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Target Report Card

Target Name and Classification

Target ID CHEMBL2695
Preferred Name Focal adhesion kinase 1
Synonyms FADK 1 | FAK | FAK1 | FRNK | Focal adhesion kinase 1 | Focal adhesion kinase-related nonkinase | PPP1R71 | PTK2 | Protein phosphatase 1 regulatory subunit 71 | Protein-tyrosine kinase 2 | p125FAK | pp125FAK
Organism Homo sapiens
Species Group No
Protein Target Classification
  • enzyme > kinase > protein kinase > tk protein kinase group > tyrosine protein kinase fak family

Target Components

Component Description Relationship Accession
Focal adhesion kinase 1 SINGLE PROTEIN Q05397

Target Relations

ChEMBL ID Pref Name Target Type
CHEMBL3301389 Focal adhesion kinase 1/vascular endothelial growth factor receptor 3 PROTEIN-PROTEIN INTERACTION

Approved Drugs and Clinical Candidates

ChEMBL ID Name Mechanism of Action Max Phase References
CHEMBL3137331 DEFACTINIB Focal adhesion kinase 1 inhibitor 2 Other PubMed PubMed
CHEMBL1084546 PF-562271 Focal adhesion kinase 1 inhibitor 1 PubMed
CHEMBL3544933 VS-4718 Focal adhesion kinase 1 inhibitor 1 PubMed PubMed
CHEMBL3544961 BI-853520 Focal adhesion kinase 1 inhibitor 1 DOI Other
CHEMBL3544967 GSK-2256098 Focal adhesion kinase 1 inhibitor 1 DOI PubMed
CHEMBL3545051 CEP-37440 Focal adhesion kinase 1 inhibitor 1 DOI PubMed PubMed

Target Associated Bioactivities

Target Associated Assays

Target Ligand Efficiencies

Target Associated Compound Properties

Target Cross References - Gene

Array Express ENSG00000169398
Ensembl ENSG00000169398
GO Cellular Component GO:0001725 (stress fiber)
GO:0005634 (nucleus)
GO:0005737 (cytoplasm)
GO:0005815 (microtubule organizing center)
GO:0005829 (cytosol)
GO:0005856 (cytoskeleton)
GO:0005886 (plasma membrane)
GO:0005925 (focal adhesion)
GO:0005938 (cell cortex)
GO:0016020 (membrane)
GO:0016324 (apical plasma membrane)
GO:0030027 (lamellipodium)
GO:0030054 (cell junction)
GO:0031234 (extrinsic component of cytoplasmic side of plasma membrane)
GO Molecular Function GO:0000166 (nucleotide binding)
GO:0003779 (actin binding)
GO:0004672 (protein kinase activity)
GO:0004713 (protein tyrosine kinase activity)
GO:0004715 (non-membrane spanning protein tyrosine kinase activity)
GO:0004871 (signal transducer activity)
GO:0005088 (Ras guanyl-nucleotide exchange factor activity)
GO:0005102 (receptor binding)
GO:0005515 (protein binding)
GO:0005524 (ATP binding)
GO:0008432 (JUN kinase binding)
GO:0016301 (kinase activity)
GO:0016740 (transferase activity)
GO:0019901 (protein kinase binding)
GO:0042169 (SH2 domain binding)
GO Biological Process GO:0000165 (MAPK cascade)
GO:0000226 (microtubule cytoskeleton organization)
GO:0001525 (angiogenesis)
GO:0001568 (blood vessel development)
GO:0001570 (vasculogenesis)
GO:0001764 (neuron migration)
GO:0001890 (placenta development)
GO:0001932 (regulation of protein phosphorylation)
GO:0001934 (positive regulation of protein phosphorylation)
GO:0003007 (heart morphogenesis)
GO:0006468 (protein phosphorylation)
GO:0006921 (cellular component disassembly involved in execution phase of apoptosis)
GO:0007172 (signal complex assembly)
GO:0007173 (epidermal growth factor receptor signaling pathway)
GO:0007179 (transforming growth factor beta receptor signaling pathway)
GO:0007229 (integrin-mediated signaling pathway)
GO:0007275 (multicellular organism development)
GO:0007411 (axon guidance)
GO:0008284 (positive regulation of cell proliferation)
GO:0008360 (regulation of cell shape)
GO:0009790 (embryo development)
GO:0010594 (regulation of endothelial cell migration)
GO:0010632 (regulation of epithelial cell migration)
GO:0014068 (positive regulation of phosphatidylinositol 3-kinase signaling)
GO:0016310 (phosphorylation)
GO:0018108 (peptidyl-tyrosine phosphorylation)
GO:0021955 (central nervous system neuron axonogenesis)
GO:0022408 (negative regulation of cell-cell adhesion)
GO:0030010 (establishment of cell polarity)
GO:0030198 (extracellular matrix organization)
GO:0030335 (positive regulation of cell migration)
GO:0033628 (regulation of cell adhesion mediated by integrin)
GO:0038007 (netrin-activated signaling pathway)
GO:0038083 (peptidyl-tyrosine autophosphorylation)
GO:0038096 (Fc-gamma receptor signaling pathway involved in phagocytosis)
GO:0040023 (establishment of nucleus localization)
GO:0042127 (regulation of cell proliferation)
GO:0043066 (negative regulation of apoptotic process)
GO:0043087 (regulation of GTPase activity)
GO:0043542 (endothelial cell migration)
GO:0043547 (positive regulation of GTPase activity)
GO:0043552 (positive regulation of phosphatidylinositol 3-kinase activity)
GO:0045087 (innate immune response)
GO:0045667 (regulation of osteoblast differentiation)
GO:0045860 (positive regulation of protein kinase activity)
GO:0046621 (negative regulation of organ growth)
GO:0046777 (protein autophosphorylation)
GO:0048010 (vascular endothelial growth factor receptor signaling pathway)
GO:0048013 (ephrin receptor signaling pathway)
GO:0048870 (cell motility)
GO:0050771 (negative regulation of axonogenesis)
GO:0051493 (regulation of cytoskeleton organization)
GO:0051893 (regulation of focal adhesion assembly)
GO:0051897 (positive regulation of protein kinase B signaling)
GO:0051964 (negative regulation of synapse assembly)
GO:0060396 (growth hormone receptor signaling pathway)
GO:0071560 (cellular response to transforming growth factor beta stimulus)
GO:1900024 (regulation of substrate adhesion-dependent cell spreading)
GO:2000060 (positive regulation of protein ubiquitination involved in ubiquitin-dependent protein catabolic process)
GO:2000811 (negative regulation of anoikis)
Wikipedia PTK2

