A hormone antagonist that blocks endothelin receptors.
ChEBI ID: 51451
| Member | Definition | Class |
|---|---|---|
| act-132577 | A member of the class of sulfamides in which one of the amino groups of sulfonamide is substituted by a 5-(4-bromophenyl)-6-{2-[(5-bromopyrimidin-2-yl)oxy]ethoxy}pyrimidin-4-yl group. An active metabolite of macitentan (obtained by oxidative depropylation), an orphan drug used for the treatment of pulmonary arterial hypertension. | ACT-132577 |
| bosentan anhydrous | bosentan | |
| enrasentan | A member of the class of indanes that is 2,3-dihydro-1H-indene which is substituted by a 1,3-benzodioxol-5-yl group, carboxy group, 2-(2-hydroxyethoxy)-4-methoxyphenyl group and a propoxy group at positions 1S, 2R, 3S and 5, respectively. It is an orally active mixed endothelin A/B receptor antagonist with a 100-fold greater affinity for the endothelin A receptor. The drug was being developed by GSK for the treatment of congestive heart failure and pulmonary hypertension (clinical trials discontinued). | enrasentan |
| losartan | A biphenylyltetrazole where a 1,1'-biphenyl group is attached at the 5-position and has an additional trisubstituted imidazol-1-ylmethyl group at the 4'-position | losartan |
| macitentan | A member of the class of sulfamides in which the two amino groups of sulfonamide are substituted by 5-(4-bromophenyl)-6-{2-[(5-bromopyrimidin-2-yl)oxy]ethoxy}pyrimidin-4-yl and propyl groups. An orphan drug used for the treatment of pulmonary arterial hypertension. | macitentan |
| pd 123319 | An imidazopyridine consisting of 4,5,6,7-tetrahydro-1H-imidazo[4,5-c]pyridine having 4-(dimethylamino)-3-methylbenzyl, diphenylacetyl and carboxy and groups at positions 1, 5 and 6 respectively | PD123319 |
| Timeframe | Studies, Drugs with This Role(%) | All Drugs % |
|---|---|---|
| pre-1990 | 1 (0.01) | 18.7374 |
| 1990's | 2,194 (23.72) | 18.2507 |
| 2000's | 3,679 (39.77) | 29.6817 |
| 2010's | 2,795 (30.22) | 24.3611 |
| 2020's | 581 (6.28) | 2.80 |
| Publication Type | Studies, Drugs with this Role (%) | All Drugs (%) |
|---|---|---|
| Trials | 1,518 (14.80%) | 5.53% |
| Reviews | 804 (7.84%) | 6.00% |
| Case Studies | 496 (4.84%) | 4.05% |
| Observational | 33 (0.32%) | 0.25% |
| Other | 7,405 (72.20%) | 84.16% |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| activating transcription factor 6 | Homo sapiens (human) | Potency | 0.2131 | 1 | 1 |
| AR protein | Homo sapiens (human) | Potency | 17.5532 | 3 | 4 |
| Chain A, Cruzipain | Trypanosoma cruzi | Potency | 39.8107 | 1 | 1 |
| Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASE | Homo sapiens (human) | Potency | 2.5119 | 1 | 1 |
| cytochrome P450 2C9, partial | Homo sapiens (human) | Potency | 10.1229 | 1 | 4 |
| cytochrome P450 3A4 isoform 1 | Homo sapiens (human) | Potency | 19.9526 | 2 | 2 |
| cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 11.5443 | 2 | 4 |
| estrogen nuclear receptor alpha | Homo sapiens (human) | Potency | 20.1363 | 3 | 3 |
| estrogen receptor 2 (ER beta) | Homo sapiens (human) | Potency | 34.3832 | 2 | 2 |
| estrogen-related nuclear receptor alpha | Homo sapiens (human) | Potency | 26.6032 | 3 | 4 |
