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Drug-Target Interaction

Drug

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PubChem ID:197712
Structure:
Synonyms:
(+-)-(2S)-2-((4,6-Dimethylpyrimidin-2-yl)oxy)-3-methoxy-3,3-diphenylpropan
(+-)-(2S)-2-((4,6-Dimethylpyrimidin-2-yl)oxy)-3-methoxy-3,3-diphenylpropanoic acid
177036-94-1
2-(4,6-dimethylpyrimidin-2-yl)oxy-3-methoxy-3,3-diphenyl-propanoic acid
2-(4,6-dimethylpyrimidin-2-yl)oxy-3-methoxy-3,3-diphenylpropanoic acid
2-[(4,6-dimethylpyrimidin-2-yl)oxy]-3-methoxy-3,3-diphenylpropanoic acid
AC1L53VT
Ambrisentan
Ambrisentan [INN]
BSF 208075
BSF-208075
BSF208075
C467894
CHEBI:205299
CHEMBL302753
Gilead brand of ambrisentan
I06-2077
Letairis
LS-186563
LS-187364
LU 208075
LU-208075
LU208075
MLS001195278
MolPort-002-945-567
NCGC00160662-01
nyl-, (S)-
SMR000502713
ST51051295
STK097095
UNII-HW6NV07QEC
Side-Effects:
Side-EffectFrequency
peripheral edema0.172414
headache0.145594
nasal congestion0.0574713
palpitations0.045977
dyspnea0.0421456
constipation0.0383142
flushing0.0383142
nasopharyngitis0.0344828
sinusitis0.0306513
abdominal pain0.0306513
nausea0
breast disorders0
pulmonary hypertension0
diarrhea0
sleep disorder0
chest pain0
insomnia0
edema0
lymphatic disorders0
anorexia0
muscle cramps0
infection0
pleural effusion0
hypokalemia0
fever0
upper respiratory tract infection0
myalgia0
arthralgia0
pharyngitis0
tachycardia0
angina pectoris0
rhinitis0
cough0
right heart failure0
pneumonia0
angioedema0
influenza0
rash0
vaginal hemorrhage0
hypersensitivity0
skin ulcer0
nocturia0
heart disease0
anemia0
mediastinal disorders0
pruritus0
dizziness0
wheezing0
hemorrhage0
gastritis0

Target

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Uniprot ID:EDNRA_HUMAN
Synonyms:
Endothelin A receptor
Endothelin-1 receptor
ET-A
ETA-R
hET-AR
EC-Numbers:-
Organism:Homo sapiens
Human
PDB IDs:-

Binding Affinities:

Ki: Kd:Ic 50:Ec50/Ic50:
----
1---

References:

18238950
Endothelin receptor antagonists in pulmonary arterial hypertension.. J Dupuis; M M Hoeper (2008) The European respiratory journal : official journal of the European Society for Clinical Respiratory Physiology display abstract
The endothelin (ET) system, especially ET-1 and the ET(A) and ET(B) receptors, has been implicated in the pathogenesis of pulmonary arterial hypertension (PAH). Together with prostanoids and phosphodiesterase 5 inhibitors, ET receptor antagonists have become mainstays in the current treatment of PAH. Three substances are currently available for the treatment of PAH. One of these substances, bosentan, blocks both ET(A) and ET(B) receptors, whereas the two other compounds, sitaxsentan and ambrisentan, are more selective blockers of the ET(A) receptor. There is ongoing debate as to whether selective or nonselective ET receptor blockade is advantageous in the setting of PAH, although there is no clear evidence that receptor selectivity is relevant with regard to the clinical effects of these drugs. For the time being, other features, such as safety profiles and the potential for pharmacokinetic interactions with other drugs used in the treatment of PAH, may be more important than selectivity or nonselectivity when selecting treatments for individual patients.