General Information of the Protein
Protein ID
PT04668
Protein Name
Thyrotropin-releasing hormone receptor
Secondarily
Protein Name
Thyroliberin receptor
Gene Name
TRHR
Sequence
MENDTVSEMNQTELQPQAAVALEYQVVTILLVVIICGLGIVGNIMVVLVVMRTKHMRTPTNCYLVSLAVADLMVLVAAGLPNITDSIYGSWVYGYVGCLCITYLQYLGINASSCSITAFTIERYIAICHPIKAQFLCTFSRAKKIIIFVWAFTSIYCMLWFFLLDLNISTYKNAVVVSCGYKISRNYYSPIYLMDFGVFYVVPMILATVLYGFIARILFLNPIPSDPKENSKMWKNDSIHQNKNLNLNATNRCFNSTVSSRKQVTKMLAVVVILFALLWMPYRTLVVVNSFLSSPFQENWFLLFCRICIYLNSAINPVIYNLMSQKFRAAFRKLCNCKQKPTEKAANYSVALNYSVIKESDRFSTELEDITVTDTYVSTTKVSFDDTCLASEN
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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)
>
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
P21761
Ensembl ID
ENSG00000174417
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: CL000006 , HEK293
Compound ID Compound Name Compound Formula
CP0067202
1-[3-(1H-4-imidazolyl)-2-(5-oxotetrahydro-1H-2-pyrrolylcarboxamido)propanoyl]tetrahydro-1H-2-pyrrolecarboxamide
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C16H22N6O4
 4
1
EC50 = 1 nM
   TI
   LI
   LO
   TS
2
EC50 = 3.2 nM
   TI
   LI
   LO
   TS
3
IC50 = 2.6 nM
   TI
   LI
   LO
   TS
4
IC50 = 26 nM
   TI
   LI
   LO
   TS
CP0403074
(2S)-N-[(2S)-3-(2-bromo-1-methylimidazol-4-yl)-1-[(2S)-2-carbamoylpyrrolidin-1-yl]-1-oxopropan-2-yl]-5-oxopyrrolidine-2-carboxamide
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C17H23BrN6O4
 3
1
EC50 = 3.4 nM
   TI
   LI
   LO
   TS
2
EC50 = 28 nM
   TI
   LI
   LO
   TS
3
IC50 = 170 nM
   TI
   LI
   LO
   TS
CP0385686
(2S)-N-[(2S)-1-[(2S)-2-carbamoylpyrrolidin-1-yl]-3-(1-ethyl-2-iodoimidazol-4-yl)-1-oxopropan-2-yl]-5-oxopyrrolidine-2-carboxamide
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C18H25IN6O4
 3
1
EC50 = 4.9 nM
   TI
   LI
   LO
   TS
2
EC50 = 13 nM
   TI
   LI
   LO
   TS
3
IC50 = 1180 nM
   TI
   LI
   LO
   TS
CP0404602
(2S)-N-[(2S)-1-[(2S)-2-carbamoylpyrrolidin-1-yl]-3-(2-iodo-1-methylimidazol-4-yl)-1-oxopropan-2-yl]-5-oxopyrrolidine-2-carboxamide
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C17H23IN6O4
 3
1
EC50 = 5.9 nM
   TI
   LI
   LO
   TS
2
EC50 = 31 nM
   TI
   LI
   LO
   TS
3
IC50 = 324 nM
   TI
   LI
   LO
   TS
CP0403073
(2S)-N-[(2S)-3-(2-bromo-1-ethylimidazol-4-yl)-1-[(2S)-2-carbamoylpyrrolidin-1-yl]-1-oxopropan-2-yl]-5-oxopyrrolidine-2-carboxamide
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C18H25BrN6O4
 3
1
EC50 = 12 nM
   TI
   LI
   LO
   TS
2
EC50 = 1830 nM
   TI
   LI
   LO
   TS
3
IC50 = 18600 nM
   TI
   LI
   LO
   TS
CP0404607
(2S)-N-[(2S)-3-(1-benzyl-2,5-diiodoimidazol-4-yl)-1-[(2S)-2-carbamoylpyrrolidin-1-yl]-1-oxopropan-2-yl]-5-oxopyrrolidine-2-carboxamide
