fibroblast growth factor receptor 1 | Type V RTKs: FGF (fibroblast growth factor) receptor family | IUPHAR/BPS Guide to PHARMACOLOGY

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fibroblast growth factor receptor 1

target has curated data in GtoImmuPdb

Target id: 1808

Nomenclature: fibroblast growth factor receptor 1

Abbreviated Name: FGFR1

Family: Type V RTKs: FGF (fibroblast growth factor) receptor family

Annotation status:  image of an orange circle Annotated and awaiting review. Please contact us if you can help with reviewing.  » Email us

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 1 820 8p12 FGFR1 fibroblast growth factor receptor 1
Mouse 1 822 8 Fgfr1 fibroblast growth factor receptor 1
Rat 1 822 16q12.4 Fgfr1 Fibroblast growth factor receptor 1
Previous and Unofficial Names
BFGFR | CD331 | CEK | FLT2 | fms-related tyrosine kinase 2 | Pfeiffer syndrome | basic fibroblast growth factor receptor 1 | FGF receptor-1 | MFR | Eask | Hspy | KAL2 | FLG | N-SAM
Database Links
ChEMBL Target
DrugBank Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
RefSeq Nucleotide
RefSeq Protein
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of the catalytic domain of FGFR1 kinase in complex with ARQ 069
Resolution:  2.01Å
Species:  Human
References:  9
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of the tyrosine kinse domain of fibroblast growth factor receptor 1
Resolution:  2.0Å
Species:  Human
References:  21
Image of receptor 3D structure from RCSB PDB
Description:  FGFR1 in complex with AZD4547.
PDB Id:  4V05
Ligand:  AZD4547
Resolution:  2.57Å
Species:  Human
References:  33
Image of receptor 3D structure from RCSB PDB
Description:  Human FGFR1 kinase in complex with CH5183284 (DEBIO1347).
PDB Id:  5B7V
Ligand:  DEBIO1347
Resolution:  2.15Å
Species:  Human
References:  22
Enzyme Reaction
EC Number:
Endogenous ligands (Human)
FGF-1 (FGF1, P05230), FGF-2 (FGF2, P09038), FGF-4 (FGF4, P08620) > FGF-5 (FGF5, P12034), FGF-6 (FGF6, P10767)  [23]

