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PsychedeliaDokholyan Laboratory
TargetEnzymes

Tyrosine-protein kinase Fyn

Named enzymes, including the metabolising cytochromes and the monoamine oxidases.

Measurements
16
Compounds
8
Binding constants
7
Median pX
—

I · Identity

What this target is

Its function as UniProt states it, where in a cell the protein is found, and which cell types and tissues transcribe its gene.

Protein

FYN_HUMANFYNHomo sapiens

Tyrosine-protein kinase Fyn

Non-receptor tyrosine-protein kinase that plays a role in many biological processes including regulation of cell growth and survival, cell adhesion, integrin-mediated signaling, cytoskeletal remodeling, cell motility, immune response and axon guidance11536198,15489916,15557120,16387660,20100835,7568038,7822789. Inactive FYN is phosphorylated on its C-terminal tail within the catalytic domain15489916. Following activation by PKA, the protein subsequently associates with PTK2/FAK1, allowing PTK2/FAK1 phosphorylation, activation and targeting to focal adhesions15489916. Involved in the regulation of cell adhesion and motility through phosphorylation of CTNNB1 (beta-catenin) and CTNND1 (delta-catenin)17194753. Regulates cytoskeletal remodeling by phosphorylating several proteins including the actin regulator WAS and the microtubule-associated proteins MAP2 and MAPT14707117,15536091. Promotes cell survival by phosphorylating AGAP2/PIKE-A and preventing its apoptotic cleavage16841086. Participates in signal transduction pathways that regulate the integrity of the glomerular slit diaphragm (an essential part of the glomerular filter of the kidney) by phosphorylating several slit diaphragm components including NPHS1, KIRREL1 and TRPC614761972,18258597,19179337. Plays a role in neural processes by phosphorylating DPYSL2, a multifunctional adapter protein within the central nervous system, ARHGAP32, a regulator for Rho family GTPases implicated in various neural functions, and SNCA, a small pre-synaptic protein11162638,12788081,19652227. Involved in reelin signaling by mediating phosphorylation of DAB1 following reelin (RELN)-binding to its receptor (By similarity). Participates in the downstream signaling pathways that lead to T-cell differentiation and proliferation following T-cell receptor (TCR) stimulation22080863. Phosphorylates PTK2B/PYK2 in response to T-cell receptor activation20028775. Also participates in negative feedback regulation of TCR signaling through phosphorylation of PAG1 and PDCD118056706,32184441. Phosphorylation of PAG1 promotes interaction between PAG1 and CSK and recruitment of CSK to lipid rafts18056706. Phosphorylation of PDCD1 leads to the recruitment of PTPN11/SHP-2 that mediates dephosphorylation of key TCR proximal signaling molecules32184441. CSK maintains LCK and FYN in an inactive form (By similarity). Promotes CD28-induced phosphorylation of VAV111005864. In mast cells, phosphorylates CLNK after activation of immunoglobulin epsilon receptor signaling (By similarity). Can also promote CD244-mediated NK cell activation15713798

Quoted from UniProt’s FUNCTION annotation for P06241 (reviewed). The superscript numbers are UniProt’s own PubMed citations, kept in the sentence and in order, each linking to the paper it names.

What it acts with

STRING’s highest-confidence human functional partners. The combined score mixes several kinds of evidence, so each channel is shown separately — a partner supported by experiment is a different claim from one supported only by text mining, and for a receptor this is where its coupling appears as evidence rather than as assertion.

PartnerCombinedExperimentDatabaseText mining
SRC0.9990.9430.9000.849
SH2D1A0.9990.9770.9000.880
LCK0.9980.2920.9000.981
PTK20.9980.7130.9000.956
CBL0.9980.9300.5000.960
CAV10.9970.5110.9000.944
LYN0.9960.0000.9000.965
GP60.9960.6480.9000.919
DLG40.9960.5350.0000.992
SHC10.9950.3150.9000.932

Where it sits in the cell

  • Plasma membrane
  • Cytosoladditional

Human Protein Atlas, by antibody immunofluorescence in cell lines — a different assay from the expression figures below, which are RNA.

UniProt, curated Cytoplasm · Nucleus · Cell membrane · Perikaryon

Expression by cell type

Single cell type RNA, the 8 highest of those the Human Protein Atlas reports for this gene. Transcript, not protein, and a cell type rather than a tissue.

  • T-cells2,000.5 nCPM
  • NK-cells1,966.4 nCPM
  • Innate lymphoid cells1,307.3 nCPM
  • Podocytes1,092.5 nCPM
  • Oligodendrocytes813.6 nCPM
  • Bergmann glia770.9 nCPM
  • Astrocytes707.1 nCPM
  • Oligodendrocyte progenitor cells609.8 nCPM

II · Anatomy

Where the gene is transcribed

The same two atlases the compound plates use, asked about this gene alone. Brain on the left, peripheral and autonomic tissues on the right.

