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P11362

Fibroblast growth factor receptor 1


Function

Tyrosine-protein kinase that acts as cell-surface receptor for fibroblast growth factors and plays an essential role in the regulation of embryonic development, cell proliferation, differentiation and migration. Required for normal mesoderm patterning and correct axial organization during embryonic development, normal skeletogenesis and normal development of the gonadotropin-releasing hormone (GnRH) neuronal system. Phosphorylates PLCG1, FRS2, GAB1 and SHB. Ligand binding leads to the activation of several signaling cascades. Activation of PLCG1 leads to the production of the cellular signaling molecules diacylglycerol and inositol 1,4,5-trisphosphate. Phosphorylation of FRS2 triggers recruitment of GRB2, GAB1, PIK3R1 and SOS1, and mediates activation of RAS, MAPK1/ERK2, MAPK3/ERK1 and the MAP kinase signaling pathway, as well as of the AKT1 signaling pathway. Promotes phosphorylation of SHC1, STAT1 and PTPN11/SHP2. In the nucleus, enhances RPS6KA1 and CREB1 activity and contributes to the regulation of transcription. FGFR1 signaling is down-regulated by IL17RD/SEF, and by FGFR1 ubiquitination, internalization and degradation.


Database Links

Database Links
UniProt P11362
PDB 1AGW, 1CVS, 1EVT, 1FGI, 1FGK, 1FQ9, 1XR0, 2CR3, 2FGI, 3C4F, 3DPK, 3GQI, 3GQL, 3JS2, 3KRJ, 3KRL, 3KXX, 3KY2, 3OJV, 3RHX, 3TT0, 4F63, 4F64, 4F65, 4NK9, 4NKA, 4NKS
BioGrid 108551
BindingDB P11362
DrugBank DB00039
Guide to PHARMACOLOGY 1808
PharmGKB PA28127
KEGG hsa:2260
BioCyc Not available
Entrez Gene (GeneID) 2260

Chemical Space of the Positive Compounds


Model Performance Metrics

Metric Mean Value Standard Deviation
AUC 0.9481 0.0024
Accuracy 0.8899 0.0047
Sensitivity 0.8496 0.0073
Specificity 0.9251 0.0036
BEDROC 0.9869 0.0033
MCC Threshold 0.492 N/A
MCC 0.795 N/A
F-score Threshold 0.486 N/A
F-score 0.8876 N/A

Downloads

R Model Object

Random Forest model object (.RData)

Download RData

Positive Set

SMILES string + affinity value (.tsv)

Download TSV


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Page generated on: 2014-04-29 14:39:23