Download all structure-activity data for this target as a CSV file

Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
brivanib Hs Inhibition 8.3 pKd 8
pKd 8.3 (Kd 5x10-9 M) [8]
rogaratinib Hs Inhibition 7.9 pKi 6
pKi 7.9 (Ki 1.22x10-8 M) [6]
Description: At a high ATP level.
PD166285 Hs Inhibition 7.4 pKi 25
pKi 7.4 (Ki 3.93x10-8 M) [25]
sunitinib Hs Inhibition 6.1 pKi 20
pKi 6.1 (Ki 8.3x10-7 M) [20]
infigratinib Hs Inhibition 9.1 pIC50 11
pIC50 9.1 (IC50 9x10-10 M) [11]
PRN1371 Hs Inhibition 8.8 – 9.2 pIC50 5
pIC50 9.2 (IC50 6x10-10 M) [5]
Description: In a kinase selectivity profiling assay.
pIC50 8.8 (IC50 1.5x10-9 M) [5]
erdafitinib Hs Inhibition 8.9 pIC50 29
pIC50 8.9 (IC50 1.14x10-9 M) [29]
AZD4547 Hs Inhibition >8.3 – 9.1 pIC50 2,19
pIC50 >8.3 – 9.1 (IC50 <5x10-9 – 7x10-10 M) [2,19]
LY2874455 Hs Inhibition 8.6 pIC50 39
pIC50 8.6 (IC50 2.8x10-9 M) [39]
compound 7r [PMID: 26080733] Hs Inhibition 8.5 pIC50 19
pIC50 8.5 (IC50 2.9x10-9 M) [19]
futibatinib Hs Inhibition 8.4 pIC50 28
pIC50 8.4 (IC50 3.6x10-9 M) [28]
derazantinib Hs Inhibition 8.4 pIC50 13
pIC50 8.4 (IC50 4.5x10-9 M) [13]
compound 8i [PMID: 22765894] Hs Inhibition 8.2 – 8.4 pIC50 18,38
pIC50 8.4 (IC50 4x10-9 M) [18]
pIC50 8.2 (IC50 6.2x10-9 M) [38]
compound 8h [PMID: 22765894] Hs Inhibition 8.2 pIC50 18
pIC50 8.2 (IC50 5.7x10-9 M) [18]
lucitanib Hs Inhibition 8.1 pIC50 40
pIC50 8.1 (IC50 7x10-9 M) [40]
compound 2c [PMID: 24900538] Hs Inhibition 8.1 pIC50 34
pIC50 8.1 (IC50 8.7x10-9 M) [34]
DEBIO1347 Hs Inhibition 8.0 pIC50 22
pIC50 8.0 (IC50 9.2x10-9 M) [22]
dovitinib Hs Inhibition 8.0 – 8.1 pIC50 27,32
pIC50 8.0 – 8.1 (IC50 1.1x10-8 – 8x10-9 M) [27,32]
CEP-11981 Hs Inhibition 7.9 pIC50 16
pIC50 7.9 (IC50 1.3x10-8 M) [16]
catequentinib Hs Inhibition 7.7 pIC50 7
pIC50 7.7 (IC50 2x10-8 M) [7]
Description: in vitro activity
pexmetinib Hs Inhibition 7.6 pIC50 3
pIC50 7.6 (IC50 2.8x10-8 M) [3]
surufatinib Hs Inhibition 7.3 pIC50 30
pIC50 7.3 (IC50 5.3x10-8 M) [30]
Description: Using a Transcreener FP technology assay.
MK-2461 Hs Inhibition 7.2 pIC50 24
pIC50 7.2 (IC50 6.5x10-8 M) [24]
nintedanib Hs Inhibition 7.2 pIC50 15
pIC50 7.2 (IC50 6.9x10-8 M) [15]
pazopanib Hs Inhibition 7.1 pIC50 14
pIC50 7.1 (IC50 7.4x10-8 M) [14]
pemigatinib Hs Inhibition >7.0 pIC50 37
pIC50 >7.0 (IC50 <1x10-7 M) [37]
brivanib Hs Inhibition 6.8 pIC50 4
pIC50 6.8 (IC50 1.48x10-7 M) [4]
SU11652 Hs Inhibition 6.8 pIC50 31
pIC50 6.8 (IC50 1.7x10-7 M) [31]
sorafenib Hs Inhibition 6.2 pIC50 35,38
pIC50 6.2 (IC50 5.8x10-7 M) [38]
pIC50 6.2 (IC50 5.8x10-7 M) [35]
BLU-9931 Hs Inhibition 6.2 pIC50 12
pIC50 6.2 (IC50 5.91x10-7 M) [12]
orantinib Hs Inhibition 5.7 pIC50 17
pIC50 5.7 (IC50 1.81x10-6 M) [17]
SU-14813 Hs Inhibition 5.5 pIC50 26
pIC50 5.5 (IC50 3.5x10-6 M) [26]
DiscoveRx KINOMEscan® screen
A screen of 72 inhibitors against 456 human kinases. Quantitative data were derived using DiscoveRx KINOMEscan® platform.
Reference: 8,36

Key to terms and symbols Click column headers to sort
Target used in screen: FGFR1
Ligand Sp. Type Action Value Parameter
tamatinib Hs Inhibitor Inhibition 7.4 pKd
NVP-TAE684 Hs Inhibitor Inhibition 7.3 pKd
cediranib Hs Inhibitor Inhibition 7.3 pKd
PD-173955 Hs Inhibitor Inhibition 7.2 pKd
staurosporine Hs Inhibitor Inhibition 7.1 pKd
brivanib Hs Inhibitor Inhibition 7.0 pKd
dovitinib Hs Inhibitor Inhibition 6.8 pKd
fedratinib Hs Inhibitor Inhibition 6.6 pKd
lestaurtinib Hs Inhibitor Inhibition 6.5 pKd
KW-2449 Hs Inhibitor Inhibition 6.4 pKd
Displaying the top 10 most potent ligands  View all ligands in screen »
EMD Millipore KinaseProfilerTM screen/Reaction Biology Kinase HotspotSM screen
A screen profiling 158 kinase inhibitors (Calbiochem Protein Kinase Inhibitor Library I and II, catalogue numbers 539744 and 539745) for their inhibitory activity at 1µM and 10µM against 234 human recombinant kinases using the EMD Millipore KinaseProfilerTM service.

A screen profiling the inhibitory activity of 178 commercially available kinase inhibitors at 0.5µM against a panel of 300 recombinant protein kinases using the Reaction Biology Corporation Kinase HotspotSM platform.

