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fibroblast growth factor receptor 3

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Target not currently curated in GtoImmuPdb

Target id: 1810

Nomenclature: fibroblast growth factor receptor 3

Abbreviated Name: FGFR3

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

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 1 806 4p16.3 FGFR3 fibroblast growth factor receptor 3
Mouse 1 801 5 17.83 cM Fgfr3 fibroblast growth factor receptor 3
Rat - 800 14q21 Fgfr3 fibroblast growth factor receptor 3
Previous and Unofficial Names Click here for help
achondroplasia, thanatophoric dwarfism | HBGFR | sam3 | Heparin-binding growth factor receptor | ACH | CD333 | CEK2 | JTK4
Database Links Click here for help
Alphafold P22607 (Hs), Q61851 (Mm)
BRENDA 2.7.10.1
CATH/Gene3D 2.60.40.10
ChEMBL Target CHEMBL2742 (Hs), CHEMBL4066 (Mm)
Ensembl Gene ENSG00000068078 (Hs), ENSMUSG00000054252 (Mm), ENSRNOG00000016818 (Rn)
Entrez Gene 2261 (Hs), 14184 (Mm), 84489 (Rn)
Human Protein Atlas ENSG00000068078 (Hs)
KEGG Enzyme 2.7.10.1
KEGG Gene hsa:2261 (Hs), mmu:14184 (Mm), rno:84489 (Rn)
OMIM 134934 (Hs)
Orphanet ORPHA121815 (Hs)
Pharos P22607 (Hs)
RefSeq Nucleotide NM_000142 (Hs), NM_001205270 (Mm), NM_053429 (Rn)
RefSeq Protein NP_000133 (Hs), NP_001156688 (Mm), NP_001156689 (Mm), NP_001192199 (Mm), NP_001156687 (Mm), NP_032036 (Mm), NP_445881 (Rn)
UniProtKB P22607 (Hs), Q61851 (Mm)
Wikipedia FGFR3 (Hs)
Selected 3D Structures Click here for help
Image of receptor 3D structure from RCSB PDB
Description:  FGFR3 in complex with a Fab
PDB Id:  3GRW
Resolution:  2.1Å
Species:  Human
References:  22
Image of receptor 3D structure from RCSB PDB
Description:  Crystal Structure of the 3 Ig form of FGFR3c in complex with FGF1
PDB Id:  1RY7
Resolution:  3.2Å
Species:  Human
References:  18
Enzyme Reaction Click here for help
EC Number: 2.7.10.1
Endogenous ligand (Human)
FGF-3 (FGF3, P11487)
Endogenous ligands (Human)
FGF-1 (FGF1, P05230), FGF-2 (FGF2, P09038), FGF-9 (FGF9, P31371) > FGF-4 (FGF4, P08620), FGF-8 (FGF8, P55075)  [19]

Download all structure-activity data for this target as a CSV file go icon to follow link

