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TargetUnclassified

NACHT, LRR and PYD domains-containing protein 3

Matched no rule. Shown as-is rather than assigned a class by guesswork. Values below are reported as measured; because this is not a molecular target, they are not treated as affinities anywhere on this site.

Measurements
5
Compounds
2
Binding constants
0
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

NLRP3_HUMANNLRP3Homo sapiens

NACHT, LRR and PYD domains-containing protein 3

Sensor component of the NLRP3 inflammasome, which mediates inflammasome activation in response to defects in membrane integrity, leading to secretion of inflammatory cytokines IL1B and IL18 and pyroptosis16407889,18403674,18604214,23582325,25686105,27929086,28656979,28847925,30487600,30612879,31086327,31086329,31189953,33231615,34133077,34341353,34512673,36442502,40250624,40450990. In response to pathogens and other damage-associated signals that affect the integrity of membranes, initiates the formation of the inflammasome polymeric complex composed of NLRP3, CASP1 and PYCARD/ASC16407889,18403674,27432880,28847925,31189953,33231615,34133077,34341353,36142182,36442502. Recruitment of pro-caspase-1 (proCASP1) to the NLRP3 inflammasome promotes caspase-1 (CASP1) activation, which subsequently cleaves and activates inflammatory cytokines IL1B and IL18 and gasdermin-D (GSDMD), promoting cytokine secretion and pyroptosis23582325,28847925,31189953,33231615,34133077,34341353. Activation of NLRP3 inflammasome is also required for HMGB1 secretion; stimulating inflammatory responses22801494. Involved in the homeostatic wound healing response to tissue injury, a multistep cascade that guides neutrophil migration to necrotic sites while avoiding collateral damage of healthy tissues. ATP released from necrotic cells triggers activation of NLRP3 inflammasome through P2RX7 signaling leading to neutrophil adhesion to the vascular endothelium close to the injury site (By similarity). Under resting conditions, ADP-bound NLRP3 is autoinhibited35114687. NLRP3 activation stimuli include extracellular ATP, nigericin, reactive oxygen species, crystals of monosodium urate or cholesterol, amyloid-beta fibers, environmental or industrial particles and nanoparticles, such as asbestos, silica, aluminum salts, cytosolic dsRNA, etc16407889,18403674,18604214,19414800,23871209. Almost all stimuli trigger intracellular K(+) efflux (By similarity). These stimuli lead to membrane perturbation and activation of NLRP3 (By similarity). Upon activation, NLRP3 is transported to microtubule organizing center (MTOC), where it is unlocked by NEK7, leading to its relocalization to dispersed trans-Golgi network (dTGN) vesicle membranes and formation of an active inflammasome complex36442502,39173637. Associates with dTGN vesicle membranes by binding to phosphatidylinositol 4-phosphate (PtdIns4P)30487600,34554188. Shows ATPase activity17483456
Independently of inflammasome activation, regulates the differentiation of T helper 2 (Th2) cells and has a role in Th2 cell-dependent asthma and tumor growth (By similarity). During Th2 differentiation, required for optimal IRF4 binding to IL4 promoter and for IRF4-dependent IL4 transcription (By similarity). Binds to the consensus DNA sequence 5'-GRRGGNRGAG-3' (By similarity). May also participate in the transcription of IL5, IL13, GATA3, CCR3, CCR4 and MAF (By similarity)

Quoted from UniProt’s FUNCTION annotation for Q96P20 (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
CASP10.9990.3070.9000.999
TXNIP0.9990.5100.9000.995
MAVS0.9990.5350.9000.983
NEK70.9990.9830.9000.994
AIM20.9990.0000.9000.999
NLRC40.9990.2920.7200.999
PYCARD0.9990.9180.9000.999
NLRP60.9980.0000.9000.985
DHX330.9980.3420.9000.983
NLRP10.9980.0000.9000.986

Where it sits in the cell

UniProt, curated Cytoplasm, cytosol · Inflammasome · Cytoplasm, cytoskeleton, microtubule organizing center · Golgi apparatus membrane · Endoplasmic reticulum · Mitochondrion · Secreted · Nucleus

Expression by cell type

Single cell type RNA, the 6 highest of those the Human Protein Atlas reports for this gene. Transcript, not protein, and a cell type rather than a tissue.

  • monocytes259.6 nCPM
  • Neutrophils173.2 nCPM
  • Microglia66.5 nCPM
  • Macrophages48.1 nCPM
  • cDC28.6 nCPM
  • Monocyte progenitors23.8 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.

  • bone marrow51.5 nTPM

IV · Evidence

Every measurement at this target

Each row links to the ChEMBL assay it came from.

Other measurements 5

Everything else ChEMBL recorded for this compound — percentage inhibition, efficacy, half-life, cytotoxicity. Reported in the assay's own units, which is why no value is converted here.

TargetClassTypeValue (nM)pXOrganismAssay
NACHT, LRR and PYD domains-containing protein 3UnclassifiedInhibition— no normalized value— value does not convert to pXHomo sapiensCHEMBL4620826
NACHT, LRR and PYD domains-containing protein 3UnclassifiedInhibition— no normalized value— value does not convert to pXHomo sapiensCHEMBL4620827
NACHT, LRR and PYD domains-containing protein 3UnclassifiedInhibition— no normalized value— value does not convert to pXHomo sapiensCHEMBL4620828
NACHT, LRR and PYD domains-containing protein 3UnclassifiedActivity— no normalized value— value does not convert to pXHomo sapiensCHEMBL4620829
NACHT, LRR and PYD domains-containing protein 3UnclassifiedInhibition— no normalized value— value does not convert to pXHomo sapiensCHEMBL5393156