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C23H26I2N6O4
 3
1
EC50 = 15 nM
   TI
   LI
   LO
   TS
2
EC50 = 53 nM
   TI
   LI
   LO
   TS
3
IC50 > 50000 nM
   TI
   LI
   LO
   TS
CP0848540
N-((S)-1-((S)-2-carbamoylpyrrolidin-1-yl)-1-oxo-3-(2-propyl-1H-imidazol-4-yl)propan-2-yl)-5-methylpyrazine-2-carboxamide
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C20H27N7O3
 2
1
EC50 = 17 nM
   TI
   LI
   LO
   TS
2
IC50 > 50000 nM
   TI
   LI
   LO
   TS
CP0455656
(2S)-N-[(2S)-3-(1-benzyl-2-iodoimidazol-4-yl)-1-[(2S)-2-carbamoylpyrrolidin-1-yl]-1-oxopropan-2-yl]-5-oxopyrrolidine-2-carboxamide
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C23H27IN6O4
 3
1
EC50 = 27 nM
   TI
   LI
   LO
   TS
2
EC50 = 339 nM
   TI
   LI
   LO
   TS
3
IC50 > 50000 nM
   TI
   LI
   LO
   TS
CP0385924
(2S)-N-[(2S)-3-(2-bromo-1-propylimidazol-4-yl)-1-[(2S)-2-carbamoylpyrrolidin-1-yl]-1-oxopropan-2-yl]-5-oxopyrrolidine-2-carboxamide
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C19H27BrN6O4
 2
1
EC50 = 32 nM
   TI
   LI
   LO
   TS
2
IC50 > 50000 nM
   TI
   LI
   LO
   TS
CP0382215
N-[(2S)-1-[(2S)-2-carbamoylpyrrolidin-1-yl]-3-(2,4-dibromo-1H-imidazol-5-yl)-1-oxopropan-2-yl]-5-methylpyrazine-2-carboxamide
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C17H19Br2N7O3
 2
1
EC50 = 77 nM
   TI
   LI
   LO
   TS
2
IC50 > 50000 nM
   TI
   LI
   LO
   TS
CP0867216
N-((S)-1-((S)-2-carbamoylpyrrolidin-1-yl)-1-oxo-3-(2-propyl-1H-imidazol-4-yl)propan-2-yl)pyrazine-2-carboxamide
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C19H25N7O3
 2
1
EC50 = 150 nM
   TI
   LI
   LO
   TS
2
IC50 > 50000 nM
   TI
   LI
   LO
   TS
CP0385687
(2S)-N-[(2S)-1-[(2S)-2-carbamoylpyrrolidin-1-yl]-3-(1-ethyl-2,5-diiodoimidazol-4-yl)-1-oxopropan-2-yl]-5-oxopyrrolidine-2-carboxamide
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C18H24I2N6O4
 3
1
EC50 = 170 nM
   TI
   LI
   LO
   TS
2
EC50 = 249 nM
   TI
   LI
   LO
   TS
3
IC50 = 29340 nM
   TI
   LI
   LO
   TS
CP0404608
(2S)-N-[(2S)-1-[(2S)-2-carbamoylpyrrolidin-1-yl]-3-(2,5-diiodo-1-methylimidazol-4-yl)-1-oxopropan-2-yl]-5-oxopyrrolidine-2-carboxamide
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C17H22I2N6O4
 3
1
EC50 = 272 nM
   TI
   LI
   LO
   TS
2
EC50 = 36350 nM
   TI
   LI
   LO
   TS
3
IC50 = 48030 nM
   TI
   LI
   LO
   TS
CP0515385
3-amino-N-[(2S)-3-(4-bromo-1H-imidazol-5-yl)-1-[(2S)-2-carbamoylpyrrolidin-1-yl]-1-oxopropan-2-yl]pyrazine-2-carboxamide
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C16H19BrN8O3
 2
1
EC50 = 287 nM
   TI
   LI
   LO
   TS
2
IC50 > 50000 nM
   TI
   LI
   LO
   TS
CP0404605
(2S)-N-[(2S)-1-[(2S)-2-carbamoylpyrrolidin-1-yl]-3-(2-chloro-1-methylimidazol-4-yl)-1-oxopropan-2-yl]-5-oxopyrrolidine-2-carboxamide
