General Information of the Protein
Protein ID
PT04767
Protein Name
Thyrotropin-releasing hormone receptor
Secondarily
Protein Name
Thyroliberin receptor
Gene Name
TRHR
Sequence
MENETVSELNQTQLQPRAVVALEYQVVTILLVLIICGLGIVGNIMVVLVVMRTKHMRTPTNCYLVSLAVADLMVLVAAGLPNITDSIYGSWVYGYVGCLCITYLQYLGINASSCSITAFTIERYIAICHPIKAQFLCTFSRAKKIIIFVWAFTSLYCMLWFFLLDLNISTYKDAIVISCGYKISRNYYSPIYLMDFGVFYVVPMILATVLYGFIARILFLNPIPSDPKENSKTWKNDSTHQNTNLNVNTSNRCFNSTVSSRKQVTKMLAVVVILFALLWMPYRTLVVVNSFLSSPFQENWFLLFCRICIYLNSAINPVIYNLMSQKFRAAFRKLCNCKQKPTEKPANYSVALNYSVIKESDHFSTELDDITVTDTYLSATKVSFDDTCLASEVSFSQS
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Organism
Homo sapiens, Human
Protein Classification
Membrane receptor
>
Family A G protein-coupled receptor
>
Peptide receptor (family A GPCR)
>
Short peptide receptor (family A GPCR)
>
Neuropeptide receptor
Function
Receptor for thyrotropin-releasing hormone (TRH). Upon ligand binding, this G-protein-coupled receptor triggers activation of the phosphatidylinositol (IP3)-calcium-protein kinase C (PKC) pathway.
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Uniprot ID
Primary ID:
P34981

Secondarily ID:
Q2M339
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Ensembl ID
ENSG00000174417
HGNC ID
HGNC:12299
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: CL001022 , HEK293EM
 Cell Line Info 
Compound ID Compound Name Compound Formula
CP0067202
 Compound Info 
1-[3-(1H-4-imidazolyl)-2-(5-oxotetrahydro-1H-2-pyrrolylcarboxamido)propanoyl]tetrahydro-1H-2-pyrrolecarboxamide
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C16H22N6O4
  1
1
EC50 = 3 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0253387
 Compound Info 
(2S)-1-{(2S)-3-(1-methyl-1H-4-imidazolyl)-2-[(2S)-6-oxohexahydro-2-pyridinylcarboxamido]propanoyl}azolane-2-carboxamide
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C18H26N6O4
  1
1
EC50 = 4.9 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0307082
 Compound Info 
(2S)-1-[(2S)-2-amino-3-(3-methyl-1H-imidazol-3-ium-4-yl)propanoyl]-N-[(2S)-1-[(2S)-2-carbamoylpyrrolidin-1-yl]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]-5-oxopyrrolidine-2-carboxamide
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C23H32N9O5+
  1
1
EC50 = 5 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0253386
 Compound Info 
(2S)-1-{(2S)-3-(1-ethyl-1H-4-imidazolyl)-2-[(2S)-6-oxohexahydro-2-pyridinylcarboxamido]propanoyl}azoazolane-2-carboxamide
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C19H28N6O4
  1
1
EC50 = 14 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0162470
 Compound Info 
(2S)-1-[(2S)-2-(2S)-6-oxohexahydro-2-pyridinylcarboxamido]-3-(2-propyl-1H-imidazolyl)propanoyl]azalone-2-carboxamide
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C20H30N6O4
  1
1
EC50 = 380 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0162668
 Compound Info 
(2S)-1-{(2S)-3-(1-allyl-1H-4-imidazolyl)-2-[(2S)-6-oxohexahydro-2-pyridinylcarboxamido]propropanoyl}azolane-2-carboxamide
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C20H28N6O4
  1
1
EC50 = 5100 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0359956
 Compound Info 
(2S)-1-{(2S)-3-(1-benzyl-1H-4-imidazolyl)-2-[(2S)-6-oxohexahydro-2-pyridinylcarboxamido]azolane-propanoyl}azolane-2-carboxamide
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C24H30N6O4
  1
1
EC50 = 17000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0157755
 Compound Info 
(2S)-1-[(2S)-2-(1S)-3-oxocyclopentylcarboxamido]-3-(2-tert-butyl-1H-imidazolyl)propanoyl]azalone-2-carboxamide
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C21H31N5O4
  1
1
EC50 > 100000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0157756
