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Target Report Card

Target Name and Classification

Target ID CHEMBL3650
Target Type SINGLE PROTEIN
Preferred Name Fibroblast growth factor receptor 1
Synonyms BFGFR | BFGFR | Basic fibroblast growth factor receptor 1 | CD_antigen=CD331 | CEK | FGFBR | FGFR-1 | FGFR1 | FLG | FLT-2 | FLT2 | Fibroblast growth factor receptor 1 | Fms-like tyrosine kinase 2 | HBGFR | N-sam | Proto-oncogene c-Fgr | bFGF-R-1
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 1 SINGLE PROTEIN P11362

Target Relations

ChEMBL ID Pref Name Target Type
CHEMBL2095217 Fibroblast growth factor receptor PROTEIN FAMILY
CHEMBL2111439 VEGF-receptor 2 and Fibroblast growth factor receptor 1 PROTEIN FAMILY

Approved Drugs and Clinical Candidates

ChEMBL ID Name Mechanism of Action Max Phase References
CHEMBL1201733 PAZOPANIB HYDROCHLORIDE Fibroblast growth factor receptor 1 inhibitor 4 DailyMed
CHEMBL1946170 REGORAFENIB Fibroblast growth factor receptor 1 inhibitor 4 Expert
CHEMBL3545251 Sulfatinib Fibroblast growth factor receptor 1 inhibitor 3 ClinicalTrials Other Other
CHEMBL403989 TG100-801 Fibroblast growth factor receptor 1 inhibitor 2 PubMed PubMed PubMed
CHEMBL2220486 LUCITANIB Fibroblast growth factor receptor 1 inhibitor 2 Other PubMed PubMed
CHEMBL1980391 RG-1530 Fibroblast growth factor receptor 1 inhibitor 1 PubMed PubMed
CHEMBL3545196 PD-0166285 Fibroblast growth factor receptor 1 inhibitor 1 PubMed

Target Associated Bioactivities

Target Associated Assays

Target Ligand Efficiencies

Target Associated Compound Properties

Target Cross References - Gene

Array Express ENSG00000077782
Ensembl ENSG00000077782
GO Cellular Component GO:0005576 (extracellular region)
GO:0005634 (nucleus)
GO:0005737 (cytoplasm)
GO:0005829 (cytosol)
GO:0005886 (plasma membrane)
GO:0005887 (integral component of plasma membrane)
GO:0016020 (membrane)
GO:0016021 (integral component of membrane)
GO:0016023 (cytoplasmic, membrane-bounded vesicle)
GO:0031410 (cytoplasmic vesicle)
GO:0043235 (receptor complex)
GO Molecular Function GO:0000166 (nucleotide binding)
GO:0001948 (glycoprotein 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:0032403 (protein complex binding)
GO:0042802 (identical protein binding)
GO:0042803 (protein homodimerization activity)
GO:0046934 (phosphatidylinositol-4,5-bisphosphate 3-kinase activity)
GO:0050839 (cell adhesion molecule binding)
GO Biological Process GO:0000122 (negative regulation of transcription from RNA polymerase II promoter)
GO:0000165 (MAPK cascade)
GO:0001501 (skeletal system development)
GO:0001525 (angiogenesis)
GO:0001657 (ureteric bud development)
GO:0001701 (in utero embryonic development)
GO:0001759 (organ induction)
GO:0001764 (neuron migration)
GO:0002053 (positive regulation of mesenchymal cell proliferation)
GO:0002062 (chondrocyte differentiation)
GO:0006351 (transcription, DNA-templated)
GO:0006355 (regulation of transcription, DNA-templated)
GO:0006468 (protein phosphorylation)
GO:0007420 (brain development)
GO:0007435 (salivary gland morphogenesis)
GO:0007605 (sensory perception of sound)
GO:0008284 (positive regulation of cell proliferation)
GO:0008543 (fibroblast growth factor receptor signaling pathway)
GO:0010468 (regulation of gene expression)
GO:0010518 (positive regulation of phospholipase activity)
GO:0010629 (negative regulation of gene expression)
GO:0010863 (positive regulation of phospholipase C activity)
GO:0010976 (positive regulation of neuron projection development)
GO:0014066 (regulation of phosphatidylinositol 3-kinase signaling)
GO:0014068 (positive regulation of phosphatidylinositol 3-kinase signaling)
GO:0016310 (phosphorylation)
GO:0016477 (cell migration)
GO:0018108 (peptidyl-tyrosine phosphorylation)
GO:0019827 (stem cell population maintenance)
GO:0021769 (orbitofrontal cortex development)
GO:0021837 (motogenic signaling involved in postnatal olfactory bulb interneuron migration)
GO:0021847 (ventricular zone neuroblast division)
GO:0021954 (central nervous system neuron development)
GO:0030324 (lung development)
GO:0030326 (embryonic limb morphogenesis)
GO:0030901 (midbrain development)
GO:0031175 (neuron projection development)
GO:0035607 (fibroblast growth factor receptor signaling pathway involved in orbitofrontal cortex development)
GO:0036092 (phosphatidylinositol-3-phosphate biosynthetic process)
GO:0042127 (regulation of cell proliferation)
GO:0042472 (inner ear morphogenesis)
GO:0042473 (outer ear morphogenesis)
GO:0042474 (middle ear morphogenesis)
GO:0043009 (chordate embryonic development)
GO:0043406 (positive regulation of MAP kinase activity)
GO:0043410 (positive regulation of MAPK cascade)
GO:0043547 (positive regulation of GTPase activity)
GO:0045595 (regulation of cell differentiation)
GO:0045666 (positive regulation of neuron differentiation)
GO:0045668 (negative regulation of osteoblast differentiation)
GO:0045787 (positive regulation of cell cycle)
GO:0046777 (protein autophosphorylation)
GO:0046854 (phosphatidylinositol phosphorylation)
GO:0048015 (phosphatidylinositol-mediated signaling)
GO:0048339 (paraxial mesoderm development)
GO:0048378 (regulation of lateral mesodermal cell fate specification)
GO:0048469 (cell maturation)
GO:0048514 (blood vessel morphogenesis)
GO:0048699 (generation of neurons)
GO:0048705 (skeletal system morphogenesis)
GO:0048762 (mesenchymal cell differentiation)
GO:0051930 (regulation of sensory perception of pain)
GO:0060045 (positive regulation of cardiac muscle cell proliferation)
GO:0060117 (auditory receptor cell development)
GO:0060445 (branching involved in salivary gland morphogenesis)
GO:0060484 (lung-associated mesenchyme development)
GO:0060665 (regulation of branching involved in salivary gland morphogenesis by mesenchymal-epithelial signaling)
GO:0072091 (regulation of stem cell proliferation)
GO:0090080 (positive regulation of MAPKKK cascade by fibroblast growth factor receptor signaling pathway)
GO:2000546 (positive regulation of endothelial cell chemotaxis to fibroblast growth factor)
GO:2001239 (regulation of extrinsic apoptotic signaling pathway in absence of ligand)
Wikipedia Fibroblast_growth_factor_receptor_1