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
futibatinib Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 9.3 pIC50 24
⤷ pIC50 9.3 (IC50 5x10-10 M) [24]
infigratinib Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 9.0 pIC50 10
⤷ pIC50 9.0 (IC50 1x10-9 M) [10]
compound 29 [PMID: 36356320] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.6 – 9.3 pIC50 26
⤷ pIC50 9.3 (IC50 5x10-10 M) [26]
Description: Inhibition of WT FGFR3 in vitro.
pIC50 8.6 (IC50 2.7x10-9 M) [26]
Description: Inhibition of FGFR3V555L in vitro.
ASP5878 Small molecule or natural product Hs Inhibition 8.7 pIC50 14
⤷ pIC50 8.7 (IC50 2.1x10-9 M) [14]
erdafitinib Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.5 pIC50 25
⤷ pIC50 8.5 (IC50 3.02x10-9 M) [25]
tinengotinib Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.5 pIC50 31
⤷ pIC50 8.5 (IC50 3.5x10-9 M) [31]
segigratinib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.4 pIC50 21
⤷ pIC50 8.4 (IC50 3.6x10-9 M) [21]
PRN1371 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.4 pIC50 3
⤷ pIC50 8.4 (IC50 4.1x10-9 M) [3]
derazantinib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.4 pIC50 12
⤷ pIC50 8.4 (IC50 4.5x10-9 M) [12]
fexagratinib Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition >8.3 pIC50 2
⤷ pIC50 >8.3 (IC50 <5x10-9 M) [2]
dovitinib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.1 – 8.5 pIC50 23,28
⤷ pIC50 8.1 – 8.5 (IC50 9x10-9 – 3x10-9 M) [23,28]
tasurgratinib Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.3 pIC50 7
⤷ pIC50 8.3 (IC50 5.4x10-9 M) [7]
compound 7 [Nguyen et al., 2023] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.3 pIC50 16
⤷ pIC50 8.3 (IC50 5.6x10-9 M) [16]
fanregratinib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.2 pIC50 27
⤷ pIC50 8.2 (IC50 6x10-9 M) [27]
LY2874455 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.2 pIC50 33
⤷ pIC50 8.2 (IC50 6.4x10-9 M) [33]
zoligratinib Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.7 pIC50 15
⤷ pIC50 7.7 (IC50 2.2x10-8 M) [15]
rogaratinib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.6 pIC50 4
⤷ pIC50 7.6 (IC50 2.48x10-8 M) [4]
MK-2461 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.3 pIC50 20
⤷ pIC50 7.3 (IC50 5x10-8 M) [20]
pemigatinib Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition >7.0 pIC50 32
⤷ pIC50 >7.0 (IC50 <1x10-7 M) [32]
nintedanib Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.0 pIC50 13
⤷ pIC50 7.0 (IC50 1.08x10-7 M) [13]
compound 1d [PMID: 21493067] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.9 pIC50 29
⤷ pIC50 6.9 (IC50 1.15x10-7 M) [29]
BLU-9931 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 6.8 pIC50 11
⤷ pIC50 6.8 (IC50 1.5x10-7 M) [11]
TAK-632 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 6.6 pIC50 17
⤷ pIC50 6.6 (IC50 2.8x10-7 M) [17]
Description: Biochemical enzyme inhibition assay.
DiscoveRx KINOMEscan® screen Click here for help
A screen of 72 inhibitors against 456 human kinases. Quantitative data were derived using DiscoveRx KINOMEscan® platform.
http://www.discoverx.com/services/drug-discovery-development-services/kinase-profiling/kinomescan
Reference: 6,30
Key to terms and symbols Click column headers to sort
Target used in screen: FGFR3
Ligand Sp. Type Action Value Parameter
cediranib Small molecule or natural product Hs Inhibitor Inhibition 7.6 pKd
PD-173955 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.3 pKd
tamatinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 7.3 pKd
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.1 pKd
NVP-TAE684 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.0 pKd
brivanib Small molecule or natural product Hs Inhibitor Inhibition 6.8 pKd
axitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 6.7 pKd
dovitinib Small molecule or natural product Hs Inhibitor Inhibition 6.6 pKd
sunitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 6.5 pKd
fedratinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 6.4 pKd
Target used in screen: FGFR3(G697C)
Ligand Sp. Type Action Value Parameter
cediranib Small molecule or natural product Hs Inhibitor Inhibition 7.5 pKd
PD-173955 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.3 pKd
tamatinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 7.2 pKd
NVP-TAE684 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.9 pKd
brivanib Small molecule or natural product Hs Inhibitor Inhibition 6.8 pKd
axitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 6.7 pKd
KW-2449 Small molecule or natural product Hs Inhibitor Inhibition 6.6 pKd
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.5 pKd
dovitinib Small molecule or natural product Hs Inhibitor Inhibition 6.4 pKd
SU-14813 Small molecule or natural product 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 Click here for help
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.

