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Target Report Card

Target Name and Classification

Target ID CHEMBL4142
Target Type SINGLE PROTEIN
Preferred Name Fibroblast growth factor receptor 2
Synonyms BEK | CD_antigen=CD332 | FGFR-2 | FGFR2 | Fibroblast growth factor receptor 2 | K-sam | KGFR | KGFR | KSAM | Keratinocyte growth factor receptor
Organism Homo sapiens
Species Group No
Protein Target Classification
  • enzyme > kinase > protein kinase > tk protein kinase group > tyrosine protein kinase fgfr family

Target Components

Component Description Relationship Accession
Fibroblast growth factor receptor 2 SINGLE PROTEIN P21802

Target Relations

ChEMBL ID Pref Name Target Type
CHEMBL2111434 VEGF-receptor 2 and Fibroblast growth factor receptor 2 SELECTIVITY GROUP
CHEMBL2095217 Fibroblast growth factor receptor PROTEIN FAMILY

Approved Drugs and Clinical Candidates

ChEMBL ID Name Mechanism of Action Max Phase References
CHEMBL1201821 PALIFERMIN Fibroblast growth factor receptor 2 agonist 4 DailyMed FDA PubMed
CHEMBL1946170 REGORAFENIB Fibroblast growth factor receptor 2 inhibitor 4 Expert
CHEMBL403989 TG100-801 Fibroblast growth factor receptor 2 inhibitor 2 PubMed PubMed PubMed
CHEMBL2220486 LUCITANIB Fibroblast growth factor receptor 2 inhibitor 2 Other PubMed PubMed
CHEMBL1980391 RG-1530 Fibroblast growth factor receptor 2 inhibitor 1 PubMed PubMed