Target Cross References - Protein

canSAR P11362
CGD Hypogonadotropic hypogonadism; Kallmann syndrome; Trigonocephaly 1; Jackson-Weiss syndrome; Pfeiffer syndrome
Human Protein Atlas ENSG00000077782
IntAct P11362
Guide to Pharmacology 1808
Open Targets ENSG00000077782
PharmGKB PA28127
Pharos P11362 (Tclin)
Reactome R-HSA-109704 (PI3K Cascade.)
R-HSA-1257604 (PIP3 activates AKT signaling.)
R-HSA-1839120 (Signaling by FGFR1 amplification mutants.)
R-HSA-1839122 (Signaling by activated point mutants of FGFR1.)
R-HSA-190370 (FGFR1b ligand binding and activation.)
R-HSA-190373 (FGFR1c ligand binding and activation.)
R-HSA-190374 (FGFR1c and Klotho ligand binding and activation.)
R-HSA-2219530 (Constitutive Signaling by Aberrant PI3K in Cancer.)
R-HSA-375165 (NCAM signaling for neurite out-growth.)
R-HSA-445144 (Signal transduction by L1.)
R-HSA-5654219 (Phospholipase C-mediated cascade: FGFR1.)
R-HSA-5654687 (Downstream signaling of activated FGFR1.)
R-HSA-5654688 (SHC-mediated cascade:FGFR1.)
R-HSA-5654689 (PI-3K cascade:FGFR1.)
R-HSA-5654693 (FRS-mediated FGFR1 signaling.)
R-HSA-5654726 (Negative regulation of FGFR1 signaling.)
R-HSA-5655302 (Signaling by FGFR1 in disease.)
R-HSA-5673001 (RAF/MAP kinase cascade.)
R-HSA-6811558 (PI5P, PP2A and IER3 Regulate PI3K/AKT Signaling.)
R-HSA-8853336 (Signaling by plasma membrane FGFR1 fusions.)
UniProt A8K6T9 A8K8V5 C1KBH8 P11362 P17049 Q02063 Q02065 Q14306 Q14307 Q53H63 Q59H40 Q5BJG2 Q8N685 Q9UD50 Q9UDF0 Q9UDF1 Q9UDF2

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.)
IPR013151 (Immunoglobulin.)
IPR013783 (Ig-like_fold.)
IPR016248 (FGF_rcpt_fam.)
IPR017441 (Protein_kinase_ATP_BS.)
IPR020635 (Tyr_kinase_cat_dom.)
IPR028174 (FGF_rcpt_1.)
Pfam PF00047 (ig)
PF07679 (I-set)
PF07714 (Pkinase_Tyr)

Target Cross References - Structure

PDBe 1AGW 1CVS 1EVT 1FGI 1FGK 1FQ9 2FGI 3C4F 3DPK 3GQI 3GQL 3JS2 3KRJ 3KRL 3KXX 3KY2 3OJV 3RHX 3TT0 4F63 4F64 4F65 4NK9 4NKA More...
CREDO 1AGW 1CVS 1EVT 1FGI 1FGK 1FQ9 2FGI 3C4F 3DPK 3GQI 3GQL 3JS2 3KRJ 3KRL 3KXX 3KY2 3OJV 3RHX 3TT0 4F63 4F64 4F65 4NK9 4NKA More...
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