Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
Target General Information  Top
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
EDNRA_HUMAN
Co-Targets of This Target  Top
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) 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 Drug Info IC50 = 63.3 nM [3]
3 Drug Info Ki = 80 nM [4]
4 Clazosentan Drug Info IC50 = 175 nM [5]
5 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
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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