General Information of the Protein
Protein ID
PT06168
Protein Name
Endothelin-1 receptor
Secondarily
Protein Name
Endothelin receptor type A
Gene Name
EDNRA
Secondarily
Gene Name
Gpcr10
Sequence
MSIFCLAAYFWLTMVGGVMADNPERYSANLSSHMEDFTPFPGTEINFLGTTHRPPNLALPSNGSMHGYCPQQTKITTAFKYINTVISCTIFIVGMVGNATLLRIIYQNKCMRNGPNALIASLALGDLIYVVIDLPINVFKLLAGRWPFDHNDFGVFLCKLFPFLQKSSVGITVLNLCALSVDRYRAVASWSRVQGIGIPLITAIEIVSIWILSFILAIPEAIGFVMVPFEYKGELHRTCMLNATSKFMEFYQDVKDWWLFGFYFCMPLVCTAIFYTLMTCEMLNRRNGSLRIALSEHLKQRREVAKTVFCLVVIFALCWFPLHLSRILKKTVYDEMDKNRCELLSFLLLMDYIGINLATMNSCINPIALYFVSKKFKNCFQSCLCCCCHQSKSLMTSVPMNGTSIQWKNQEQNNHNTERSSHKDSMN
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Organism
Mus musculus, Mouse
Protein Classification
Membrane receptor
>
Family A G protein-coupled receptor
>
Peptide receptor (family A GPCR)
>
Short peptide receptor (family A GPCR)
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Endothelin receptor
Function
Receptor for endothelin-1. Mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. The rank order of binding affinities for ET-A is: ET1 > ET2 >> ET3 (By similarity).
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Uniprot ID
Primary ID:
Q61614

Secondarily ID:
O54993
Q91VV2
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Ensembl ID
ENSG00000151617
Subcellular Location
Cell membrane
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000035 , NIH 3T3
 Cell Line Info 
Compound ID Compound Name Compound Formula
CP0185800
 Compound Info 
(S)-3-{2-[((R)-2-Acetylamino-3-phenyl-propionyl)-benzyl-amino]-acetylamino}-N-((1S,2R)-1-{(1S,2R)-1-[(S)-1-carboxy-2-(1H-indol-3-yl)-ethylcarbamoyl]-2-methyl-butylcarbamoyl}-2-methyl-butyl)-succinamic acid
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C47H59N7O10
  1
1
IC50 = 12 nM
 Bioactivity Info 
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CP0212909
 Compound Info 
(S)-3-{(S)-2-[(R)-2-Acetylamino-3-(1H-indol-3-yl)-propionylamino]-5-amino-pentanoylamino}-N-((1S,2R)-1-{(1S,2R)-1-[(S)-1-carboxy-2-(1H-indol-3-yl)-ethylcarbamoyl]-2-methyl-butylcarbamoyl}-2-methyl-butyl)-succinamic acid
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C45H61N9O10
  1
1
IC50 = 15 nM
 Bioactivity Info 
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CP0370269
 Compound Info 
(S)-3-{(S)-2-[(R)-2-Acetylamino-3-(4-hydroxy-phenyl)-propionylamino]-5-amino-pentanoylamino}-N-((1S,2R)-1-{(1S,2R)-1-[(S)-1-carboxy-2-(1H-indol-3-yl)-ethylcarbamoyl]-2-methyl-butylcarbamoyl}-2-methyl-butyl)-succinamic acid
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C43H60N8O11
  1
1
IC50 = 26 nM
 Bioactivity Info 
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CP0061928
 Compound Info 
(R)-3-{[(R)-1-((R)-2-Acetylamino-3-phenyl-propionyl)-pyrrolidine-2-carbonyl]-amino}-N-((1R,2S)-1-{(1R,2S)-1-[(R)-1-carboxy-2-(1H-indol-3-yl)-ethylcarbamoyl]-2-methyl-butylcarbamoyl}-2-methyl-butyl)-succinamic acid
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C43H57N7O10
  1
1
IC50 = 45 nM
 Bioactivity Info 
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CP0514930
 Compound Info 
(S)-3-[(S)-2-((R)-2-Acetylamino-3-phenyl-propionylamino)-propionylamino]-N-((1S,2R)-1-{(1S,2R)-1-[(S)-1-carboxy-2-(1H-indol-3-yl)-ethylcarbamoyl]-2-methyl-butylcarbamoyl}-2-methyl-butyl)-succinamic acid
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C41H55N7O10
  1
1
IC50 = 57 nM
 Bioactivity Info 
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CP0460733
