4 (FGFR4) Selective Inhibitors as Hepatocellular Carcinoma Therapy: Advances and Prospects..  J Med Chem,  62  (6): (2905-2915).  [PMID:30403487]
189. Andrews LD, Kane TR, Dozzo P, Haglund CM, Hilderbrandt DJ, Linsell MS, Machajewski T, McEnroe G, Serio AW, Wlasichuk KB, Neau DB, Pakhomova S, Waldrop GL, Sharp M, Pogliano J, Cirz RT, Cohen F..  (2019)  Optimization and Mechanistic Characterization of Pyridopyrimidine Inhibitors of Bacterial Biotin Carboxylase..  J Med Chem,  62  (16): (7489-7505).  [PMID:31306011]
190. 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]
191. Xie Z, Wu K, Wang Y, Pan Y, Chen B, Cheng D, Pan S, Guo T, Du X, Fang L, Wang X, Ye F..  (2020)  Discovery of 4,6-pyrimidinediamine derivatives as novel dual EGFR/FGFR inhibitors aimed EGFR/FGFR1-positive NSCLC..  Eur J Med Chem,  187  (111943-111943).  [PMID:31846829]
192. 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]
193. 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]
194. Kuriwaki I, Kameda M, Hisamichi H, Kikuchi S, Iikubo K, Kawamoto Y, Moritomo H, Kondoh Y, Amano Y, Tateishi Y, Echizen Y, Iwai Y, Noda A, Tomiyama H, Suzuki T, Hirano M..  (2020)  Structure-based drug design of 1,3,5-triazine and pyrimidine derivatives as novel FGFR3 inhibitors with high selectivity over VEGFR2..  Bioorg Med Chem,  28  (10): (115453-115453).  [PMID:32278710]
195. Zak M,Hanan EJ,Lupardus P,Brown DG,Robinson C,Siu M,Lyssikatos JP,Romero FA,Zhao G,Kellar T,Mendonca R,Ray NC,Goodacre SC,Crackett PH,McLean N,Hurley CA,Yuen PW,Cheng YX,Liu X,Liimatta M,Kohli PB,Nonomiya J,Salmon G,Buckley G,Lloyd J,Gibbons P,Ghilardi N,Kenny JR,Johnson A.  (2019)  Discovery of a class of highly potent Janus Kinase 1/2 (JAK1/2) inhibitors demonstrating effective cell-based blockade of IL-13 signaling..  Bioorg Med Chem Lett,  29  (12.0): (1522-1531).  [PMID:30981576]
196. 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]
197. 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]
198. Rezende Miranda R,Fu Y,Chen X,Perino J,Cao P,Carpten J,Chen Y,Zhang C.  (2020)  Development of a Potent and Specific FGFR4 Inhibitor for the Treatment of Hepatocellular Carcinoma..  J Med Chem,  63  (20): (11484-11497).  [PMID:33030342]
199. Ebrahim HY,Mohyeldin MM,Hailat MM,El Sayed KA.  (2016)  (1S,2E,4S,7E,11E)-2,7,11-Cembratriene-4,6-diol semisynthetic analogs as novel c-Met inhibitors for the control of c-Met-dependent breast malignancies..  Bioorg Med Chem,  24  (22.0): (5748-5761).  [PMID:27681240]
200. 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]
201. Dart ML,Machleidt T,Jost E,Schwinn MK,Robers MB,Shi C,Kirkland TA,Killoran MP,Wilkinson JM,Hartnett JR,Zimmerman K,Wood KV.  (2018)  Homogeneous Assay for Target Engagement Utilizing Bioluminescent Thermal Shift..  ACS Med Chem Lett,  9  (6.0): (546-551).  [PMID:29937980]
202. Fairhurst RA,Knoepfel T,Buschmann N,Leblanc C,Mah R,Todorov M,Nimsgern P,Ripoche S,Niklaus M,Warin N,Luu VH,Madoerin M,Wirth J,Graus-Porta D,Weiss A,Kiffe M,Wartmann M,Kinyamu-Akunda J,Sterker D,Stamm C,Adler F,Buhles A,Schadt H,Couttet P,Blank J,Galuba I,Trappe J,Voshol J,Ostermann N,Zou C,Berghausen J,Del Rio Espinola A,Jahnke W,Furet P.  (2020)  Discovery of Roblitinib (FGF401) as a Reversible-Covalent Inhibitor of the Kinase Activity of Fibroblast Growth Factor Receptor 4..  J Med Chem,  63  (21.0): (12542-12573).  [PMID:32930584]