| Fumarate hydratase | Homo sapiens (human) | Potency | 37.2212 | 1 | 1 |
| G | Vesicular stomatitis virus | Potency | 10.1229 | 1 | 4 |
| GABA theta subunit | Rattus norvegicus (Norway rat) | Potency | 19.9526 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-1 | Rattus norvegicus (Norway rat) | Potency | 19.9526 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-2 | Rattus norvegicus (Norway rat) | Potency | 19.9526 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-3 | Rattus norvegicus (Norway rat) | Potency | 19.9526 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-4 | Rattus norvegicus (Norway rat) | Potency | 19.9526 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-5 | Rattus norvegicus (Norway rat) | Potency | 19.9526 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-6 | Rattus norvegicus (Norway rat) | Potency | 19.9526 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit beta-1 | Rattus norvegicus (Norway rat) | Potency | 19.9526 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit beta-2 | Rattus norvegicus (Norway rat) | Potency | 19.9526 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit beta-3 | Rattus norvegicus (Norway rat) | Potency | 19.9526 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit delta | Rattus norvegicus (Norway rat) | Potency | 19.9526 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit epsilon | Rattus norvegicus (Norway rat) | Potency | 19.9526 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit gamma-1 | Rattus norvegicus (Norway rat) | Potency | 19.9526 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit gamma-2 | Rattus norvegicus (Norway rat) | Potency | 19.9526 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit gamma-3 | Rattus norvegicus (Norway rat) | Potency | 19.9526 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit pi | Rattus norvegicus (Norway rat) | Potency | 19.9526 | 1 | 1 |
| GLI family zinc finger 3 | Homo sapiens (human) | Potency | 8.6241 | 2 | 4 |
| glucocorticoid receptor [Homo sapiens] | Homo sapiens (human) | Potency | 0.2391 | 1 | 1 |
| heat shock protein beta-1 | Homo sapiens (human) | Potency | 33.4889 | 1 | 1 |
| histone acetyltransferase KAT2A isoform 1 | Homo sapiens (human) | Potency | 39.8107 | 1 | 1 |
| HLA class I histocompatibility antigen, B alpha chain | Homo sapiens (human) | Potency | 10.1229 | 1 | 4 |
| Inositol hexakisphosphate kinase 1 | Homo sapiens (human) | Potency | 10.1229 | 1 | 8 |
| Interferon beta | Homo sapiens (human) | Potency | 10.1229 | 1 | 4 |
| nuclear factor erythroid 2-related factor 2 isoform 1 | Homo sapiens (human) | Potency | 33.4889 | 1 | 1 |
| nuclear receptor ROR-gamma isoform 1 | Mus musculus (house mouse) | Potency | 35.4813 | 1 | 1 |
| peroxisome proliferator activated receptor gamma | Homo sapiens (human) | Potency | 22.4819 | 3 | 3 |
| phosphopantetheinyl transferase | Bacillus subtilis | Potency | 56.2341 | 1 | 1 |
| polyprotein | Zika virus | Potency | 37.2212 | 1 | 1 |
| pregnane X nuclear receptor | Homo sapiens (human) | Potency | 9.2671 | 2 | 2 |
