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GPCR

Name	Thyrotropin-releasing hormone receptor
Species	Mus musculus (Mouse)
Gene	Trhr
Synonym	Thyroliberin receptor TRH receptor TRH-R TRH-R1 TRH1 receptor
Disease	N/A for non-human GPCRs
Length	393
Amino acid sequence	MENDTVSEMNQTELQPQAAVALEYQVVTILLVVIICGLGIVGNIMVVLVVMRTKHMRTPTNCYLVSLAVADLMVLVAAGLPNITDSIYGSWVYGYVGCLCITYLQYLGINASSCSITAFTIERYIAICHPIKAQFLCTFSRAKKIIIFVWAFTSIYCMLWFFLLDLNISTYKNAVVVSCGYKISRNYYSPIYLMDFGVFYVVPMILATVLYGFIARILFLNPIPSDPKENSKMWKNDSIHQNKNLNLNATNRCFNSTVSSRKQVTKMLAVVVILFALLWMPYRTLVVVNSFLSSPFQENWFLLFCRICIYLNSAINPVIYNLMSQKFRAAFRKLCNCKQKPTEKAANYSVALNYSVIKESDRFSTELEDITVTDTYVSTTKVSFDDTCLASEN
UniProt	P21761
Protein Data Bank	N/A
GPCR-HGmod model	N/A
3D structure model	No available structures or models
BioLiP	N/A
Therapeutic Target Database	N/A
ChEMBL	CHEMBL2467
IUPHAR	N/A
DrugBank	N/A