203. Kuriwaki I,Kameda M,Iikubo K,Hisamichi H,Kawamoto Y,Kikuchi S,Moritomo H,Kondoh Y,Terasaka T,Amano Y,Tateishi Y,Echizen Y,Iwai Y,Noda A,Tomiyama H,Nakazawa T,Hirano M.  (2021)  Synthesis and structure-activity relationships of pyrimidine derivatives as potent and orally active FGFR3 inhibitors with both increased systemic exposure and enhanced in vitro potency..  Bioorg Med Chem,  33  (116019-116019).  [PMID:33486159]
204. Ashraf-Uz-Zaman M,Shahi S,Akwii R,Sajib MS,Farshbaf MJ,Kallem RR,Putnam W,Wang W,Zhang R,Alvina K,Trippier PC,Mikelis CM,German NA.  (2021)  Design, synthesis and structure-activity relationship study of novel urea compounds as FGFR1 inhibitors to treat metastatic triple-negative breast cancer..  Eur J Med Chem,  209  (112866-112866).  [PMID:33039722]
205. Chen X,Liu Y,Zhang L,Chen D,Dong Z,Zhao C,Liu Z,Xia Q,Wu J,Chen Y,Zheng X,Cai Y.  (2021)  Design, synthesis, and biological evaluation of indazole derivatives as selective and potent FGFR4 inhibitors for the treatment of FGF19-driven hepatocellular cancer..  Eur J Med Chem,  214  (113219-113219).  [PMID:33618175]
206. Zhang CH,Chen K,Jiao Y,Li LL,Li YP,Zhang RJ,Zheng MW,Zhong L,Huang SZ,Song CL,Lin WT,Yang J,Xiang R,Peng B,Han JH,Lu GW,Wei YQ,Yang SY.  (2016)  From Lead to Drug Candidate: Optimization of 3-(Phenylethynyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine Derivatives as Agents for the Treatment of Triple Negative Breast Cancer..  J Med Chem,  59  (21.0): (9788-9805).  [PMID:27739679]
207. 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]
208. Liang X, Tang S, Liu X, Liu Y, Xu Q, Wang X, Saidahmatov A, Li C, Wang J, Zhou Y, Zhang Y, Geng M, Huang M, Liu H..  (2022)  Discovery of Novel Pyrrolo[2,3-d]pyrimidine-based Derivatives as Potent JAK/HDAC Dual Inhibitors for the Treatment of Refractory Solid Tumors..  J Med Chem,  65  (2.0): (1243-1264).  [PMID:33586434]
209. Hattori, Y Y and 8 more authors..  (1992)  K-sam-related gene, N-sam, encodes fibroblast growth factor receptor and is expressed in T-lymphocytic tumors..  Cancer research,    (15):   [PMID:1317750]
210. Peters, K G KG and 7 more authors..  (1992)  Point mutation of an FGF receptor abolishes phosphatidylinositol turnover and Ca2+ flux but not mitogenesis..  Nature,    (20):   [PMID:1379697]
211. Mohammadi, M M and 7 more authors..  (1992)  Point mutation in FGF receptor eliminates phosphatidylinositol hydrolysis without affecting mitogenesis..  Nature,    (20):   [PMID:1379698]
212. Eisemann, A A, Ahn, J A JA, Graziani, G G, Tronick, S R SR and Ron, D D..  (1991)  Alternative splicing generates at least five different isoforms of the human basic-FGF receptor..  Oncogene,      [PMID:1650441]
213. Johnson, D E DE, Lu, J J, Chen, H H, Werner, S S and Williams, L T LT..  (1991)  The human fibroblast growth factor receptor genes: a common structural arrangement underlies the mechanisms for generating receptor forms that differ in their third immunoglobulin domain..  Molecular and cellular biology,      [PMID:1652059]
214. Mohammadi, M M and 9 more authors..  (1991)  A tyrosine-phosphorylated carboxy-terminal peptide of the fibroblast growth factor receptor (Flg) is a binding site for the SH2 domain of phospholipase C-gamma 1..  Molecular and cellular biology,      [PMID:1656221]
215. Kiefer, M C MC and 7 more authors..  (1991)  Molecular cloning of a human basic fibroblast growth factor receptor cDNA and expression of a biologically active extracellular domain in a baculovirus system..  Growth factors (Chur, Switzerland),      [PMID:1662973]
