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Target Report Card

Target Name and Classification

Target ID CHEMBL249
Preferred Name Neurokinin 1 receptor
Synonyms NK-1 receptor | NK-1R | NK1R | SPR | Substance-P receptor | TAC1R | TACR1 | Tachykinin receptor 1
Organism Homo sapiens
Species Group No
Protein Target Classification
  • membrane receptor > family a g protein-coupled receptor > peptide receptor (family a gpcr) > short peptide receptor (family a gpcr) > neurokinin receptor

Target Components

Component Description Relationship Accession
Substance-P receptor SINGLE PROTEIN P25103

Approved Drugs and Clinical Candidates

ChEMBL ID Name Mechanism of Action Max Phase References
CHEMBL206253 NETUPITANT Neurokinin 1 receptor antagonist 4 FDA
CHEMBL1471 APREPITANT Neurokinin 1 receptor antagonist 4 DailyMed
CHEMBL1201782 FOSAPREPITANT DIMEGLUMINE Neurokinin 1 receptor antagonist 4 DailyMed
CHEMBL3707330 ROLAPITANT HYDROCHLORIDE Neurokinin 1 receptor antagonist 4 DailyMed
CHEMBL1672054 CASOPITANT Neurokinin 1 receptor antagonist 3 PubMed PubMed
CHEMBL105060 DNK333 Neurokinin 1 receptor antagonist 2 PubMed PubMed
CHEMBL522302 VOFOPITANT Neurokinin 1 receptor antagonist 2 PubMed
CHEMBL515966 EZLOPITANT Neurokinin 1 receptor antagonist 2 PubMed
CHEMBL447955 SERLOPITANT Neurokinin 1 receptor antagonist 2 Other PubMed
CHEMBL2104992 VESTIPITANT MESYLATE Neurokinin 1 receptor antagonist 2 PubMed
CHEMBL2105667 ORVEPITANT Neurokinin 1 receptor antagonist 2 PubMed
CHEMBL3544947 BURAPITANT Neurokinin 1 receptor antagonist 2 PubMed
CHEMBL3544984 TRADIPITANT Neurokinin 1 receptor antagonist 2 PubMed
CHEMBL2104927 FIGOPITANT Neurokinin 1 receptor antagonist 1 PubMed PubMed

Target Associated Bioactivities

Target Associated Assays

Target Ligand Efficiencies

Target Associated Compound Properties

Target Cross References - Gene

Array Express ENSG00000115353
Ensembl ENSG00000115353
GO Cellular Component GO:0005737 (cytoplasm)
GO:0005886 (plasma membrane)
GO:0005887 (integral component of plasma membrane)
GO:0009986 (cell surface)
GO:0016020 (membrane)
GO:0016021 (integral component of membrane)
GO:0030425 (dendrite)
GO:0036126 (sperm flagellum)
GO:0044297 (cell body)
GO:0061827 (sperm head)
GO:0071944 (cell periphery)
GO:0097225 (sperm midpiece)
GO Molecular Function GO:0004871 (signal transducer activity)
GO:0004930 (G-protein coupled receptor activity)
GO:0004995 (tachykinin receptor activity)
GO:0005515 (protein binding)
GO:0016496 (substance P receptor activity)
GO Biological Process GO:0002118 (aggressive behavior)
GO:0002526 (acute inflammatory response)
GO:0002687 (positive regulation of leukocyte migration)
GO:0003051 (angiotensin-mediated drinking behavior)
GO:0006954 (inflammatory response)
GO:0007165 (signal transduction)
GO:0007186 (G-protein coupled receptor signaling pathway)
GO:0007200 (phospholipase C-activating G-protein coupled receptor signaling pathway)
GO:0007204 (positive regulation of cytosolic calcium ion concentration)
GO:0007217 (tachykinin receptor signaling pathway)
GO:0007268 (chemical synaptic transmission)
GO:0007611 (learning or memory)
GO:0007616 (long-term memory)
GO:0008217 (regulation of blood pressure)
GO:0008306 (associative learning)
GO:0009408 (response to heat)
GO:0009582 (detection of abiotic stimulus)
GO:0009725 (response to hormone)
GO:0010193 (response to ozone)
GO:0010634 (positive regulation of epithelial cell migration)
GO:0010996 (response to auditory stimulus)
GO:0014070 (response to organic cyclic compound)
GO:0014910 (regulation of smooth muscle cell migration)
GO:0019233 (sensory perception of pain)
GO:0032224 (positive regulation of synaptic transmission, cholinergic)
GO:0032230 (positive regulation of synaptic transmission, GABAergic)
GO:0032355 (response to estradiol)
GO:0032570 (response to progesterone)
GO:0035094 (response to nicotine)
GO:0035106 (operant conditioning)
GO:0035815 (positive regulation of renal sodium excretion)
GO:0042713 (sperm ejaculation)
GO:0042755 (eating behavior)
GO:0043117 (positive regulation of vascular permeability)
GO:0043278 (response to morphine)
GO:0045471 (response to ethanol)
GO:0045760 (positive regulation of action potential)
GO:0045777 (positive regulation of blood pressure)
GO:0045778 (positive regulation of ossification)
GO:0045907 (positive regulation of vasoconstriction)
GO:0045987 (positive regulation of smooth muscle contraction)
GO:0046878 (positive regulation of saliva secretion)
GO:0046887 (positive regulation of hormone secretion)
GO:0048265 (response to pain)
GO:0048266 (behavioral response to pain)
GO:0048660 (regulation of smooth muscle cell proliferation)
GO:0050671 (positive regulation of lymphocyte proliferation)
GO:0050679 (positive regulation of epithelial cell proliferation)
GO:0051496 (positive regulation of stress fiber assembly)
GO:0051602 (response to electrical stimulus)
GO:0060083 (smooth muscle contraction involved in micturition)
GO:0070472 (regulation of uterine smooth muscle contraction)
GO:0070474 (positive regulation of uterine smooth muscle contraction)
GO:1902093 (positive regulation of flagellated sperm motility)
Wikipedia Tachykinin_receptor_1

Target Cross References - Protein

canSAR P25103
Human Protein Atlas ENSG00000115353
IntAct P25103
Guide to Pharmacology 360
MICAD NBK23714 (NK1 receptor)
Open Targets ENSG00000115353
PharmGKB PA36302
Pharos P25103 (Tclin)
Reactome R-HSA-380095 (Tachykinin receptors bind tachykinins.)
R-HSA-416476 (G alpha (q) signalling events.)
R-HSA-8856825 (Cargo recognition for clathrin-mediated endocytosis.)
R-HSA-8856828 (Clathrin-mediated endocytosis.)
UniProt A8K150 P25103

Target Cross References - Domain

InterPro IPR000046 (NK1_rcpt.)
IPR000276 (GPCR_Rhodpsn.)
IPR001681 (Neurokn_rcpt.)
IPR017452 (GPCR_Rhodpsn_7TM.)
Pfam PF00001 (7tm_1)