http://www.millipore.com/techpublications/tech1/pf3036
http://www.reactionbiology.com/webapps/main/pages/kinase.aspx

Reference: 1,8
Key to terms and symbols Click column headers to sort
Target used in screen: FGFR3/FGFR3
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 3.7 2.0 -0.5
Cdk1/2 inhibitor III Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 5.0 3.0 0.0
SU11652 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 12.3 8.0 1.0
dovitinib Small molecule or natural product Hs Inhibitor Inhibition 12.4
PDK1/Akt/Flt dual pathway inhibitor Small molecule or natural product Hs Inhibitor Inhibition 26.7 125.0 132.0
Syk inhibitor Small molecule or natural product Immunopharmacology Ligand Hs Inhibitor Inhibition 33.8 17.0 14.0
PKR inhibitor Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 34.8 19.0 9.0
SB 218078 Small molecule or natural product Hs Inhibitor Inhibition 36.3 82.0 92.0
pazopanib Small molecule or natural product Approved drug Hs Inhibitor Inhibition 39.3
sunitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 39.7
Displaying the top 10 most potent ligands  View all ligands in screen »
Immuno Process Associations
Immuno Process:  Cellular signalling
Immuno Process:  Immune regulation
Immuno Process:  Immune system development
Clinically-Relevant Mutations and Pathophysiology Click here for help
Disease:  Achondroplasia
Disease Ontology: DOID:4480
OMIM: 100800
Orphanet: ORPHA15
Disease:  Bladder cancer
Disease Ontology: DOID:11054
OMIM: 109800
Disease:  Camptodactyly, tall stature, and hearing loss syndrome
Synonyms: Camptodactyly - tall stature - scoliosis - hearing loss [Orphanet: ORPHA85164]
OMIM: 610474
Orphanet: ORPHA85164
Disease:  Cervical cancer
Disease Ontology: DOID:4362
OMIM: 603956
Disease:  Crouzon syndrome with acanthosis nigricans
OMIM: 612247
Orphanet: ORPHA93262
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:  Hypochondroplasia
Disease Ontology: DOID:0080041
OMIM: 146000
Orphanet: ORPHA429
Disease:  Isolated brachycephaly
Orphanet: ORPHA35099
Disease:  Isolated cloverleaf skull syndrome
Orphanet: ORPHA2343
Disease:  Isolated plagiocephaly
Orphanet: ORPHA35098
Disease:  Keratosis, seborrheic
Synonyms: Seborrheic keratosis [Disease Ontology: DOID:6498]
Disease Ontology: DOID:6498
OMIM: 182000
Disease:  Lacrimoauriculodentodigital syndrome
Synonyms: LADD syndrome [Disease Ontology: DOID:0050331]
Disease Ontology: DOID:0050331
OMIM: 149730
Orphanet: ORPHA2363
Disease:  Muenke syndrome
OMIM: 602849
Orphanet: ORPHA53271
Disease:  Myeloma, multiple
Disease Ontology: DOID:9538
OMIM: 254500
References:  5
Disease:  Nevus, epidermal
Disease Ontology: DOID:0050532
OMIM: 162900
Disease:  Saethre-Chotzen syndrome
Disease Ontology: DOID:14768
OMIM: 101400
Orphanet: ORPHA794
Disease:  Severe achondroplasia - developmental delay - acanthosis nigricans
OMIM: 187600
Orphanet: ORPHA85165
Disease:  Testicular germ cell tumor
Synonyms: Seminoma [Disease Ontology: DOID:4440]
Testicular pure germ cell tumor [Disease Ontology: DOID:4087]
Disease Ontology: DOID:4440, DOID:4087
OMIM: 273300
References:  9
Disease:  Thanatophoric dysplasia, type I
Synonyms: Thanatophoric dysplasia [Disease Ontology: DOID:13481]
Disease Ontology: DOID:13481
OMIM: 187600
Orphanet: ORPHA1860
Disease:  Thanatophoric dysplasia, type II
Synonyms: Thanatophoric dysplasia [Disease Ontology: DOID:13481]
Disease Ontology: DOID:13481
OMIM: 187601
Orphanet: ORPHA93274