 Compound Info 
(2S)-1-[(2S)-2-(1R)-3-oxocyclopentylcarboxamido]-3-(2-propyl-1H-imidazolyl)propanoyl]azalone-2-carboxamide
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C20H29N5O4
  1
1
EC50 > 100000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0162459
 Compound Info 
(2S)-1-[(2S)-2-(2S)-6-oxohexahydro-2-pyridinylcarboxamido]-3-(2-cyclohexyl-1H-imidazolyl)propanoyl]-azalone-2-carboxamide
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C23H34N6O4
  1
1
EC50 > 100000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0162460
 Compound Info 
(2S)-1-[(2S)-2-(2S)-6-oxohexahydro-2-pyridinylcarboxamido]-3-(2-tert-butyl-1H-imidazolyl)propanoyl]-azalone-2-carboxamide
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C21H32N6O4
  1
1
EC50 > 100000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0253385
 Compound Info 
(2S)-1-[(2S)-2-(1R)-3-oxocyclopentylcarboxamido]-3-(2-tert-butyl-1H-imidazolyl)propanoyl]azalone-2-carboxamide
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C21H31N5O4
  1
1
EC50 > 100000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0253388
 Compound Info 
(2S)-1-[(2S)-2-(1S)-3-oxocyclopentylcarboxamido]-3-(2-propyl-1H-imidazolyl)propanoyl]azalone-2-carboxamide
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C20H29N5O4
  1
1
EC50 > 100000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0307083
 Compound Info 
(2S)-1-[(2S)-2-(1S)-3-oxocyclopentylcarboxamido]-3-(2-isopropyl-1H-imidazolyl)propanoyl]azalone-2-carboxamide
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C20H29N5O4
  1
1
EC50 > 100000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0335691
 Compound Info 
(2S)-1-[(2S)-2-(1S)-3-oxocyclopentylcarboxamido]-3-(2-cyclohexyl-1H-imidazolyl)propanoyl]azalone-2-carboxamide
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C23H33N5O4
  1
1
EC50 > 100000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0335692
 Compound Info 
(2S)-1-[(2S)-2-(1R)-3-oxocyclopentylcarboxamido]-3-(2-cyclohexyl-1H-imidazolyl)propanoyl]azalone-2-carboxamide
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C23H33N5O4
  1
1
EC50 > 100000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0339773
 Compound Info 
(2S)-1-[(2S)-2-(1R)-3-oxocyclopentylcarboxamido]-3-(2-isopropyl-1H-imidazolyl)propanoyl]azalone-2-carboxamide
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C20H29N5O4
  1
1
EC50 > 100000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0359955
 Compound Info 
(2S)-1-[(2S)-2-(2S)-6-oxohexahydro-2-pyridinylcarboxamido]-3-(2-isopropyl-1H-imidazolyl)propanoyl]-azalone-2-carboxamide
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C20H30N6O4
  1
1
EC50 > 100000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0307082
 Compound Info 
(2S)-1-[(2S)-2-amino-3-(3-methyl-1H-imidazol-3-ium-4-yl)propanoyl]-N-[(2S)-1-[(2S)-2-carbamoylpyrrolidin-1-yl]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]-5-oxopyrrolidine-2-carboxamide
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C23H32N9O5+
  1
1 Ki = 3 nM
CP0253387
 Compound Info 
(2S)-1-{(2S)-3-(1-methyl-1H-4-imidazolyl)-2-[(2S)-6-oxohexahydro-2-pyridinylcarboxamido]propanoyl}azolane-2-carboxamide
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C18H26N6O4
  1
1 Ki = 3.2 nM
CP0253386
 Compound Info 
(2S)-1-{(2S)-3-(1-ethyl-1H-4-imidazolyl)-2-[(2S)-6-oxohexahydro-2-pyridinylcarboxamido]propanoyl}azoazolane-2-carboxamide
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C19H28N6O4
  1
1 Ki = 11 nM
CP0067202
 Compound Info 
1-[3-(1H-4-imidazolyl)-2-(5-oxotetrahydro-1H-2-pyrrolylcarboxamido)propanoyl]tetrahydro-1H-2-pyrrolecarboxamide
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C16H22N6O4