Target Associated Bioactivities

Target Associated Assays

Target Ligand Efficiencies

Target Associated Compound Properties

Target Cross References - Gene

Array Express ENSG00000066468
Ensembl ENSG00000066468
GO Cellular Component GO:0005576 (extracellular region)
GO:0005634 (nucleus)
GO:0005654 (nucleoplasm)
GO:0005737 (cytoplasm)
GO:0005794 (Golgi apparatus)
GO:0005886 (plasma membrane)
GO:0005887 (integral component of plasma membrane)
GO:0005938 (cell cortex)
GO:0009986 (cell surface)
GO:0016020 (membrane)
GO:0016021 (integral component of membrane)
GO:0016023 (cytoplasmic, membrane-bounded vesicle)
GO:0031012 (extracellular matrix)
GO:0031410 (cytoplasmic vesicle)
GO:0043231 (intracellular membrane-bounded organelle)
GO:0060076 (excitatory synapse)
GO Molecular Function GO:0000166 (nucleotide binding)
GO:0004672 (protein kinase activity)
GO:0004713 (protein tyrosine kinase activity)
GO:0004714 (transmembrane receptor protein tyrosine kinase activity)
GO:0005007 (fibroblast growth factor-activated receptor activity)
GO:0005088 (Ras guanyl-nucleotide exchange factor activity)
GO:0005515 (protein binding)
GO:0005524 (ATP binding)
GO:0008201 (heparin binding)
GO:0016301 (kinase activity)
GO:0016303 (1-phosphatidylinositol-3-kinase activity)
GO:0016740 (transferase activity)
GO:0017134 (fibroblast growth factor binding)
GO:0042803 (protein homodimerization activity)
GO:0046934 (phosphatidylinositol-4,5-bisphosphate 3-kinase activity)
GO Biological Process GO:0000122 (negative regulation of transcription from RNA polymerase II promoter)
GO:0000165 (MAPK cascade)
GO:0001525 (angiogenesis)
GO:0001657 (ureteric bud development)
GO:0001701 (in utero embryonic development)
GO:0001837 (epithelial to mesenchymal transition)
GO:0002053 (positive regulation of mesenchymal cell proliferation)
GO:0003148 (outflow tract septum morphogenesis)
GO:0003149 (membranous septum morphogenesis)
GO:0006468 (protein phosphorylation)
GO:0006915 (apoptotic process)
GO:0007267 (cell-cell signaling)
GO:0007409 (axonogenesis)
GO:0008284 (positive regulation of cell proliferation)
GO:0008543 (fibroblast growth factor receptor signaling pathway)
GO:0008589 (regulation of smoothened signaling pathway)
GO:0009791 (post-embryonic development)
GO:0009880 (embryonic pattern specification)
GO:0009887 (organ morphogenesis)
GO:0010453 (regulation of cell fate commitment)
GO:0010518 (positive regulation of phospholipase activity)
GO:0014066 (regulation of phosphatidylinositol 3-kinase signaling)
GO:0016310 (phosphorylation)
GO:0016331 (morphogenesis of embryonic epithelium)
GO:0018108 (peptidyl-tyrosine phosphorylation)
GO:0021769 (orbitofrontal cortex development)
GO:0021847 (ventricular zone neuroblast division)
GO:0021860 (pyramidal neuron development)
GO:0022612 (gland morphogenesis)
GO:0030177 (positive regulation of Wnt signaling pathway)
GO:0030282 (bone mineralization)
GO:0030324 (lung development)
GO:0030855 (epithelial cell differentiation)
GO:0030901 (midbrain development)
GO:0030916 (otic vesicle formation)
GO:0031069 (hair follicle morphogenesis)
GO:0032808 (lacrimal gland development)
GO:0033688 (regulation of osteoblast proliferation)
GO:0035264 (multicellular organism growth)
GO:0035265 (organ growth)
GO:0035602 (fibroblast growth factor receptor signaling pathway involved in negative regulation of apoptotic process in bone marrow)
GO:0035603 (fibroblast growth factor receptor signaling pathway involved in hemopoiesis)
GO:0035604 (fibroblast growth factor receptor signaling pathway involved in positive regulation of cell proliferation in bone marrow)
GO:0035607 (fibroblast growth factor receptor signaling pathway involved in orbitofrontal cortex development)
GO:0036092 (phosphatidylinositol-3-phosphate biosynthetic process)
GO:0040014 (regulation of multicellular organism growth)
GO:0040036 (regulation of fibroblast growth factor receptor signaling pathway)
GO:0042472 (inner ear morphogenesis)
GO:0042476 (odontogenesis)
GO:0043410 (positive regulation of MAPK cascade)
GO:0043547 (positive regulation of GTPase activity)
GO:0045165 (cell fate commitment)
GO:0045667 (regulation of osteoblast differentiation)
GO:0045787 (positive regulation of cell cycle)
GO:0045944 (positive regulation of transcription from RNA polymerase II promoter)
GO:0046777 (protein autophosphorylation)
GO:0046854 (phosphatidylinositol phosphorylation)
GO:0048015 (phosphatidylinositol-mediated signaling)
GO:0048286 (lung alveolus development)
GO:0048333 (mesodermal cell differentiation)
GO:0048557 (embryonic digestive tract morphogenesis)
GO:0048562 (embryonic organ morphogenesis)
GO:0048565 (digestive tract development)
GO:0048568 (embryonic organ development)
GO:0048608 (reproductive structure development)
GO:0048661 (positive regulation of smooth muscle cell proliferation)
GO:0048701 (embryonic cranial skeleton morphogenesis)
GO:0048705 (skeletal system morphogenesis)
GO:0048730 (epidermis morphogenesis)
GO:0048755 (branching morphogenesis of a nerve)
GO:0048762 (mesenchymal cell differentiation)
GO:0050679 (positive regulation of epithelial cell proliferation)
GO:0050680 (negative regulation of epithelial cell proliferation)
GO:0051150 (regulation of smooth muscle cell differentiation)
GO:0051781 (positive regulation of cell division)
GO:0055010 (ventricular cardiac muscle tissue morphogenesis)
GO:0060045 (positive regulation of cardiac muscle cell proliferation)
GO:0060174 (limb bud formation)
GO:0060348 (bone development)
GO:0060349 (bone morphogenesis)
GO:0060442 (branching involved in prostate gland morphogenesis)
GO:0060445 (branching involved in salivary gland morphogenesis)
GO:0060449 (bud elongation involved in lung branching)
GO:0060463 (lung lobe morphogenesis)
GO:0060484 (lung-associated mesenchyme development)
GO:0060501 (positive regulation of epithelial cell proliferation involved in lung morphogenesis)
GO:0060512 (prostate gland morphogenesis)
GO:0060523 (prostate epithelial cord elongation)
GO:0060527 (prostate epithelial cord arborization involved in prostate glandular acinus morphogenesis)
GO:0060529 (squamous basal epithelial stem cell differentiation involved in prostate gland acinus development)
GO:0060595 (fibroblast growth factor receptor signaling pathway involved in mammary gland specification)
GO:0060601 (lateral sprouting from an epithelium)
GO:0060615 (mammary gland bud formation)
GO:0060664 (epithelial cell proliferation involved in salivary gland morphogenesis)
GO:0060667 (branch elongation involved in salivary gland morphogenesis)
GO:0060670 (branching involved in labyrinthine layer morphogenesis)
GO:0060687 (regulation of branching involved in prostate gland morphogenesis)
GO:0060688 (regulation of morphogenesis of a branching structure)
GO:0060915 (mesenchymal cell differentiation involved in lung development)
GO:0060916 (mesenchymal cell proliferation involved in lung development)
GO:0070372 (regulation of ERK1 and ERK2 cascade)
GO:0070374 (positive regulation of ERK1 and ERK2 cascade)
GO:0090263 (positive regulation of canonical Wnt signaling pathway)
Wikipedia Fibroblast_growth_factor_receptor_2