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C17H23ClN6O4
 3
1
EC50 = 320 nM
   TI
   LI
   LO
   TS
2
EC50 = 790 nM
   TI
   LI
   LO
   TS
3
IC50 > 50000 nM
   TI
   LI
   LO
   TS
CP0380508
N-[(2S)-3-(5-bromo-1-methylimidazol-4-yl)-1-[(2S)-2-carbamoylpyrrolidin-1-yl]-1-oxopropan-2-yl]pyrazine-2-carboxamide
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C17H20BrN7O3
 2
1
EC50 = 340 nM
   TI
   LI
   LO
   TS
2
IC50 > 50000 nM
   TI
   LI
   LO
   TS
CP0380484
N-[(2S)-3-(4-bromo-1H-imidazol-5-yl)-1-[(2S)-2-carbamoylpyrrolidin-1-yl]-1-oxopropan-2-yl]-5-methylpyrazine-2-carboxamide
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C17H20BrN7O3
 2
1
EC50 = 498 nM
   TI
   LI
   LO
   TS
2
IC50 > 50000 nM
   TI
   LI
   LO
   TS
CP0380507
N-[(2S)-3-(1-benzyl-2,5-diiodoimidazol-4-yl)-1-[(2S)-2-carbamoylpyrrolidin-1-yl]-1-oxopropan-2-yl]-5-methylpyrazine-2-carboxamide
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C24H25I2N7O3
 2
1
EC50 = 740 nM
   TI
   LI
   LO
   TS
2
IC50 > 50000 nM
   TI
   LI
   LO
   TS
CP0448149
(2S)-N-[(2S)-1-[(2S)-2-carbamoylpyrrolidin-1-yl]-3-(2,5-diiodo-1-propylimidazol-4-yl)-1-oxopropan-2-yl]-5-oxopyrrolidine-2-carboxamide
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C19H26I2N6O4
 3
1
EC50 = 780 nM
   TI
   LI
   LO
   TS
2
EC50 = 2400 nM
   TI
   LI
   LO
   TS
3
IC50 > 50000 nM
   TI
   LI
   LO
   TS
CP0380486
(2R)-N-[(2S)-1-[(2S)-2-carbamoylpyrrolidin-1-yl]-1-oxo-3-(2-propyl-1H-imidazol-5-yl)propan-2-yl]piperidine-2-carboxamide
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C20H32N6O3
 2
1
EC50 = 940 nM
   TI
   LI
   LO
   TS
2
IC50 > 50000 nM
   TI
   LI
   LO
   TS
CP0429046
N-[(2S)-3-(1-benzyl-2,5-diiodoimidazol-4-yl)-1-[(2S)-2-carbamoylpyrrolidin-1-yl]-1-oxopropan-2-yl]pyrazine-2-carboxamide
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C23H23I2N7O3
 2
1
EC50 = 980 nM
   TI
   LI
   LO
   TS
2
IC50 > 50000 nM
   TI
   LI
   LO
   TS
CP0431472
(2R)-N-[(2S)-1-[(2S)-2-carbamoylpyrrolidin-1-yl]-1-oxo-3-(2-propan-2-yl-1H-imidazol-5-yl)propan-2-yl]piperidine-2-carboxamide
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C20H32N6O3
 2
1
EC50 = 1000 nM
   TI
   LI
   LO
   TS
2
IC50 > 50000 nM
   TI
   LI
   LO
   TS
CP0867217
3-amino-N-((S)-1-((S)-2-carbamoylpyrrolidin-1-yl)-3-(2,5-dibromo-1H-imidazol-4-yl)-1-oxopropan-2-yl)pyrazine-2-carboxamide
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C16H18Br2N8O3
 2
1
EC50 = 1410 nM
   TI
   LI
   LO
   TS
2
IC50 > 50000 nM
   TI
   LI
   LO
   TS
CP0380485
3-amino-N-[(2S)-1-[(2S)-2-carbamoylpyrrolidin-1-yl]-1-oxo-3-(2-propyl-1H-imidazol-5-yl)propan-2-yl]pyrazine-2-carboxamide
   Show/Hide
C19H26N8O3
 2