216. Dionne, C A CA and 8 more authors..  (1990)  Cloning and expression of two distinct high-affinity receptors cross-reacting with acidic and basic fibroblast growth factors..  The EMBO journal,      [PMID:1697263]
217. Wennström, S S, Sandström, C C and Claesson-Welsh, L L..  (1991)  cDNA cloning and expression of a human FGF receptor which binds acidic and basic FGF..  Growth factors (Chur, Switzerland),      [PMID:1722683]
218. Hou, J Z JZ and 5 more authors..  (1991)  Fibroblast growth factor receptors from liver vary in three structural domains..  Science (New York, N.Y.),    (8):   [PMID:1846977]
219. Gutkind, J S JS and 6 more authors..  (1991)  A novel c-fgr exon utilized in Epstein-Barr virus-infected B lymphocytes but not in normal monocytes..  Molecular and cellular biology,      [PMID:1847500]
220. Isacchi, A A, Bergonzoni, L L and Sarmientos, P P..  (1990)  Complete sequence of a human receptor for acidic and basic fibroblast growth factors..  Nucleic acids research,    (11):   [PMID:2159626]
221. Itoh, N N, Terachi, T T, Ohta, M M and Seo, M K MK..  (1990)  The complete amino acid sequence of the shorter form of human basic fibroblast growth factor receptor deduced from its cDNA..  Biochemical and biophysical research communications,    (15):   [PMID:2162671]
222. Johnson, D E DE, Lee, P L PL, Lu, J J and Williams, L T LT..  (1990)  Diverse forms of a receptor for acidic and basic fibroblast growth factors..  Molecular and cellular biology,      [PMID:2167437]
223. Sorokin, A A, Mohammadi, M M, Huang, J J and Schlessinger, J J..  (1994)  Internalization of fibroblast growth factor receptor is inhibited by a point mutation at tyrosine 766..  The Journal of biological chemistry,    (24):   [PMID:7516330]
224. Muenke, M M and 9 more authors..  (1994)  A common mutation in the fibroblast growth factor receptor 1 gene in Pfeiffer syndrome..  Nature genetics,      [PMID:7874169]
225. Rusnati, M M and 7 more authors..  (1994)  Distinct role of 2-O-, N-, and 6-O-sulfate groups of heparin in the formation of the ternary complex with basic fibroblast growth factor and soluble FGF receptor-1..  Biochemical and biophysical research communications,    (30):   [PMID:8074689]
226. Mohammadi, M M and 5 more authors..  (1996)  Identification of six novel autophosphorylation sites on fibroblast growth factor receptor 1 and elucidation of their importance in receptor activation and signal transduction..  Molecular and cellular biology,      [PMID:8622701]
227. DiGabriele, A D AD and 6 more authors..  (1998)  Structure of a heparin-linked biologically active dimer of fibroblast growth factor..  Nature,    (25):   [PMID:9655399]
228. Reiter, A A and 10 more authors..  (1998)  Consistent fusion of ZNF198 to the fibroblast growth factor receptor-1 in the t(8;13)(p11;q12) myeloproliferative syndrome..  Blood,    (1):   [PMID:9716603]
229. Wang, F F and 6 more authors..  (1999)  Common and specific determinants for fibroblast growth factors in the ectodomain of the receptor kinase complex..  Biochemistry,    (5):   [PMID:9890894]
230. Popovici, C C and 6 more authors..  (1999)  The t(6;8)(q27;p11) translocation in a stem cell myeloproliferative disorder fuses a novel gene, FOP, to fibroblast growth factor receptor 1..  Blood,    (15):   [PMID:9949182]