 Compound Info 
(S)-3-[(S)-2-((R)-2-Acetylamino-3-phenyl-propionylamino)-4-phenyl-butyrylamino]-N-((1S,2R)-1-{(1S,2R)-1-[(S)-1-carboxy-2-(1H-indol-3-yl)-ethylcarbamoyl]-2-methyl-butylcarbamoyl}-2-methyl-butyl)-succinamic acid
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C48H61N7O10
  1
1
IC50 = 70 nM
 Bioactivity Info 
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CP0403704
 Compound Info 
(S)-3-[(S)-2-((R)-2-Acetylamino-3-phenyl-propionylamino)-3-carbamoyl-propionylamino]-N-((1S,2R)-1-{(1S,2R)-1-[(S)-1-carboxy-2-(1H-indol-3-yl)-ethylcarbamoyl]-2-methyl-butylcarbamoyl}-2-methyl-butyl)-succinamic acid
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C42H56N8O11
  1
1
IC50 = 75 nM
 Bioactivity Info 
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CP0509980
 Compound Info 
(S)-3-[(S)-2-((R)-2-Acetylamino-3-phenyl-propionylamino)-3-(4-hydroxy-phenyl)-propionylamino]-N-((1S,2R)-1-{(1S,2R)-1-[(S)-1-carboxy-2-(1H-indol-3-yl)-ethylcarbamoyl]-2-methyl-butylcarbamoyl}-2-methyl-butyl)-succinamic acid
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C47H59N7O11
  1
1
IC50 = 77 nM
 Bioactivity Info 
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CP0378027
 Compound Info 
(S)-3-[(S)-2-((R)-2-Acetylamino-3-phenyl-propionylamino)-3-(1H-indol-3-yl)-propionylamino]-N-((1S,2R)-1-{(1S,2R)-1-[(S)-1-carboxy-2-(1H-indol-3-yl)-ethylcarbamoyl]-2-methyl-butylcarbamoyl}-2-methyl-butyl)-succinamic acid
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C49H60N8O10
  1
1
IC50 = 79 nM
 Bioactivity Info 
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CP0470126
 Compound Info 
(S)-3-[(R)-2-((R)-2-Acetylamino-3-phenyl-propionylamino)-3-phenyl-propionylamino]-N-((1S,2R)-1-{(1S,2R)-1-[(S)-1-carboxy-2-(1H-indol-3-yl)-ethylcarbamoyl]-2-methyl-butylcarbamoyl}-2-methyl-butyl)-succinamic acid
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C47H59N7O10
  1
1
IC50 = 98 nM
 Bioactivity Info 
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CP0460780
 Compound Info 
(S)-3-[(S)-2-((R)-2-Acetylamino-3-phenyl-propionylamino)-5-amino-pentanoylamino]-N-((S)-1-{(1S,2R)-1-[(S)-1-carboxy-2-(1H-indol-3-yl)-ethylcarbamoyl]-2-methyl-butylcarbamoyl}-3-phenyl-propyl)-succinamic acid
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C47H60N8O10
  1
1
IC50 = 114 nM
 Bioactivity Info 
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CP0192397
 Compound Info 
(S)-3-[(S)-2-((R)-2-Acetylamino-3-phenyl-propionylamino)-5-amino-pentanoylamino]-N-((1S,2R)-1-{(1S,2R)-1-[(S)-1-carboxy-2-(1H-indol-3-yl)-ethylcarbamoyl]-2-methyl-butylcarbamoyl}-2-methyl-butyl)-succinamic acid
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C43H60N8O10
  1
1
IC50 = 230 nM
 Bioactivity Info 
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CP0407022
 Compound Info 
(S)-3-[(S)-2-((R)-2-Acetylamino-3-phenyl-propionylamino)-3-phenyl-propionylamino]-N-((1S,2R)-1-{(1S,2R)-1-[(S)-1-carboxy-2-(1H-indol-3-yl)-ethylcarbamoyl]-2-methyl-butylcarbamoyl}-2-methyl-butyl)-succinamic acid
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C47H59N7O10
  1
1
IC50 = 270 nM
 Bioactivity Info 
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Similar Protein(s) and Bioactivity Statistics
90% Identity
Protein ID Protein Name Protein Organism
PT01372 Endothelin-1 receptor Homo sapiens, Human
 Protein Info 
PT01785 Endothelin-1 receptor Rattus norvegicus, Rat
 Protein Info