1
EC50 = 1560 nM
   TI
   LI
   LO
   TS
2
IC50 > 50000 nM
   TI
   LI
   LO
   TS
CP0045937
N-[(2S)-1-[(2S)-2-carbamoylpyrrolidin-1-yl]-3-(2,4-dibromo-1H-imidazol-5-yl)-1-oxopropan-2-yl]pyrazine-2-carboxamide
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C16H17Br2N7O3
 2
1
EC50 = 2540 nM
   TI
   LI
   LO
   TS
2
IC50 > 50000 nM
   TI
   LI
   LO
   TS
CP0431506
N-[(2S)-3-(4-bromo-1H-imidazol-5-yl)-1-[(2S)-2-carbamoylpyrrolidin-1-yl]-1-oxopropan-2-yl]pyrazine-2-carboxamide
   Show/Hide
C16H18BrN7O3
 2
1
EC50 = 3980 nM
   TI
   LI
   LO
   TS
2
IC50 > 50000 nM
   TI
   LI
   LO
   TS
CP0392458
(2S)-N-[(2S)-1-[(2S)-2-carbamoylpyrrolidin-1-yl]-3-(2,4-dichloro-1H-imidazol-5-yl)-1-oxopropan-2-yl]-5-oxopyrrolidine-2-carboxamide
   Show/Hide
C16H20Cl2N6O4
 3
1
EC50 = 5970 nM
   TI
   LI
   LO
   TS
2
EC50 = 12900 nM
   TI
   LI
   LO
   TS
3
IC50 > 50000 nM
   TI
   LI
   LO
   TS
CP0411527
N-[(2S)-1-[(2S)-2-carbamoylpyrrolidin-1-yl]-3-(1-ethyl-2,5-diiodoimidazol-4-yl)-1-oxopropan-2-yl]pyrazine-2-carboxamide
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C18H21I2N7O3
 2
1
EC50 = 7210 nM
   TI
   LI
   LO
   TS
2
IC50 > 50000 nM
   TI
   LI
   LO
   TS
CP0849355
N-((S)-1-((S)-2-carbamoylpyrrolidin-1-yl)-3-(2,5-diiodo-1H-imidazol-4-yl)-1-oxopropan-2-yl)pyrazine-2-carboxamide
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C16H17I2N7O3
 2
1
EC50 = 11280 nM
   TI
   LI
   LO
   TS
2
IC50 > 50000 nM
   TI
   LI
   LO
   TS
CP0385688
(2S)-N-[(2S)-3-(1-benzyl-2-chloroimidazol-4-yl)-1-[(2S)-2-carbamoylpyrrolidin-1-yl]-1-oxopropan-2-yl]-5-oxopyrrolidine-2-carboxamide
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C23H27ClN6O4
 3
1
EC50 = 15720 nM
   TI
   LI
   LO
   TS
2
EC50 = 26270 nM
   TI
   LI
   LO
   TS
3
IC50 = 20400 nM
   TI
   LI
   LO
   TS
CP0515386
N-[(2S)-1-[(2S)-2-carbamoylpyrrolidin-1-yl]-3-(4-chloro-1H-imidazol-5-yl)-1-oxopropan-2-yl]pyrazine-2-carboxamide
   Show/Hide
C16H18ClN7O3
 2
1
EC50 = 19350 nM
   TI
   LI
   LO
   TS
2
IC50 > 50000 nM
   TI
   LI
   LO
   TS
CP0392457
(2S)-N-[(2S)-3-(1-benzyl-2-bromoimidazol-4-yl)-1-[(2S)-2-carbamoylpyrrolidin-1-yl]-1-oxopropan-2-yl]-5-oxopyrrolidine-2-carboxamide
   Show/Hide
C23H27BrN6O4
 2
1
EC50 > 50000 nM
   TI
   LI
   LO
   TS
2
IC50 > 50000 nM
   TI
   LI
   LO
   TS
CP0392456
(2S)-N-[(2S)-1-[(2S)-2-carbamoylpyrrolidin-1-yl]-3-(2,4-diiodo-1H-imidazol-5-yl)-1-oxopropan-2-yl]-5-oxopyrrolidine-2-carboxamide
   Show/Hide
C16H20I2N6O4
 2
1
EC50 > 50000 nM
   TI
   LI
   LO
   TS
2
IC50 > 50000 nM
   TI
   LI
   LO
   TS
Similar Protein(s) and Bioactivity Statistics
90% Identity
Protein ID Protein Name Protein Organism
PT04767 Thyrotropin-releasing hormone receptor Homo sapiens, Human