An antagonist at the neurokinin-1 receptor.
| Member | Definition | Class |
|---|
| aprepitant | A 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 |
| fosaprepitant | A morpholine derivative that is the (1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethyl ether of (3-{[(2R,3S)-3-(4-fluorophenyl)-2-hydroxymorpholin-4-yl]methyl}-5-oxo-4,5-dihydro-1H-1,2,4-triazol-1-yl)phosphonic acid. | fosaprepitant |
| netupitant | A monocarboxylic acid amide obtained by formal condensation of the carboxy group of 2-[3,5-bis(trifluoromethyl)phenyl]-2-methylpropanoic acid with the secondary amino group of N-methyl-4-(2-methylphenyl)-6-(4-methylpiperazin-1-yl)pyridin-3-amine; an antiemetic used in combination with palonosetron hydrochloride (under the trade name Akynzeo) to treat nausea and vomiting in patients undergoing cancer chemotherapy. | netupitant |
| rolapitant | An azaspiro compound that is 1,7-diazaspiro[4.5]decan-2-one carrying additional phenyl and 1-{[3,5-bis(trifluoromethyl)phenyl]ethoxy}methyl substituents at position 8. Used (in the form of the hydrochloride hydrate) for the prevention of delayed nausea and vomiting associated with initial and repeat courses of emetogenic cancer chemotherapy. | rolapitant |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|
| AR protein | Homo sapiens (human) | Potency | 29.0533 | 6 | 6 |
| caspase 7, apoptosis-related cysteine protease | Homo sapiens (human) | Potency | 33.4915 | 1 | 1 |
| caspase-3 | Homo sapiens (human) | Potency | 33.4915 | 1 | 1 |
| Cellular tumor antigen p53 | Homo sapiens (human) | Potency | 30.7336 | 2 | 2 |
| cytochrome P450 2C9, partial | Homo sapiens (human) | Potency | 14.0092 | 1 | 3 |
| cytochrome P450 2D6 | Homo sapiens (human) | Potency | 16.3642 | 1 | 3 |
| cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 3.4065 | 1 | 3 |
| cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_a | Homo sapiens (human) | Potency | 29.8493 | 1 | 1 |
| estrogen nuclear receptor alpha | Homo sapiens (human) | Potency | 26.3828 | 5 | 5 |
| estrogen receptor 2 (ER beta) | Homo sapiens (human) | Potency | 26.6032 | 1 | 1 |
| estrogen-related nuclear receptor alpha | Homo sapiens (human) | Potency | 25.8482 | 6 | 7 |
| farnesoid X nuclear receptor | Homo sapiens (human) | Potency | 29.8470 | 1 | 1 |
| G | Vesicular stomatitis virus | Potency | 14.0092 | 1 | 3 |
| GALC protein | Homo sapiens (human) | Potency | 0.6310 | 1 | 2 |
| GLI family zinc finger 3 | Homo sapiens (human) | Potency | 11.5708 | 2 | 2 |
| glucocorticoid receptor [Homo sapiens] | Homo sapiens (human) | Potency | 27.1824 | 3 | 3 |
| Glutamate receptor 2 | Rattus norvegicus (Norway rat) | Potency | 29.8493 | 1 | 1 |
| heat shock protein beta-1 | Homo sapiens (human) | Potency | 33.4889 | 2 | 2 |
| Histone H2A.x | Cricetulus griseus (Chinese hamster) | Potency | 61.9315 | 2 | 2 |
| HLA class I histocompatibility antigen, B alpha chain | Homo sapiens (human) | Potency | 14.0092 | 1 | 3 |
| hypoxia-inducible factor 1 alpha subunit | Homo sapiens (human) | Potency | 26.8325 | 1 | 1 |
| Inositol hexakisphosphate kinase 1 | Homo sapiens (human) | Potency | 14.0092 | 1 | 6 |
| Interferon beta | Homo sapiens (human) | Potency | 20.1107 | 2 | 6 |
| nuclear factor erythroid 2-related factor 2 isoform 1 | Homo sapiens (human) | Potency | 33.4889 | 1 | 1 |
| nuclear receptor subfamily 1, group I, member 3 | Homo sapiens (human) | Potency | 10.0150 | 2 | 2 |
| peroxisome proliferator activated receptor gamma | Homo sapiens (human) | Potency | 33.4889 | 1 | 1 |
| peroxisome proliferator-activated receptor delta | Homo sapiens (human) | Potency | 31.6680 | 2 | 2 |
| PPM1D protein | Homo sapiens (human) | Potency | 26.2123 | 1 | 2 |
| pregnane X nuclear receptor | Homo sapiens (human) | Potency | 9.4392 | 1 | 1 |
| progesterone receptor | Homo sapiens (human) | Potency | 22.0412 | 2 | 2 |
| RAR-related orphan receptor gamma | Mus musculus (house mouse) | Potency | 26.6032 | 2 | 2 |
| retinoic acid nuclear receptor alpha variant 1 | Homo sapiens (human) | Potency | 29.6067 | 3 | 3 |
| retinoid X nuclear receptor alpha | Homo sapiens (human) | Potency | 12.0651 | 2 | 2 |
| Spike glycoprotein | Severe acute respiratory syndrome-related coronavirus | Potency | 39.8107 | 1 | 2 |
| TDP1 protein | Homo sapiens (human) | Potency | 19.9868 | 2 | 2 |
| thyroid hormone receptor beta isoform 2 | Rattus norvegicus (Norway rat) | Potency | 10.0741 | 3 | 3 |
| thyroid stimulating hormone receptor | Homo sapiens (human) | Potency | 29.8493 | 1 | 1 |
| v-jun sarcoma virus 17 oncogene homolog (avian) | Homo sapiens (human) | Potency | 26.8325 | 2 | 2 |
| vitamin D (1,25- dihydroxyvitamin D3) receptor | Homo sapiens (human) | Potency | 28.3398 | 2 | 2 |
| Voltage-dependent calcium channel gamma-2 subunit | Mus musculus (house mouse) | Potency | 29.8493 | 1 | 1 |