231. Wang, J J and 8 more authors..  (1999)  Grb10, a positive, stimulatory signaling adapter in platelet-derived growth factor BB-, insulin-like growth factor I-, and insulin-mediated mitogenesis..  Molecular and cellular biology,      [PMID:10454568]
232. Guasch, G G and 6 more authors..  (2000)  FGFR1 is fused to the centrosome-associated protein CEP110 in the 8p12 stem cell myeloproliferative disorder with t(8;9)(p12;q33)..  Blood,    (1):   [PMID:10688839]
233. Plotnikov, A N AN, Hubbard, S R SR, Schlessinger, J J and Mohammadi, M M..  (2000)  Crystal structures of two FGF-FGFR complexes reveal the determinants of ligand-receptor specificity..  Cell,    (12):   [PMID:10830168]
234. Roscioli, T T and 6 more authors..  (2000)  Clinical findings in a patient with FGFR1 P252R mutation and comparison with the literature..  American journal of medical genetics,    (3):   [PMID:10861678]
235. Sher, I I and 7 more authors..  (2000)  Identification of residues important both for primary receptor binding and specificity in fibroblast growth factor-7..  The Journal of biological chemistry,    (10):   [PMID:10950949]
236. Schlessinger, J J and 7 more authors..  (2000)  Crystal structure of a ternary FGF-FGFR-heparin complex reveals a dual role for heparin in FGFR binding and dimerization..  Molecular cell,      [PMID:11030354]
237. Matsubara A, Yasumoto H and Usui T..  (1999)  Hormone Refractory Prostate Cancer and Fibroblast Growth Factor Receptor..  Breast cancer (Tokyo, Japan),    (25):   [PMID:11091737]
238. Kress, W W, Petersen, B B, Collmann, H H and Grimm, T T..  (2000)  An unusual FGFR1 mutation (fibroblast growth factor receptor 1 mutation) in a girl with non-syndromic trigonocephaly..  Cytogenetics and cell genetics,      [PMID:11173846]
239. Ong, S H SH and 5 more authors..  (2001)  Stimulation of phosphatidylinositol 3-kinase by fibroblast growth factor receptors is mediated by coordinated recruitment of multiple docking proteins..  Proceedings of the National Academy of Sciences of the United States of America,    (22):   [PMID:11353842]
240. Groth, Casper C and Lardelli, Michael M..  (2002)  The structure and function of vertebrate fibroblast growth factor receptor 1..  The International journal of developmental biology,      [PMID:12141425]
241. Cross, Michael J MJ and 6 more authors..  (2002)  The Shb adaptor protein binds to tyrosine 766 in the FGFR-1 and regulates the Ras/MEK/MAPK pathway via FRS2 phosphorylation in endothelial cells..  Molecular biology of the cell,      [PMID:12181353]
242. Dodé, Catherine C and 29 more authors..  (2003)  Loss-of-function mutations in FGFR1 cause autosomal dominant Kallmann syndrome..  Nature genetics,      [PMID:12627230]
243. Sato, Naoko N and 18 more authors..  (2004)  Clinical assessment and mutation analysis of Kallmann syndrome 1 (KAL1) and fibroblast growth factor receptor 1 (FGFR1, or KAL2) in five families and 18 sporadic patients..  The Journal of clinical endocrinology and metabolism,      [PMID:15001591]
244. Grand, Effie K EK and 6 more authors..  (2004)  Identification of a novel gene, FGFR1OP2, fused to FGFR1 in 8p11 myeloproliferative syndrome..  Genes, chromosomes & cancer,      [PMID:15034873]
245. Ibrahimi, Omar A OA, Zhang, Fuming F, Hrstka, Sybil C Lang SC, Mohammadi, Moosa M and Linhardt, Robert J RJ..  (2004)  Kinetic model for FGF, FGFR, and proteoglycan signal transduction complex assembly..  Biochemistry,    (27):   [PMID:15096041]