| progesterone receptor | Homo sapiens (human) | Potency | 33.4915 | 1 | 1 |
| RAR-related orphan receptor gamma | Mus musculus (house mouse) | Potency | 20.6087 | 2 | 2 |
| retinoic acid nuclear receptor alpha variant 1 | Homo sapiens (human) | Potency | 29.8493 | 1 | 1 |
| Spike glycoprotein | Severe acute respiratory syndrome-related coronavirus | Potency | 9.0532 | 1 | 2 |
| TDP1 protein | Homo sapiens (human) | Potency | 18.8375 | 1 | 1 |
| v-jun sarcoma virus 17 oncogene homolog (avian) | Homo sapiens (human) | Potency | 30.1065 | 1 | 1 |
| vitamin D (1,25- dihydroxyvitamin D3) receptor | Homo sapiens (human) | Potency | 33.4889 | 1 | 1 |
| vitamin D3 receptor isoform VDRA | Homo sapiens (human) | Potency | 28.1838 | 1 | 1 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| 5-hydroxytryptamine receptor 1A | Rattus norvegicus (Norway rat) | IC50 | 0.0190 | 1 | 1 |
| Adenosine receptor A2a | Rattus norvegicus (Norway rat) | IC50 | 0.0032 | 1 | 1 |
| Angiotensin-converting enzyme | Homo sapiens (human) | IC50 | 0.0190 | 1 | 1 |
| ATP-binding cassette sub-family C member 3 | Homo sapiens (human) | IC50 | 42.0000 | 1 | 1 |
| Atrial natriuretic peptide receptor 3 | Homo sapiens (human) | IC50 | 0.0018 | 1 | 1 |
| Bile salt export pump | Homo sapiens (human) | IC50 | 20.5538 | 7 | 8 |
| Bile salt export pump | Rattus norvegicus (Norway rat) | IC50 | 30.6000 | 1 | 1 |
| Bile salt export pump | Rattus norvegicus (Norway rat) | Ki | 12.0000 | 1 | 1 |
| Broad substrate specificity ATP-binding cassette transporter ABCG2 | Homo sapiens (human) | IC50 | 35.0000 | 1 | 1 |
| cAMP-specific 3',5'-cyclic phosphodiesterase 4A | Homo sapiens (human) | IC50 | 26.0000 | 1 | 1 |
| cAMP-specific 3',5'-cyclic phosphodiesterase 4B | Homo sapiens (human) | IC50 | 26.0000 | 1 | 1 |
| cAMP-specific 3',5'-cyclic phosphodiesterase 4C | Homo sapiens (human) | IC50 | 26.0000 | 1 | 1 |
| cAMP-specific 3',5'-cyclic phosphodiesterase 4D | Homo sapiens (human) | IC50 | 26.0000 | 1 | 1 |
| cGMP-inhibited 3',5'-cyclic phosphodiesterase A | Homo sapiens (human) | IC50 | 13.0000 | 1 | 1 |
| cGMP-inhibited 3',5'-cyclic phosphodiesterase B | Homo sapiens (human) | IC50 | 13.0000 | 1 | 1 |
| Cytochrome P450 2C9 | Homo sapiens (human) | IC50 | 2.8820 | 1 | 1 |
| Deoxyhypusine synthase | Homo sapiens (human) | IC50 | 60.8300 | 1 | 1 |
| Endothelin receptor type B | Homo sapiens (human) | IC50 | 0.4895 | 9 | 12 |
| Endothelin receptor type B | Rattus norvegicus (Norway rat) | IC50 | 0.4910 | 2 | 3 |
| Endothelin receptor type B | Homo sapiens (human) | Ki | 0.1602 | 3 | 4 |
| Endothelin-1 receptor | Homo sapiens (human) | IC50 | 0.1434 | 10 | 13 |
| Endothelin-1 receptor | Rattus norvegicus (Norway rat) | IC50 | 0.0047 | 1 | 1 |
| Endothelin-1 receptor | Sus scrofa (pig) | IC50 | 0.0075 | 1 | 1 |
| Endothelin-1 receptor | Homo sapiens (human) | Ki | 0.0042 | 3 | 4 |
| Endothelin-1 receptor | Rattus norvegicus (Norway rat) | Ki | 0.0065 | 1 | 1 |
| Multidrug and toxin extrusion protein 1 | Homo sapiens (human) | IC50 | 250.0000 | 1 | 1 |
| Multidrug resistance-associated protein 4 | Homo sapiens (human) | IC50 | 22.0000 | 1 | 1 |
