Page last updated: 2024-08-05 15:50:56

substance P receptor antagonist

An antagonist at the substance P receptor.

ChEBI ID: 55351

Members (1)

MemberDefinitionClass
aprepitantA morpholine-based antiemetic, which is or the prevention of acute and delayed nausea and vomiting associated with initial and repeat courses of highly emetogenic cancer chemotherapy. Aprepitant is a selective high-affinity antagonist of human substance P/neurokinin 1 (NK1) receptors.aprepitant

Research

Studies (737)

TimeframeStudies, Drugs with This Role(%)All Drugs %
pre-19905 (0.68)18.7374
1990's11 (1.49)18.2507
2000's174 (23.61)29.6817
2010's400 (54.27)24.3611
2020's147 (19.95)2.80

Study Types

Publication TypeStudies, Drugs with this Role (%)All Drugs (%)
Trials229 (29.78%)5.53%
Reviews115 (14.95%)6.00%
Case Studies33 (4.29%)4.05%
Observational15 (1.95%)0.25%
Other377 (49.02%)84.16%

Protein Targets (48)

Potency Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
AR proteinHomo sapiens (human)Potency29.053366
caspase 7, apoptosis-related cysteine proteaseHomo sapiens (human)Potency33.491511
caspase-3Homo sapiens (human)Potency33.491511
Cellular tumor antigen p53Homo sapiens (human)Potency30.733622
cytochrome P450 2C9, partialHomo sapiens (human)Potency11.987711
cytochrome P450 2D6Homo sapiens (human)Potency15.487111
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency0.691811
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency29.849311
estrogen nuclear receptor alphaHomo sapiens (human)Potency26.382855
estrogen receptor 2 (ER beta)Homo sapiens (human)Potency26.603211
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency25.848267
farnesoid X nuclear receptorHomo sapiens (human)Potency29.847011
GVesicular stomatitis virusPotency11.987711
GALC proteinHomo sapiens (human)Potency0.631012
GLI family zinc finger 3Homo sapiens (human)Potency11.570822
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency27.182433
Glutamate receptor 2Rattus norvegicus (Norway rat)Potency29.849311
heat shock protein beta-1Homo sapiens (human)Potency33.488922
Histone H2A.xCricetulus griseus (Chinese hamster)Potency61.931522
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency11.987711
hypoxia-inducible factor 1 alpha subunitHomo sapiens (human)Potency26.832511
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency11.987712
Interferon betaHomo sapiens (human)Potency11.987711
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency33.488911
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency10.015022
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency33.488911
peroxisome proliferator-activated receptor deltaHomo sapiens (human)Potency31.668022
pregnane X nuclear receptorHomo sapiens (human)Potency9.439211
progesterone receptorHomo sapiens (human)Potency22.041222
RAR-related orphan receptor gammaMus musculus (house mouse)Potency26.603222
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency29.606733
retinoid X nuclear receptor alphaHomo sapiens (human)Potency12.065122
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency39.810711
TDP1 proteinHomo sapiens (human)Potency19.986822
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency10.074133
thyroid stimulating hormone receptorHomo sapiens (human)Potency29.849311
v-jun sarcoma virus 17 oncogene homolog (avian)Homo sapiens (human)Potency26.832522
vitamin D (1,25- dihydroxyvitamin D3) receptorHomo sapiens (human)Potency28.339822
Voltage-dependent calcium channel gamma-2 subunitMus musculus (house mouse)Potency29.849311

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50133.000011
Bile salt export pumpHomo sapiens (human)IC50133.000011
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50133.000011
Cytochrome P450 3A4Homo sapiens (human)IC500.046011
Multidrug resistance-associated protein 4Homo sapiens (human)IC50133.000011
Neuromedin-K receptorHomo sapiens (human)Ki0.454111
Substance-P receptorHomo sapiens (human)IC500.00021010
Substance-P receptorMeriones unguiculatus (Mongolian gerbil)IC500.000111
Substance-P receptorHomo sapiens (human)Ki0.001333

Activation Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
cGMP-dependent protein kinase 1 Homo sapiens (human)EC50200.000011
Substance-P receptorHomo sapiens (human)Kd0.008311