246. Hu, Yafang Y and 5 more authors..  (2004)  90-kDa ribosomal S6 kinase is a direct target for the nuclear fibroblast growth factor receptor 1 (FGFR1): role in FGFR1 signaling..  The Journal of biological chemistry,    (9):   [PMID:15117958]
247. Albuisson, Juliette J and 13 more authors..  (2005)  Kallmann syndrome: 14 novel mutations in KAL1 and FGFR1 (KAL2)..  Human mutation,      [PMID:15605412]
248. White, Kenneth E KE and 14 more authors..  (2005)  Mutations that cause osteoglophonic dysplasia define novel roles for FGFR1 in bone elongation..  American journal of human genetics,      [PMID:15625620]
249. Sato, Naoko N and 5 more authors..  (2005)  Gonadotrophin therapy in Kallmann syndrome caused by heterozygous mutations of the gene for fibroblast growth factor receptor 1: report of three families: case report..  Human reproduction (Oxford, England),      [PMID:15845591]
250. Eswarakumar, V P VP, Lax, I I and Schlessinger, J J..  (2005)  Cellular signaling by fibroblast growth factor receptors..  Cytokine & growth factor reviews,      [PMID:15863030]
251. Liu, Tao T and 6 more authors..  ()  Human plasma N-glycoproteome analysis by immunoaffinity subtraction, hydrazide chemistry, and mass spectrometry..  Journal of proteome research,      [PMID:16335952]
252. Nusbaum, Chad C and 75 more authors..  (2006)  DNA sequence and analysis of human chromosome 8..  Nature,    (19):   [PMID:16421571]
253. Farrow, Emily G EG and 7 more authors..  (2006)  Extended mutational analyses of FGFR1 in osteoglophonic dysplasia..  American journal of medical genetics. Part A,    (1):   [PMID:16470795]
254. Carlomagno, Francesca F and 6 more authors..  (2006)  BAY 43-9006 inhibition of oncogenic RET mutants..  Journal of the National Cancer Institute,    (1):   [PMID:16507829]
255. Zhang, Xiuqin X and 5 more authors..  (2006)  Receptor specificity of the fibroblast growth factor family. The complete mammalian FGF family..  The Journal of biological chemistry,    (9):   [PMID:16597617]
256. Pitteloud, Nelly N and 14 more authors..  (2006)  Mutations in fibroblast growth factor receptor 1 cause both Kallmann syndrome and normosmic idiopathic hypogonadotropic hypogonadism..  Proceedings of the National Academy of Sciences of the United States of America,    (18):   [PMID:16606836]
257. Zenaty, Delphine D and 6 more authors..  (2006)  Paediatric phenotype of Kallmann syndrome due to mutations of fibroblast growth factor receptor 1 (FGFR1)..  Molecular and cellular endocrinology,    (25):   [PMID:16757108]
258. Pitteloud, Nelly N and 14 more authors..  (2006)  Mutations in fibroblast growth factor receptor 1 cause Kallmann syndrome with a wide spectrum of reproductive phenotypes..  Molecular and cellular endocrinology,    (25):   [PMID:16764984]
259. Trarbach, Ericka Barbosa EB and 7 more authors..  (2006)  Novel fibroblast growth factor receptor 1 mutations in patients with congenital hypogonadotropic hypogonadism with and without anosmia..  The Journal of clinical endocrinology and metabolism,      [PMID:16882753]
260. Gu, Ting-Lei TL and 11 more authors..  (2006)  Phosphotyrosine profiling identifies the KG-1 cell line as a model for the study of FGFR1 fusions in acute myeloid leukemia..  Blood,    (15):   [PMID:16946300]
261. Dodé, Catherine C and 18 more authors..  (2007)  Novel FGFR1 sequence variants in Kallmann syndrome, and genetic evidence that the FGFR1c isoform is required in olfactory bulb and palate morphogenesis..  Human mutation,      [PMID:17154279]