Reference: 1,10

Key to terms and symbols Click column headers to sort
Target used in screen: FGFR1/FGFR1
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
staurosporine Hs Inhibitor Inhibition 1.7 0.5 -0.5
Cdk1/2 inhibitor III Hs Inhibitor Inhibition 6.6 1.0 -1.0
dovitinib Hs Inhibitor Inhibition 18.2
SU11652 Hs Inhibitor Inhibition 20.3 7.0 1.0
PDK1/Akt/Flt dual pathway inhibitor Hs Inhibitor Inhibition 24.2 113.0 81.0
indirubin derivative E804 Hs Inhibitor Inhibition 27.9 2.0 -1.0
SB 218078 Hs Inhibitor Inhibition 29.1 72.0 41.0
midostaurin Hs Inhibitor Inhibition 36.1 5.0 -4.0
JNJ-7706621 Hs Inhibitor Inhibition 38.2 10.0 0.0
TWS119 Hs Inhibitor Inhibition 39.3 2.0 0.0
Displaying the top 10 most potent ligands  View all ligands in screen »
Immunopharmacology Comments
A FGFR1 isoform (FGFR1(IIIc)) in complex with the Klotho protein (KL; Q9UEF7) forms a high affinity receptor for FGF-23.
In the choroid plexus (the interface between the brain and immune system) Klotho enhances FGF23 signalling and activation of the NLRP3 inflammasome in resident macrophages, in a system that regulates the level of immune system activation at the blood-brain barrier. Experimental evidence from mice suggests that age-related decline of Klotho in the choroid plexus may be part of the mechanism responisble for "inflammaging", the progressive systemic increase in brain inflammation that is believed to contribute to neurodegeneration in old age [41].
Immuno Process Associations
Immuno Process:  Cytokine production & signalling
GO Annotations:  Associated to 1 GO processes, IEA only
click arrow to show/hide IEA associations
GO:0090272 negative regulation of fibroblast growth factor production IEA
Clinically-Relevant Mutations and Pathophysiology
Disease:  Giant cell glioblastoma
Synonyms: Glioma susceptibility 1; GLM1 [OMIM: 137800]
Disease Ontology: DOID:3074
OMIM: 137800
Orphanet: ORPHA251579
Disease:  Gliosarcoma
Disease Ontology: DOID:3071
Orphanet: ORPHA251576
Disease:  Hartsfield syndrome
OMIM: 615465
Orphanet: ORPHA2117
Disease:  Hypogonadotropic hypogonadism 2 with or without anosmia; HH2
Synonyms: Kallmann syndrome [Orphanet: ORPHA478] [Disease Ontology: DOID:3614]
Normosmic congenital hypogonadotropic hypogonadism [Orphanet: ORPHA432]
Disease Ontology: DOID:3614
OMIM: 147950
Orphanet: ORPHA432, ORPHA478
Disease:  Jackson-Weiss syndrome
Synonyms: Craniosynostosis - midfacial hypoplasia - foot abnormalities
OMIM: 123150
Orphanet: ORPHA1540
Disease:  Myeloid neoplasm associated with FGFR1 rearrangement
Orphanet: ORPHA168953
Disease:  Oligodontia
Orphanet: ORPHA99798
Disease:  Osteoglophonic dysplasia
Synonyms: Osteoglophonic dwarfism [Orphanet: ORPHA2645]
OMIM: 166250
Orphanet: ORPHA2645
Disease:  Pfeiffer syndrome type 1
Synonyms: Pfeiffer syndrome [Disease Ontology: DOID:14705]
Disease Ontology: DOID:14705
OMIM: 101600
Orphanet: ORPHA93258
Disease:  Pilocytic astrocytoma
Disease Ontology: DOID:4851
Orphanet: ORPHA251612
Disease:  Septo-optic dysplasia
OMIM: 182230
Orphanet: ORPHA3157
Disease:  Trigonocephaly 1; TRIGNO1
Synonyms: Isolated trigonocephaly [Orphanet: ORPHA3366]
Metopic craniosynostosis
OMIM: 190440
Orphanet: ORPHA3366


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1. Anastassiadis T, Deacon SW, Devarajan K, Ma H, Peterson JR. (2011) Comprehensive assay of kinase catalytic activity reveals features of kinase inhibitor selectivity. Nat. Biotechnol., 29 (11): 1039-45. [PMID:22037377]