References

Show »

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2. AstraZeneca. AZD4547. Accessed on 11/09/2014. Modified on 11/09/2014. astrazeneca.com, http://openinnovation.astrazeneca.com/what-we-offer/compound/azd4547/

3. 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]

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8. 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]

9. Goriely A, Hansen RM, Taylor IB, Olesen IA, Jacobsen GK, McGowan SJ, Pfeifer SP, McVean GA, Rajpert-De Meyts E, Wilkie AO. (2009) Activating mutations in FGFR3 and HRAS reveal a shared genetic origin for congenital disorders and testicular tumors. Nat Genet, 41 (11): 1247-52. [PMID:19855393]

10. 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]

11. 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]

12. 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]

13. 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]

14. Kuriwaki I, Kameda M, Iikubo K, Hisamichi H, Kawamoto Y, Kikuchi S, Moritomo H, Terasaka T, Iwai Y, Noda A et al.. (2022) Discovery of ASP5878: Synthesis and structure-activity relationships of pyrimidine derivatives as pan-FGFRs inhibitors with improved metabolic stability and suppressed hERG channel inhibitory activity. Bioorg Med Chem, 59: 116657. [PMID:35219181]

15. 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]

16. Nguyen MH, Ye HF, Xu Y, Truong L, Horsey A, Styduhar ED, Frascella M, Leffet L, Federowicz K, Behshad E et al.. (2023) Discovery of Orally Bioavailable FGFR2/FGFR3 Dual Inhibitors via Structure-Guided Scaffold Repurposing Approach. ACS Medicinal Chemistry Letters, 14 (3): 312–318. DOI: 10.1021/acsmedchemlett.3c00003

17. Okaniwa M, Hirose M, Arita T, Yabuki M, Nakamura A, Takagi T, Kawamoto T, Uchiyama N, Sumita A, Tsutsumi S et al.. (2013) Discovery of a selective kinase inhibitor (TAK-632) targeting pan-RAF inhibition: design, synthesis, and biological evaluation of C-7-substituted 1,3-benzothiazole derivatives. J Med Chem, 56 (16): 6478-94. [PMID:23906342]

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21. Peng X, Hou P, Chen Y, Dai Y, Ji Y, Shen Y, Su Y, Liu B, Wang Y, Sun D et al.. (2019) Preclinical evaluation of 3D185, a novel potent inhibitor of FGFR1/2/3 and CSF-1R, in FGFR-dependent and macrophage-dominant cancer models. J Exp Clin Cancer Res, 38 (1): 372. [PMID:31438996]

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25. 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.

26. Shvartsbart A, Roach JJ, Witten MR, Koblish H, Harris JJ, Covington M, Hess R, Lin L, Frascella M, Truong L et al.. (2022) Discovery of Potent and Selective Inhibitors of Wild-Type and Gatekeeper Mutant Fibroblast Growth Factor Receptor (FGFR) 2/3. J Med Chem, 65 (22): 15433-15442. [PMID:36356320]

27. Su WG, Zhang W, Li J. (2014) Novel pyrimidine and pyridine compounds and their usage. Patent number: WO2014139465A1. Assignee: Hutchison Medipharma Limited. Priority date: 14/03/2014. Publication date: 18/09/2014.

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30. 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]

31. Wu F. (2021) Multi-kinase inhibitor compound, and crystal form and use thereof. Patent number: US10889586B2. Assignee: Nanjing Transthera Biosciences Co Ltd. Priority date: 13/12/2016. Publication date: 12/01/2021.

32. 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.

33. 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]

How to cite this page

Type V RTKs: FGF (fibroblast growth factor) receptor family: fibroblast growth factor receptor 3. Last modified on 14/08/2024. Accessed on 22/01/2025. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1810.