Brain

cerebral cortex — 94.8 nTPM, from FYNcerebellum — 59.8 nTPM, from FYNhippocampal formation — 89.6 nTPM, from FYNamygdala — 109.0 nTPM, from FYNhypothalamus — 74.9 nTPM, from FYNthalamus — no resolved target expressed herebasal ganglia — 84.3 nTPM, from FYNmedulla oblongata — no resolved target expressed here

basal ganglia: drawn as the caudate nucleus, putamen and globus pallidus.

Measured but not drawn — this anatomogram has no outline for them: midbrain 82.5, spinal cord 71.4, retina 25.2, pituitary gland 21.1.

Body

heart — 38.3 nTPM, from FYNsmooth muscle — 36.0 nTPM, from FYNlung — 58.9 nTPM, from FYNliver — 18.7 nTPM, from FYNkidney — 21.9 nTPM, from FYNstomach — 27.7 nTPM, from FYNduodenum — 15.4 nTPM, from FYNsmall intestine — 43.3 nTPM, from FYNcolon — 30.9 nTPM, from FYNadrenal gland — 10.3 nTPM, from FYNthyroid gland — 42.8 nTPM, from FYNpancreas — 7.4 nTPM, from FYNurinary bladder — 45.5 nTPM, from FYNskeletal muscle — 11.5 nTPM, from FYNspleen — 69.2 nTPM, from FYNsalivary gland — 12.0 nTPM, from FYN
0109 nTPM

Square-root ramp · shared scale across both plates

Shading is transcript level — not affinity, and not affinity combined with expression. Outlined but unshaded organs hold none of FYN transcript above the atlas’s detection threshold. Anatomy from EMBL-EBI Anatomogram (Apache License 2.0); regions identified by Uberon (uberon.org), CC BY 3.0.

Brain · 10

  • amygdala109.0 nTPM
  • cerebral cortex94.8 nTPM
  • hippocampal formation89.6 nTPM
  • basal ganglia84.3 nTPM
  • midbrain82.5 nTPM
  • hypothalamus74.9 nTPM
  • spinal cord71.4 nTPM
  • cerebellum59.8 nTPM
  • retina25.2 nTPM
  • pituitary gland21.1 nTPM

Peripheral and autonomic · 16

  • spleen69.2 nTPM
  • lung58.9 nTPM
  • urinary bladder45.5 nTPM
  • small intestine43.3 nTPM
  • thyroid gland42.8 nTPM
  • heart muscle38.3 nTPM
  • smooth muscle36.0 nTPM
  • colon30.9 nTPM
  • stomach 127.7 nTPM
  • kidney21.9 nTPM
  • liver18.7 nTPM
  • duodenum15.4 nTPM
  • salivary gland12.0 nTPM
  • skeletal muscle11.5 nTPM
  • adrenal gland10.3 nTPM
  • pancreas7.4 nTPM

Transcript is not protein. These are RNA levels for FYN, shaded on √nTPM so that a three-order range stays legible — on a linear ramp every region but the strongest would read as blank, which looks like absence rather than less. A region carrying no shading is one the atlas reports no consensus value for, not one where the gene is silent. And a gene being transcribed somewhere is not evidence that any compound reaches it. Human Protein Atlas, RNA expression, nTPM (normalized transcripts per million), consensus tissue dataset.

IV · Evidence

Every measurement at this target

Each row links to the ChEMBL assay it came from.

Equilibrium binding constants 7

Ki and Kd — a concentration at equilibrium. Directly comparable across rows at the same target.

TargetClassTypeValue (nM)pXOrganismAssay
Tyrosine-protein kinase FynEnzymesKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909204
Tyrosine-protein kinase FynEnzymesKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909204
Tyrosine-protein kinase FynEnzymesKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909204
Tyrosine-protein kinase FynEnzymesKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909204
Tyrosine-protein kinase FynEnzymesKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909204
Tyrosine-protein kinase FynEnzymesKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909204
Tyrosine-protein kinase FynEnzymesKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909204

Functional readouts 9

IC₅₀, EC₅₀, AC₅₀ and potency. Assay-dependent, and not interchangeable with a binding constant.

TargetClassTypeValue (nM)pXOrganismAssay
Tyrosine-protein kinase FynEnzymesIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL680963
Tyrosine-protein kinase FynEnzymesIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909204
Tyrosine-protein kinase FynEnzymesIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5235550
Tyrosine-protein kinase FynEnzymesIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909204
Tyrosine-protein kinase FynEnzymesIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909204
Tyrosine-protein kinase FynEnzymesIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909204
Tyrosine-protein kinase FynEnzymesIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909204
Tyrosine-protein kinase FynEnzymesIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909204
Tyrosine-protein kinase FynEnzymesIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909204
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