2. AstraZeneca. AZD4547. Accessed on 11/09/2014. Modified on 11/09/2014.,

3. 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]

4. Bhide RS, Cai ZW, Zhang YZ, Qian L, Wei D, Barbosa S, Lombardo LJ, Borzilleri RM, Zheng X, Wu LI et al.. (2006) Discovery and preclinical studies of (R)-1-(4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5- methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy)propan- 2-ol (BMS-540215), an in vivo active potent VEGFR-2 inhibitor. J. Med. Chem., 49 (7): 2143-6. [PMID:16570908]

5. 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]

6. Brohm D, Heroult M, Collin M-P, Hübsch W, Lobell M, Lustig K, Grünewald S, Bömer U, Voehringer V. (2013) Disubstituted benzothienyl-pyrrolotriazines and their use as FGFR kinase inhibitors. Patent number: WO2013087578. Assignee: Bayer Intellectual Property Gmbh. Priority date: 15/12/2011. Publication date: 20/06/2013.

7. Chen GP. (2008) Spiro substituted compounds as angiogenesis inhibitors. Patent number: WO2008112407 A1. Assignee: Advenchen Laboratories, Llc. Priority date: 14/03/2007. Publication date: 18/09/2008.

8. Davis MI, Hunt JP, Herrgard S, Ciceri P, Wodicka LM, Pallares G, Hocker M, Treiber DK, Zarrinkar PP. (2011) Comprehensive analysis of kinase inhibitor selectivity. Nat. Biotechnol., 29 (11): 1046-51. [PMID:22037378]

9. Eathiraj S, Palma R, Hirschi M, Volckova E, Nakuci E, Castro J, Chen CR, Chan TC, France DS, Ashwell MA. (2011) A novel mode of protein kinase inhibition exploiting hydrophobic motifs of autoinhibited kinases: discovery of ATP-independent inhibitors of fibroblast growth factor receptor. J. Biol. Chem., 286 (23): 20677-87. [PMID:21454610]

10. Gao Y, Davies SP, Augustin M, Woodward A, Patel UA, Kovelman R, Harvey KJ. (2013) A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. Biochem. J., 451 (2): 313-28. [PMID:23398362]

11. 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]

12. 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]

13. 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]

14. Harris PA, Boloor A, Cheung M, Kumar R, Crosby RM, Davis-Ward RG, Epperly AH, Hinkle KW, Hunter 3rd RN, Johnson JH et al.. (2008) Discovery of 5-[[4-[(2,3-dimethyl-2H-indazol-6-yl)methylamino]-2-pyrimidinyl]amino]-2-methyl-benzenesulfonamide (Pazopanib), a novel and potent vascular endothelial growth factor receptor inhibitor. J. Med. Chem., 51 (15): 4632-40. [PMID:18620382]

15. Hilberg F, Roth GJ, Krssak M, Kautschitsch S, Sommergruber W, Tontsch-Grunt U, Garin-Chesa P, Bader G, Zoephel A, Quant J et al.. (2008) BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. Cancer Res., 68 (12): 4774-82. [PMID:18559524]

16. 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]

17. Kammasud N, Boonyarat C, Sanphanya K, Utsintong M, Tsunoda S, Sakurai H, Saiki I, André I, Grierson DS, Vajragupta O. (2009) 5-Substituted pyrido[2,3-d]pyrimidine, an inhibitor against three receptor tyrosine kinases. Bioorg. Med. Chem. Lett., 19 (3): 745-50. [PMID:19110422]

18. Kim MH, Tsuhako AL, Co EW, Aftab DT, Bentzien F, Chen J, Cheng W, Engst S, Goon L, Klein RR et al.. (2012) The design, synthesis, and biological evaluation of potent receptor tyrosine kinase inhibitors. Bioorg. Med. Chem. Lett., 22 (15): 4979-85. [PMID:22765894]

19. Liu J, Peng X, Dai Y, Zhang W, Ren S, Ai J, Geng M, Li Y. (2015) Design, synthesis and biological evaluation of novel FGFR inhibitors bearing an indazole scaffold. Org. Biomol. Chem., 13 (28): 7643-54. [PMID:26080733]

20. 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]

21. 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]

22. Nakanishi Y, Akiyama N, Tsukaguchi T, Fujii T, Sakata K, Sase H, Isobe T, Morikami K, Shindoh H, Mio T et al.. (2014) The fibroblast growth factor receptor genetic status as a potential predictor of the sensitivity to CH5183284/Debio 1347, a novel selective FGFR inhibitor. Mol. Cancer Ther., 13 (11): 2547-58. [PMID:25169980]