| Neprilysin | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| Platelet glycoprotein VI | Homo sapiens (human) | IC50 | 4.0000 | 2 | 2 |
| Sodium/bile acid cotransporter | Homo sapiens (human) | IC50 | 20,000.0000 | 2 | 2 |
| Solute carrier organic anion transporter family member 1B1 | Homo sapiens (human) | IC50 | 0.2884 | 1 | 1 |
| Solute carrier organic anion transporter family member 1B1 | Homo sapiens (human) | Ki | 0.1600 | 1 | 1 |
| Solute carrier organic anion transporter family member 1B3 | Homo sapiens (human) | IC50 | 1.1482 | 1 | 1 |
| Solute carrier organic anion transporter family member 1B3 | Homo sapiens (human) | Ki | 0.8900 | 1 | 1 |
| Squalene synthase | Rattus norvegicus (Norway rat) | Ki | 0.0050 | 1 | 1 |
| Thromboxane A2 receptor | Homo sapiens (human) | IC50 | 20.0000 | 1 | 1 |
| Type-1 angiotensin II receptor | Cavia porcellus (domestic guinea pig) | IC50 | 0.0180 | 1 | 1 |
| Type-1 angiotensin II receptor | Homo sapiens (human) | IC50 | 0.0470 | 11 | 12 |
| Type-1 angiotensin II receptor | Oryctolagus cuniculus (rabbit) | IC50 | 0.0250 | 2 | 2 |
| Type-1 angiotensin II receptor | Homo sapiens (human) | Ki | 0.0115 | 4 | 4 |
| Type-1A angiotensin II receptor | Rattus norvegicus (Norway rat) | IC50 | 0.0356 | 15 | 17 |
| Type-1A angiotensin II receptor | Rattus norvegicus (Norway rat) | Ki | 0.0132 | 5 | 8 |
| Type-1B angiotensin II receptor | Rattus norvegicus (Norway rat) | IC50 | 1.6672 | 20 | 22 |
| Type-1B angiotensin II receptor | Rattus norvegicus (Norway rat) | Ki | 0.0212 | 6 | 9 |
| Type-2 angiotensin II receptor | Homo sapiens (human) | IC50 | 8.0038 | 5 | 5 |
| Type-2 angiotensin II receptor | Rattus norvegicus (Norway rat) | IC50 | 24.9148 | 9 | 9 |
| Type-2 angiotensin II receptor | Homo sapiens (human) | Ki | 120.0000 | 1 | 1 |
| Type-2 angiotensin II receptor | Rattus norvegicus (Norway rat) | Ki | 0.0316 | 1 | 1 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Endothelin receptor type B | Bos taurus (cattle) | Kd | 0.0724 | 1 | 1 |
| Endothelin receptor type B | Homo sapiens (human) | Kd | 0.0724 | 1 | 1 |
| Endothelin-1 receptor | Rattus norvegicus (Norway rat) | Kd | 0.0561 | 2 | 2 |
| Nuclear receptor subfamily 1 group I member 2 | Homo sapiens (human) | EC50 | 11.8667 | 3 | 3 |
| Platelet glycoprotein VI | Homo sapiens (human) | Kd | 170.0000 | 2 | 2 |
| Type-1 angiotensin II receptor | Cavia porcellus (domestic guinea pig) | Kd | 0.0126 | 1 | 1 |
| Type-1 angiotensin II receptor | Homo sapiens (human) | Kd | 0.0033 | 1 | 1 |
| Type-1 angiotensin II receptor | Oryctolagus cuniculus (rabbit) | Kd | 0.0426 | 5 | 6 |
| Type-1A angiotensin II receptor | Rattus norvegicus (Norway rat) | Kd | 0.0100 | 1 | 1 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| ATP-dependent translocase ABCB1 | Homo sapiens (human) | Km | 245.0667 | 3 | 3 |
| Platelet glycoprotein VI | Homo sapiens (human) | MEC | 500.0000 | 1 | 1 |
| Thromboxane A2 receptor | Homo sapiens (human) | MEC | 0.5000 | 1 | 1 |
| Type-1 angiotensin II receptor | Homo sapiens (human) | Affinity | 0.0064 | 1 | 1 |
| Type-1 angiotensin II receptor | Homo sapiens (human) | Kb | 0.0060 | 3 | 3 |