General Information of the Protein
Protein ID
PT09875
Protein Name
Thyrotropin-releasing hormone receptor 2
Sequence
MDGPSNVSLIHGDTTLGLPEYKVVSVFLVLLVCTLGIVGNAMVILVVLTSRDMHTPTNCYLVSLALADLLVLLAAGLPNVSDSLVGHWIYGRAGCLGITYFQYLGINVSSFSILAFTVERYIAICHPLRAQTVCTVARAKRIIAGIWGVTSLYCLLWFFLVDLNVRDNQRLECGYKVPRGLYLPIYLLDFAVFFIGPLLVTLVLYGLIGRILFQSPLSQEAWQKERQPHGQSEAAPGNCSRAKSSRKQATRMLAVVVLLFAVLWTPYRTLVLLNSFVAQPFLDPWVLLFCRTCVYTNSAVNPVVYSLMSQKFRAAFLKLCWCRAAGPQRRAARVLTSNYSAAQETSEGTEKM
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Protein Classification
Membrane receptor
>
Family A G protein-coupled receptor
>
Peptide receptor (family A GPCR)
>
Short peptide receptor (family A GPCR)
>
Neuropeptide receptor
Uniprot ID
Q9R297
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
Compound ID Compound Name Compound Formula
CP0253387
(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 = 2.4 nM
   TI
   LI
   LO
   TS
CP0253386
(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 = 2.8 nM
   TI
   LI
   LO
   TS
CP0067202
1-[3-(1H-4-imidazolyl)-2-(5-oxotetrahydro-1H-2-pyrrolylcarboxamido)propanoyl]tetrahydro-1H-2-pyrrolecarboxamide
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C16H22N6O4
 2
1
EC50 = 3 nM
   TI
   LI
   LO
   TS
2
Ki = 10 nM
   TI
   LI
   LO
   TS
CP0408102
1-[2-[5-oxo-(2S)-tetrahydro-1H-2-pyrrolylcarboxamido]-3-(2-propyl-1H-4-imidazolyl)-(2S)-propanoyl]-(2S)-tetrahydro-1H-2-pyrrolecarboxamide
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C19H28N6O4
 2
1
EC50 = 24 nM
   TI
   LI
   LO
   TS
2
Ki = 17000 nM
   TI
   LI
   LO
   TS
CP0162470
(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 = 29 nM
   TI
   LI
   LO
   TS
CP0162668
(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 = 340 nM
   TI
   LI
   LO
   TS
CP0497471
1-[3-(2-cyclopropyl-1H-4-imidazolyl)-2-[5-oxo-(2S)-tetrahydro-1H-2-pyrrolylcarboxamido]-(2S)-propanoyl]-(2S)-tetrahydro-1H-2-pyrrolecarboxamide
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C19H26N6O4
 2
1
EC50 = 410 nM
   TI
   LI
   LO
   TS
2
Ki > 100000 nM
   TI
   LI
   LO
   TS
CP0393980
1-[3-(2-cyclohexyl-1H-4-imidazolyl)-2-[5-oxo-(2S)-tetrahydro-1H-2-pyrrolylcarboxamido]-(2S)-propanoyl]-(2S)-tetrahydro-1H-2-pyrrolecarboxamide
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C22H32N6O4
 2
1
EC50 = 1100 nM
   TI
   LI
   LO
   TS
2
Ki > 100000 nM
   TI
   LI
   LO
   TS
CP0381542
1-[3-[2-(tert-butyl)-1H-4-imidazolyl]-2-[5-oxo-(2S)-tetrahydro-1H-2-pyrrolylcarboxamido]-(2S)-propanoyl]-(2S)-tetrahydro-1H-2-pyrrolecarboxamide
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C20H30N6O4
 2
1
EC50 = 1300 nM
   TI
   LI
   LO
   TS
2
Ki > 100000 nM
   TI
   LI
   LO
   TS
CP0431207
1-[3-(2-isopropyl-1H-4-imidazolyl)-2-[5-oxo-(2S)-tetrahydro-1H-2-pyrrolylcarboxamido]-(2S)-propanoyl]-(2S)-tetrahydro-1H-2-pyrrolecarboxamide
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C19H28N6O4
 2
1
EC50 = 1500 nM
   TI
   LI
   LO
   TS
2
Ki > 100000 nM
   TI
   LI
   LO
   TS
CP0359955
(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 = 1900 nM
   TI
   LI
   LO
   TS
CP0359956
(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 = 2000 nM
   TI
   LI
   LO
   TS
CP0162460
(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 = 3300 nM
   TI
   LI
   LO
   TS
CP0391620
1-[3-{2-[1-(1-adamantyl)ethyl]-1H-4-imidazolyl}-2-[5-oxo-(2S)-tetrahydro-1H-2-pyrrolylcarboxamido]-(2S)-propanoyl]-(2S)-tetrahydro-1H-2-pyrrolecarboxamide
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C26H36N6O4
 2
1
EC50 > 100000 nM
   TI
   LI
   LO
   TS
2
Ki > 100000 nM
   TI
   LI
   LO
   TS
CP0157755
(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
   TI
   LI
   LO
   TS
CP0157756
(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
   TI
   LI
   LO
   TS
CP0162459
(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
   TI
   LI
   LO
   TS
CP0253385
(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
   TI
   LI
   LO
   TS
CP0253388
(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
   TI
   LI
   LO
   TS
CP0307083
(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
   TI
   LI
   LO
   TS
CP0335691
(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
   TI
   LI
   LO
   TS
CP0335692
(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
   TI
   LI
   LO
   TS
CP0339773
(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
   TI
   LI
   LO
   TS
Biochemical Assays
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
 1
1 Ki = 10 nM
CP0253387
(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 = 13 nM
CP0253386
(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 = 34 nM
CP0162470
(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 = 290 nM
CP0162668
(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 = 21000 nM
CP0157755
(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
(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
(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
(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
(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
(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
(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
(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
(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
(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
(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
(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