Target Cross References - Protein

canSAR Q05397
Human Protein Atlas ENSG00000169398
IntAct Q05397
Guide to Pharmacology 2180
Open Targets ENSG00000169398
PharmGKB PA33955
Pharos Q05397 (Tchem)
Reactome R-HSA-111465 (Apoptotic cleavage of cellular proteins.)
R-HSA-2029482 (Regulation of actin dynamics for phagocytic cup formation.)
R-HSA-354192 (Integrin alphaIIb beta3 signaling.)
R-HSA-354194 (GRB2:SOS provides linkage to MAPK signaling for Integrins.)
R-HSA-372708 (p130Cas linkage to MAPK signaling for integrins.)
R-HSA-375165 (NCAM signaling for neurite out-growth.)
R-HSA-391160 (Signal regulatory protein (SIRP) family interactions.)
R-HSA-3928662 (EPHB-mediated forward signaling.)
R-HSA-3928663 (EPHA-mediated growth cone collapse.)
R-HSA-418885 (DCC mediated attractive signaling.)
R-HSA-418886 (Netrin mediated repulsion signals.)
R-HSA-4420097 (VEGFA-VEGFR2 Pathway.)
R-HSA-5663213 (RHO GTPases Activate WASPs and WAVEs.)
R-HSA-5673001 (RAF/MAP kinase cascade.)
UniProt B4E2N6 F5H4S4 J3QT16 Q05397 Q14291 Q8IYN9 Q9UD85

Target Cross References - Domain

InterPro IPR000299 (FERM_domain.)
IPR000719 (Prot_kinase_dom.)
IPR001245 (Ser-Thr/Tyr_kinase_cat_dom.)
IPR005189 (Focal_adhesion_kin_target_dom.)
IPR008266 (Tyr_kinase_AS.)
IPR011009 (Kinase-like_dom.)
IPR011993 (PH_dom-like.)
IPR017441 (Protein_kinase_ATP_BS.)
IPR019748 (FERM_central.)
IPR019749 (Band_41_domain.)
IPR020635 (Tyr_kinase_cat_dom.)
IPR029071 (Ubiquitin-rel_dom.)
Pfam PF00373 (FERM_M)
PF03623 (Focal_AT)
PF07714 (Pkinase_Tyr)

Target Cross References - Structure

PDBe 1K04 1K05 1MP8 1OW6 1OW7 1OW8 2ETM 2IJM 3B71 3BZ3 3PXK 3S9O 4EBV 4EBW 4GU6 4GU9 4I4E 4I4F 4K8A 4K9Y 4KAB 4KAO 4NY0 4Q9S
CREDO 1K04 1K05 1MP8 1OW6 1OW7 1OW8 2ETM 2IJM 3B71 3BZ3 3PXK 3S9O 4EBV 4EBW 4GU6 4GU9 4I4E 4I4F 4K8A 4K9Y 4KAB 4KAO 4NY0 4Q9S