Target Cross References - Protein

canSAR P21802
CGD Lacrimoauriculodentodigital syndrome; Antley-Bixler syndrome without genital anomalies or disordered steroidogenesis; Crouzon syndrome; Jackson-Weiss syndrome; Pfeiffer syndrome; Apert syndrome; Beare-Stevenson cutis gyrata syndrome
Human Protein Atlas ENSG00000066468
IntAct P21802
Guide to Pharmacology 1809
Open Targets ENSG00000066468
PharmGKB PA28128
Pharos P21802 (Tclin)
Reactome R-HSA-109704 (PI3K Cascade.)
R-HSA-1257604 (PIP3 activates AKT signaling.)
R-HSA-190375 (FGFR2c ligand binding and activation.)
R-HSA-190377 (FGFR2b ligand binding and activation.)
R-HSA-2023837 (Signaling by FGFR2 amplification mutants.)
R-HSA-2033519 (Activated point mutants of FGFR2.)
R-HSA-2219530 (Constitutive Signaling by Aberrant PI3K in Cancer.)
R-HSA-5654221 (Phospholipase C-mediated cascade, FGFR2.)
R-HSA-5654695 (PI-3K cascade:FGFR2.)
R-HSA-5654699 (SHC-mediated cascade:FGFR2.)
R-HSA-5654700 (FRS-mediated FGFR2 signaling.)
R-HSA-5654727 (Negative regulation of FGFR2 signaling.)
R-HSA-5655253 (Signaling by FGFR2 in disease.)
R-HSA-5673001 (RAF/MAP kinase cascade.)
R-HSA-6811558 (PI5P, PP2A and IER3 Regulate PI3K/AKT Signaling.)
R-HSA-8851708 (Signaling by FGFR2 IIIa TM.)
R-HSA-8853333 (Signaling by FGFR2 fusions.)
UniProt B4DFC2 E7EVR6 E9PCR0 P18443 P21802 Q01742 Q12922 Q14300 Q14301 Q14302 Q14303 Q14304 Q14305 Q14672 Q14718 Q14719 Q1KHY5 Q86YI4 Q8IXC7 Q96KL9 Q96KM0 Q96KM1 Q96KM2 Q9NZU2 Q9NZU3 Q9UD01 Q9UD02 Q9UIH3 Q9UIH4 Q9UIH5 Q9UIH6 Q9UIH7 Q9UIH8 Q9UM87 Q9UMC6 Q9UNS7 Q9UQH7 Q9UQH8 Q9UQH9 Q9UQI0

Target Cross References - Domain

InterPro IPR000719 (Prot_kinase_dom.)
IPR001245 (Ser-Thr/Tyr_kinase_cat_dom.)
IPR003598 (Ig_sub2.)
IPR003599 (Ig_sub.)
IPR007110 (Ig-like_dom.)
IPR008266 (Tyr_kinase_AS.)
IPR011009 (Kinase-like_dom.)
IPR013098 (Ig_I-set.)
IPR013783 (Ig-like_fold.)
IPR016248 (FGF_rcpt_fam.)
IPR017441 (Protein_kinase_ATP_BS.)
IPR020635 (Tyr_kinase_cat_dom.)
IPR028175 (FGF_rcpt_2.)
Pfam PF07679 (I-set)
PF07714 (Pkinase_Tyr)

Target Cross References - Structure

PDBe 1DJS 1E0O 1EV2 1GJO 1II4 1IIL 1NUN 1OEC 2FDB 2PSQ 2PVF 2PVY 2PWL 2PY3 2PZ5 2PZP 2PZR 2Q0B 3B2T 3CAF 3CLY 3CU1 3DAR 3EUU More...
CREDO 1DJS 1E0O 1EV2 1GJO 1II4 1IIL 1NUN 1OEC 2FDB 2PSQ 2PVF 2PVY 2PWL 2PY3 2PZ5 2PZP 2PZR 2Q0B 3B2T 3CAF 3CLY 3CU1 3DAR 3EUU More...
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