23. Ornitz DM, Xu J, Colvin JS, McEwen DG, MacArthur CA, Coulier F, Gao G, Goldfarb M. (1996) Receptor specificity of the fibroblast growth factor family. J. Biol. Chem., 271 (25): 15292-7. [PMID:8663044]

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. 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]

26. Patyna S, Laird AD, Mendel DB, O'farrell AM, Liang C, Guan H, Vojkovsky T, Vasile S, Wang X, Chen J et al.. (2006) SU14813: a novel multiple receptor tyrosine kinase inhibitor with potent antiangiogenic and antitumor activity. Mol. Cancer Ther., 5 (7): 1774-82. [PMID:16891463]

27. Renhowe PA, Pecchi S, Shafer CM, Machajewski TD, Jazan EM, Taylor C, Antonios-McCrea W, McBride CM, Frazier K, Wiesmann M et al.. (2009) Design, structure-activity relationships and in vivo characterization of 4-amino-3-benzimidazol-2-ylhydroquinolin-2-ones: a novel class of receptor tyrosine kinase inhibitors. J. Med. Chem., 52 (2): 278-92. [PMID:19113866]

28. Sagara T, Ito S, Otsuki S, Sootome H. (2013) 3,5-disubstituted alkynylbenzene compound and salt thereof. Patent number: WO2013108809. Assignee: Taiho Pharmaceutical Co., Ltd.. Priority date: 19/01/2012. Publication date: 25/07/2013.

29. Saxty G, Murray CW, Berdini V, Besong GE, Hamlett CCF, Johnson CN, Woodhead SJ, Reader M, Rees DC, Mevellec LA et al.. (2011) Pyrazolyl quinazoline kinase inhibitors. Patent number: WO2011135376 A1. Assignee: Astex Therapeutics Limited. Priority date: 30/04/2010. Publication date: 03/11/2011.

30. Su W-G, Zhang W, Jia H, Cui Y, Ren Y, Sai Y, Wu Z, Li W, Shao J. (2011) Compound, certain novel forms thereof, pharmaceutical compositions thereof and methods for preparation and use. Patent number: WO2011060746. Assignee: Hutchison Medipharma Limited. Priority date: 23/11/2009. Publication date: 26/05/2011.

31. 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]

32. 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]

33. Tucker JA, Klein T, Breed J, Breeze AL, Overman R, Phillips C, Norman RA. (2014) Structural insights into FGFR kinase isoform selectivity: diverse binding modes of AZD4547 and ponatinib in complex with FGFR1 and FGFR4. Structure, 22 (12): 1764-74. [PMID:25465127]

34. Wang T, Lamb ML, Block MH, Davies AM, Han Y, Hoffmann E, Ioannidis S, Josey JA, Liu ZY, Lyne PD et al.. (2012) Discovery of Disubstituted Imidazo[4,5-b]pyridines and Purines as Potent TrkA Inhibitors. ACS Med Chem Lett, 3 (9): 705-9. [PMID:24900538]

35. 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]

36. Wodicka LM, Ciceri P, Davis MI, Hunt JP, Floyd M, Salerno S, Hua XH, Ford JM, Armstrong RC, Zarrinkar PP et al.. (2010) Activation state-dependent binding of small molecule kinase inhibitors: structural insights from biochemistry. Chem. Biol., 17 (11): 1241-9. [PMID:21095574]

37. Wu L, Zhang C, He C, Sun Y, Lu L, Qian D-Q, Xu M, Zhou J, Yao W. (2014) Substituted tricyclic compounds as FGFR inhibitors. Patent number: WO2014007951. Assignee: Incyte Corporation. Priority date: 13/06/2012. Publication date: 09/01/2014.

38. 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]

39. 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]

40. 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]

41. Zhu L, Stein LR, Kim D, Ho K, Yu GQ, Zhan L, Larsson TE, Mucke L. (2018) Klotho controls the brain-immune system interface in the choroid plexus. Proc. Natl. Acad. Sci. U.S.A., 115 (48): E11388-E11396. [PMID:30413620]

How to cite this page

Type V RTKs: FGF (fibroblast growth factor) receptor family: fibroblast growth factor receptor 1. Last modified on 20/04/2020. Accessed on 13/07/2020. IUPHAR/BPS Guide to PHARMACOLOGY,