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TargetEnzymes

Tyrosine-protein kinase Lck

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

Measurements
18
Compounds
10
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

LCK_HUMANLCKHomo sapiens

Tyrosine-protein kinase Lck

Non-receptor tyrosine-protein kinase that plays an essential role in the selection and maturation of developing T-cells in the thymus and in the function of mature T-cells2470098. Plays a key role in T-cell antigen receptor (TCR)-linked signal transduction pathways2470098. Constitutively associated with the cytoplasmic portions of the CD4 and CD8 surface receptors2470098. Association of the TCR with a peptide antigen-bound MHC complex facilitates the interaction of CD4 and CD8 with MHC class II and class I molecules, respectively, thereby recruiting the associated LCK protein to the vicinity of the TCR-CD3 complex2470098. LCK then phosphorylates tyrosine residues within the immunoreceptor tyrosine-based activation motifs (ITAM) of the cytoplasmic tails of the TCR-gamma chains and CD3 subunits, initiating the TCR-CD3 signaling pathway2470098,40592325. Once stimulated, the TCR recruits the tyrosine kinase ZAP70, that becomes phosphorylated and activated by LCK. Following this, a large number of signaling molecules are recruited, ultimately leading to lymphokine production. LCK also contributes to signaling by other receptor molecules. Associates directly with the cytoplasmic tail of CD2, which leads to hyperphosphorylation and activation of LCK. Also plays a role in the IL2 receptor-linked signaling pathway that controls the T-cell proliferative response. Binding of IL2 to its receptor results in increased activity of LCK. Is expressed at all stages of thymocyte development and is required for the regulation of maturation events that are governed by both pre-TCR and mature alpha beta TCR. Phosphorylates other substrates including RUNX3, PTK2B/PYK2, the microtubule-associated protein MAPT, RHOH or TYROBP. Interacts with FYB227335501

Quoted from UniProt’s FUNCTION annotation for P06239 (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
PTPRC0.9990.8480.9000.993
LCP20.9990.5090.5000.995
CD8A0.9990.9030.9000.998
ZAP700.9990.8290.9000.986
CD40.9990.9810.9000.998
CD280.9980.0000.4000.996
FYN0.9980.2920.9000.981
CD2470.9960.8080.5000.945
VAV10.9880.2920.4000.967
SYK0.9870.7400.5000.901

Where it sits in the cell

  • Golgi apparatus

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

UniProt, curated Cell membrane · Cytoplasm, cytosol

Expression by cell type

Single cell type RNA, the 5 highest of those the Human Protein Atlas reports for this gene. Transcript, not protein, and a cell type rather than a tissue.

  • T-cells256.2 nCPM
  • NK-cells172.2 nCPM
  • Innate lymphoid cells53.6 nCPM
  • Thymocytes52.5 nCPM
  • B-cells24.4 nCPM

Expression by tissue

The tissues this gene is enriched in, by consensus RNA. A tissue absent from this list is one the Atlas does not call specific for this gene, which is not the same as absent from it.

  • lymphoid tissue325.6 nTPM

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.

034 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 LCK 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 · 8

  • spinal cord1.0 nTPM
  • pituitary gland0.6 nTPM
  • midbrain0.4 nTPM
  • hippocampal formation0.3 nTPM
  • hypothalamus0.3 nTPM
  • cerebral cortex0.2 nTPM
  • amygdala0.2 nTPM
  • basal ganglia0.2 nTPM

Peripheral and autonomic · 16

  • spleen33.8 nTPM
  • small intestine18.7 nTPM
  • urinary bladder11.6 nTPM
  • stomach 110.2 nTPM
  • lung9.6 nTPM
  • duodenum6.6 nTPM
  • colon6.1 nTPM
  • salivary gland4.1 nTPM
  • thyroid gland3.4 nTPM
  • liver3.2 nTPM
  • kidney2.2 nTPM
  • adrenal gland1.8 nTPM
  • smooth muscle1.7 nTPM
  • heart muscle1.6 nTPM
  • skeletal muscle0.8 nTPM
  • pancreas0.7 nTPM

Transcript is not protein. These are RNA levels for LCK, 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 LckEnzymesKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909206
Tyrosine-protein kinase LckEnzymesKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909206
Tyrosine-protein kinase LckEnzymesKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909206
Tyrosine-protein kinase LckEnzymesKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909206
Tyrosine-protein kinase LckEnzymesKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909206
Tyrosine-protein kinase LckEnzymesKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909206
Tyrosine-protein kinase LckEnzymesKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909206

Functional readouts 11

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

TargetClassTypeValue (nM)pXOrganismAssay
Tyrosine-protein kinase LckEnzymesIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL872814
Tyrosine-protein kinase LckEnzymesIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5235552
Tyrosine-protein kinase LckEnzymesIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL823217
Tyrosine-protein kinase LckEnzymesIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909206
Tyrosine-protein kinase LckEnzymesIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL823217
Tyrosine-protein kinase LckEnzymesIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909206
Tyrosine-protein kinase LckEnzymesIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909206
Tyrosine-protein kinase LckEnzymesIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909206
Tyrosine-protein kinase LckEnzymesIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909206
Tyrosine-protein kinase LckEnzymesIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909206
Tyrosine-protein kinase LckEnzymesIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909206