Co-Target(s) Information
Target General Information | Top | ||||
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Target ID | T23499 | Target Info | |||
Target Name | Endothelin A receptor (EDNRA) | ||||
Synonyms |
HET-AR; Endothelin-1 receptor; Endothelin receptor type A; Endothelin receptor A; ETRA; ETA-R; ETA receptor; ETA; ET-A
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Target Type | Successful Target | ||||
Gene Name | EDNRA | ||||
Biochemical Class | GPCR rhodopsin | ||||
UniProt ID |
Co-Targets of This Target | Top | |||||
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Co-Target Name | Angiotensin II receptor type-1 (AGTR1) | Successful Target | ||||
UniProt ID | AGTR1_HUMAN | |||||
Gene Name | AGTR1 | |||||
Synonyms |
Type-1 angiotensin II receptor; Angiotensin II type-1 receptor; Angiotensin II receptor 1; Angiotensin 1 receptor; AT2R1B; AT2R1; AT1BR; AT1AR; AT1; AGTR1B; AGTR1A
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Representative Drug(s) | Sparsentan | Drug Info | Ki = 0.8 nM | [1] | ||
Co-Target Name | Endothelin B receptor (EDNRB) | Successful Target | ||||
UniProt ID | EDNRB_HUMAN | |||||
Gene Name | EDNRB | |||||
Synonyms |
Endothelin receptor type B; Endothelin receptor Non-selective type; Endothelin receptor B; ETRB; ET-BR; ET-B
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Representative Drug(s) | Darusentan | Drug Info | IC50 = 16 nM | Click to Show More | [2] | |
2 | Atrasentan | Drug Info | IC50 = 63.3 nM | [3] | ||
3 | Bosentan | Drug Info | Ki = 80 nM | [4] | ||
4 | Clazosentan | Drug Info | IC50 = 175 nM | [5] | ||
5 | Ambrisentan | Drug Info | IC50 = 195 nM | [5] | ||
6 | Macitentan | Drug Info | IC50 = 391 nM | [6] | ||
7 | BQ-123 | Drug Info | IC50 ~ 1000 nM | [6] |
References | Top | ||||
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REF 1 | Chemokine receptor antagonists. J Med Chem. 2012 Nov 26;55(22):9363-92. | ||||
REF 2 | The design and synthesis of a novel series of indole derived selective ET(A) antagonists. Bioorg Med Chem Lett. 2002 Jan 21;12(2):125-8. | ||||
REF 3 | Design, synthesis, and activity of a series of pyrrolidine-3-carboxylic acid-based, highly specific, orally active ET(B) antagonists containing a diphenylmethylamine acetamide side chain. J Med Chem. 1999 Sep 9;42(18):3679-89. | ||||
REF 4 | Biphenylsulfonamide endothelin receptor antagonists. 4. Discovery of N-[[2'-[[(4,5-dimethyl-3-isoxazolyl)amino]sulfonyl]-4-(2-oxazolyl)[1,1'-biphenyl]- 2-yl]methyl]-N,3,3-trimethylbutanamide (BMS-207940), a highly potent and orally active ET(A) selective antagonist. J Med Chem. 2003 Jan 2;46(1):125-37. | ||||
REF 5 | From bosentan (Tracleer to macitentan (Opsumit: The medicinal chemistry perspective. Bioorg Med Chem Lett. 2016 Aug 1;26(15):3381-94. | ||||
REF 6 | The discovery of N-[5-(4-bromophenyl)-6-[2-[(5-bromo-2-pyrimidinyl)oxy]ethoxy]-4-pyrimidinyl]-N'-propylsulfamide (Macitentan), an orally active, potent dual endothelin receptor antagonist. J Med Chem. 2012 Sep 13;55(17):7849-61. |
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