  1
1 Ki = 20 nM
CP0162470
 Compound Info 
(2S)-1-[(2S)-2-(2S)-6-oxohexahydro-2-pyridinylcarboxamido]-3-(2-propyl-1H-imidazolyl)propanoyl]azalone-2-carboxamide
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C20H30N6O4
  1
1 Ki = 400 nM
CP0162668
 Compound Info 
(2S)-1-{(2S)-3-(1-allyl-1H-4-imidazolyl)-2-[(2S)-6-oxohexahydro-2-pyridinylcarboxamido]propropanoyl}azolane-2-carboxamide
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C20H28N6O4
  1
1 Ki = 7500 nM
CP0157755
 Compound Info 
(2S)-1-[(2S)-2-(1S)-3-oxocyclopentylcarboxamido]-3-(2-tert-butyl-1H-imidazolyl)propanoyl]azalone-2-carboxamide
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C21H31N5O4
  1
1 Ki > 100000 nM
CP0157756
 Compound Info 
(2S)-1-[(2S)-2-(1R)-3-oxocyclopentylcarboxamido]-3-(2-propyl-1H-imidazolyl)propanoyl]azalone-2-carboxamide
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C20H29N5O4
  1
1 Ki > 100000 nM
CP0162459
 Compound Info 
(2S)-1-[(2S)-2-(2S)-6-oxohexahydro-2-pyridinylcarboxamido]-3-(2-cyclohexyl-1H-imidazolyl)propanoyl]-azalone-2-carboxamide
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C23H34N6O4
  1
1 Ki > 100000 nM
CP0162460
 Compound Info 
(2S)-1-[(2S)-2-(2S)-6-oxohexahydro-2-pyridinylcarboxamido]-3-(2-tert-butyl-1H-imidazolyl)propanoyl]-azalone-2-carboxamide
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C21H32N6O4
  1
1 Ki > 100000 nM
CP0253385
 Compound Info 
(2S)-1-[(2S)-2-(1R)-3-oxocyclopentylcarboxamido]-3-(2-tert-butyl-1H-imidazolyl)propanoyl]azalone-2-carboxamide
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C21H31N5O4
  1
1 Ki > 100000 nM
CP0253388
 Compound Info 
(2S)-1-[(2S)-2-(1S)-3-oxocyclopentylcarboxamido]-3-(2-propyl-1H-imidazolyl)propanoyl]azalone-2-carboxamide
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C20H29N5O4
  1
1 Ki > 100000 nM
CP0307083
 Compound Info 
(2S)-1-[(2S)-2-(1S)-3-oxocyclopentylcarboxamido]-3-(2-isopropyl-1H-imidazolyl)propanoyl]azalone-2-carboxamide
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C20H29N5O4
  1
1 Ki > 100000 nM
CP0335691
 Compound Info 
(2S)-1-[(2S)-2-(1S)-3-oxocyclopentylcarboxamido]-3-(2-cyclohexyl-1H-imidazolyl)propanoyl]azalone-2-carboxamide
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C23H33N5O4
  1
1 Ki > 100000 nM
CP0335692
 Compound Info 
(2S)-1-[(2S)-2-(1R)-3-oxocyclopentylcarboxamido]-3-(2-cyclohexyl-1H-imidazolyl)propanoyl]azalone-2-carboxamide
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C23H33N5O4
  1
1 Ki > 100000 nM
CP0339773
 Compound Info 
(2S)-1-[(2S)-2-(1R)-3-oxocyclopentylcarboxamido]-3-(2-isopropyl-1H-imidazolyl)propanoyl]azalone-2-carboxamide
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C20H29N5O4
  1
1 Ki > 100000 nM
CP0359955
 Compound Info 
(2S)-1-[(2S)-2-(2S)-6-oxohexahydro-2-pyridinylcarboxamido]-3-(2-isopropyl-1H-imidazolyl)propanoyl]-azalone-2-carboxamide
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C20H30N6O4
  1
1 Ki > 100000 nM
CP0359956
 Compound Info 
(2S)-1-{(2S)-3-(1-benzyl-1H-4-imidazolyl)-2-[(2S)-6-oxohexahydro-2-pyridinylcarboxamido]azolane-propanoyl}azolane-2-carboxamide
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C24H30N6O4
  1
1 Ki > 100000 nM
Clinical Information about the Protein
Target 1 ( Thyrotropin-releasing hormone receptor (TRHR) )
Target Type Successful Target
Disease 1 Target-related Disease  1
1 Central nervous system disease [ICD-11: 8A04-8D87]
Approved Drug(s) 1 Approved Drug  1
1 protirelin
 Drug Info 
Approved
Central nervous system disease
Similar Protein(s) and Bioactivity Statistics
90% Identity
Protein ID Protein Name Protein Organism
PT04668 Thyrotropin-releasing hormone receptor Mus musculus, Mouse
 Protein Info