262. Dong, Shaozhong S and 8 more authors..  (2007)  14-3-3 Integrates prosurvival signals mediated by the AKT and MAPK pathways in ZNF198-FGFR1-transformed hematopoietic cells..  Blood,    (1):   [PMID:17389761]
263. Matsui, Junji J and 7 more authors..  (2008)  E7080, a novel inhibitor that targets multiple kinases, has potent antitumor activities against stem cell factor producing human small cell lung cancer H146, based on angiogenesis inhibition..  International journal of cancer,    (1):   [PMID:17943726]
264. Mori, Seiji S and 10 more authors..  (2008)  Direct binding of integrin alphavbeta3 to FGF1 plays a role in FGF1 signaling..  The Journal of biological chemistry,    (27):   [PMID:18441324]
265. Haugsten, Ellen Margrethe EM, Malecki, Jedrzej J, Bjørklund, Sunniva Maria Stordal SM, Olsnes, Sjur S and Wesche, Jørgen J..  (2008)  Ubiquitination of fibroblast growth factor receptor 1 is required for its intracellular sorting but not for its endocytosis..  Molecular biology of the cell,      [PMID:18480409]
266. Sardon, Teresa T, Cottin, Thomas T, Xu, Jing J, Giannis, Athanassios A and Vernos, Isabelle I..  (2009)  Development and biological evaluation of a novel aurora A kinase inhibitor..  Chembiochem : a European journal of chemical biology,    (13):   [PMID:19199284]
267. Lew, Erin D ED, Furdui, Cristina M CM, Anderson, Karen S KS and Schlessinger, Joseph J..  (2009)  The precise sequence of FGF receptor autophosphorylation is kinetically driven and is disrupted by oncogenic mutations..  Science signaling,    (17):   [PMID:19224897]
268. Bae, Jae Hyun JH and 5 more authors..  (2009)  The selectivity of receptor tyrosine kinase signaling is controlled by a secondary SH2 domain binding site..  Cell,    (7):   [PMID:19665973]
269. Hu, Youli Y and 7 more authors..  (2009)  Novel mechanisms of fibroblast growth factor receptor 1 regulation by extracellular matrix protein anosmin-1..  The Journal of biological chemistry,    (23):   [PMID:19696444]
270. Raivio, Taneli T and 17 more authors..  (2009)  Impaired fibroblast growth factor receptor 1 signaling as a cause of normosmic idiopathic hypogonadotropic hypogonadism..  The Journal of clinical endocrinology and metabolism,      [PMID:19820032]
271. Goetz, Regina R and 11 more authors..  (2010)  Isolated C-terminal tail of FGF23 alleviates hypophosphatemia by inhibiting FGF23-FGFR-Klotho complex formation..  Proceedings of the National Academy of Sciences of the United States of America,    (5):   [PMID:19966287]
272. Hu, Youli Y and Bouloux, Pierre-Marc PM..  (2010)  Novel insights in FGFR1 regulation: lessons from Kallmann syndrome..  Trends in endocrinology and metabolism: TEM,      [PMID:20117945]
273. Bae, Jae Hyun JH and 5 more authors..  (2010)  Asymmetric receptor contact is required for tyrosine autophosphorylation of fibroblast growth factor receptor in living cells..  Proceedings of the National Academy of Sciences of the United States of America,    (16):   [PMID:20133753]
274. Miura, Kiyonori K and 6 more authors..  (2010)  A case of Kallmann syndrome carrying a missense mutation in alternatively spliced exon 8A encoding the immunoglobulin-like domain IIIb of fibroblast growth factor receptor 1..  Human reproduction (Oxford, England),      [PMID:20139426]
275. Tornberg, Janne J and 15 more authors..  (2011)  Heparan sulfate 6-O-sulfotransferase 1, a gene involved in extracellular sugar modifications, is mutated in patients with idiopathic hypogonadotrophic hypogonadism..  Proceedings of the National Academy of Sciences of the United States of America,    (12):   [PMID:21700882]
276. Persaud, Avinash A and 8 more authors..  (2011)  Nedd4-1 binds and ubiquitylates activated FGFR1 to control its endocytosis and function..  The EMBO journal,    (15):   [PMID:21765395]
277. Hanchate, Naresh Kumar NK and 23 more authors..  (2012)  SEMA3A, a gene involved in axonal pathfinding, is mutated in patients with Kallmann syndrome..  PLoS genetics,      [PMID:22927827]
278. Gervais, C C and 9 more authors..  (2013)  A translocation t(2;8)(q12;p11) fuses FGFR1 to a novel partner gene, RANBP2/NUP358, in a myeloproliferative/myelodysplastic neoplasm..  Leukemia,      [PMID:23041776]
279. Gozgit, Joseph M JM and 9 more authors..  (2013)  Combined targeting of FGFR2 and mTOR by ponatinib and ridaforolimus results in synergistic antitumor activity in FGFR2 mutant endometrial cancer models..  Cancer chemotherapy and pharmacology,      [PMID:23468082]
280. Urich, Robert R and 8 more authors..  (2013)  De novo design of protein kinase inhibitors by in silico identification of hinge region-binding fragments..  ACS chemical biology,    (17):   [PMID:23534475]
281. Ren, Mingqiang M and 8 more authors..  (2013)  Novel FGFR inhibitor ponatinib suppresses the growth of non-small cell lung cancer cells overexpressing FGFR1..  Oncology reports,      [PMID:23563700]
282. Miraoui, Hichem H and 28 more authors..  (2013)  Mutations in FGF17, IL17RD, DUSP6, SPRY4, and FLRT3 are identified in individuals with congenital hypogonadotropic hypogonadism..  American journal of human genetics,    (2):   [PMID:23643382]
283. Simonis, Nicolas N and 15 more authors..  (2013)  FGFR1 mutations cause Hartsfield syndrome, the unique association of holoprosencephaly and ectrodactyly..  Journal of medical genetics,      [PMID:23812909]
284. Dhamija, Radhika R and 6 more authors..  (2014)  Novel de novo heterozygous FGFR1 mutation in two siblings with Hartsfield syndrome: a case of gonadal mosaicism..  American journal of medical genetics. Part A,      [PMID:24888332]
285. Marcos, Séverine S and 25 more authors..  (2014)  The prevalence of CHD7 missense versus truncating mutations is higher in patients with Kallmann syndrome than in typical CHARGE patients..  The Journal of clinical endocrinology and metabolism,      [PMID:25077900]
286. Gonçalves, Catarina C and 8 more authors..  (2015)  Novel FGFR1 mutations in Kallmann syndrome and normosmic idiopathic hypogonadotropic hypogonadism: evidence for the involvement of an alternatively spliced isoform..  Fertility and sterility,      [PMID:26277103]
287. Tabernero, Josep J and 18 more authors..  (2015)  Phase I Dose-Escalation Study of JNJ-42756493, an Oral Pan-Fibroblast Growth Factor Receptor Inhibitor, in Patients With Advanced Solid Tumors..  Journal of clinical oncology : official journal of the American Society of Clinical Oncology,    (20):   [PMID:26324363]
288. Bennett, James T JT and 26 more authors..  (2016)  Mosaic Activating Mutations in FGFR1 Cause Encephalocraniocutaneous Lipomatosis..  American journal of human genetics,    (3):   [PMID:26942290]
289. Wind, Sven and 7 more authors..  (2019)  Clinical Pharmacokinetics and Pharmacodynamics of Nintedanib..  Clinical pharmacokinetics,      [PMID:31016670]

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