Ligand

Name	protirelin
Molecular formula	C16H22N6O4
IUPAC name	(2S)-N-[(2S)-1-[(2S)-2-carbamoylpyrrolidin-1-yl]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]-5-oxopyrrolidine-2-carboxamide
Molecular weight	362.39
Hydrogen bond acceptor	5
Hydrogen bond donor	4
XlogP	-2.5
Synonyms	pyroglutamyl-histidyl-prolinamide 2-Pyrrolidinecarboxamide, N-[1-[(2-Carbamoyl-1-pyrrolidinyl)carbonyl]-2-imidazol-4-ylethyl]-5-oxo-, (S,S,S)- Stimu-TSH Thypinone ABBOTT-38579 Thyrotrophin releasing hormone CHEBI:35940 Thyrotropin-releasing factor TSH-releasing factor FT-0638410 L-Pyroglutamyl-L-histidinyl-L-prolinamide PR-546 Protirelin, European Pharmacopoeia (EP) Reference Standard (Pyro)-L-glutamic acid-L-histidine-L-proline-NH2 Rifathyroin 22365-17-9 Synthetic thyrotropin-releasing hormone 77666-61-6 Thyroid releasing hormone BDBM50072394 Thyrotropic releasing hormone CP-236 Tox21_111939 DSSTox_GSID_23533 UNII-5Y5F15120W Hirtonin L-Pyroglutamyl-L-histidyl-L-prolineamide (2S)-N-[(1S)-2-[(2S)-2-carbamoylpyrrolidino]-1-(1H-imidazol-5-ylmethyl)-2-keto-ethyl]-5-keto-pyrrolidine-2-carboxamide Protireline 1-(3-(1H-Imidazol-5-yl)-2-([(5-oxo-2-pyrrolidinyl)carbonyl]amino)propanoyl)-2-pyrrolidinecarboxamide # 117217-40-0 SCHEMBL19825647 39422-15-6 Synthetic tsh-releasing factor AB0011512 Thyrothropin relasing hormone CAS-24305-27-9 Thyrotropin releasing hormone, >=98% (HPLC), powder D08BTB trh-sr EINECS 246-143-4 KS-00002WUW NCGC00160616-01 Protirelin tartrate (2S)-N-[(2S)-1-[(2S)-2-carbamoylpyrrolidin-1-yl]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]-5-oxopyrrolidine-2-carboxamide Protirelinum [INN-Latin] Relefact TRH (TN) Synthetic thyrotopin releasing factor 53935-32-3 (1:1 tartrate) Thyrefact AC1LCWUZ Thyrotropic hormone-releasing factor Thyrotropin-releasing factor (pig) DB09421 TSH-releasing hormone FT-0639185 L-Pyroglutamyl-L-histidyl-L-prolinamide Prolinamide, 1-[N-(5-oxo-L-prolyl)-L-histidyl]-, L- Protirelina (S)-N-((S)-1-((S)-2-carbamoylpyrrolidin-1-yl)-3-(1H-imidazol-4-yl)-1-oxopropan-2-yl)-5-oxopyrrolidine-2-carboxamide Ro 8-6270/9 24305-27-9 Synthetic TRF 9015-91-2 Thyroid-stimulating hormone-releasing factor C03958 Thyrotropic-releasing factor CS-7080 TRF DSSTox_RID_77067 XNSAINXGIQZQOO-SRVKXCTJSA-N HS-2023 Lopremone Protirelin (JP17/USAN/INN) (2S)-N-[(2S)-1-[(2S)-2-aminocarbonylpyrrolidin-1-yl]-3-(1H-imidazol-5-yl)-1-oxidanylidene-propan-2-yl]-5-oxidanylidene-pyrrolidine-2-carboxamide Protireline [INN-French] 1-[3-(1H-4-imidazolyl)-2-(5-oxotetrahydro-1H-2-pyrrolylcarboxamido)propanoyl]tetrahydro-1H-2-pyrrolecarboxamide 2-Pyrrolidinecarboxamide, N-[1-[(2-carbamoyl-1-pyrrolidinyl)carbonyl]-2-imidazol-4-ylethyl]-5-oxo-, SCHEMBL33419 5-Oxo-L-prolyl-L-histidyl-L-prolinamide Synthetic tsh-releasing hormone Abbott 38579 Thyrotrophic hormone releasing hormone CCRIS 2593 Thyrotropin releasing hormone, powder, gamma-irradiated, cell culture tested D0E9TD TRH-SR, Takeda FDA 1725 L-Prolinamide, 5-oxo-L-prolyl-L-histidyl- PR 546 Protirelin [USAN:INN:BAN:JAN] (2S)-N-[(2S)-1-[(2S)-2-carbamoylpyrrolidin-1-yl]-3-(3H-imidazol-4-yl)-1-oxopropan-2-yl]-5-oxopyrrolidine-2-carboxamide PyroGlu-His-prolinamide Relefact-TRH 22365-02-2 Synthetic thyrotropin-releasing factor 5Y5F15120W THYREL TRH AKOS015994636 Thyrotropic hormone-releasing hormone CHEMBL1472 Thyrotropin-releasing hormone DSSTox_CID_3533 TSH-RF GTPL2139 L-Pyroglutamyl-L-histidyl-L-proline amide Prolinamide, 5-oxo-L-prolyl-L-histidyl-, L- Protirelina [INN-Spanish] (S)-N-((S)-1-((S)-2-carbamoylpyrrolidin-1-yl)-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl)-5-oxopyrrolidine-2-carboxamide 11096-37-0 s4680 305T279 Synthetic TRH A-38579 Thyroliberin C16H22N6O4 Thyrotropin releasing hormone D00176 TRH DTXSID0023533 ZINC4096261 HY-P0002 MolPort-006-124-300 Protirelin acetate (2S)-N-[(2S)-1-[(2S)-2-carbamoylpyrrolidin-1-yl]-3-(1H-imidazol-4-yl)-1-oxopropan-2-yl]-5-oxopyrrolidine-2-carboxamide Protirelinum [ Show all ]
Inchi Key	XNSAINXGIQZQOO-SRVKXCTJSA-N
Inchi ID	InChI=1S/C16H22N6O4/c17-14(24)12-2-1-5-22(12)16(26)11(6-9-7-18-8-19-9)21-15(25)10-3-4-13(23)20-10/h7-8,10-12H,1-6H2,(H2,17,24)(H,18,19)(H,20,23)(H,21,25)/t10-,11-,12-/m0/s1
PubChem CID	638678
ChEMBL	CHEMBL1472
IUPHAR	2139
BindingDB	50072394
DrugBank	DB09421
Structure SDF download
Lipinski's druglikeness	This ligand satisfies Lipinski's rule of five.

Experimental Data

Parameter	Value	Reference	Database source
Activity	334.0 cpm	PMID26854379	ChEMBL
Activity	393.0 cpm	PMID26854379	ChEMBL
Activity	513.46 cpm	PMID26854379	ChEMBL
Activity	719.25 cpm	PMID26854379	ChEMBL
EC50	0.49 nM	PMID9873682	BindingDB
EC50	0.49 nM	PMID9873682	ChEMBL
EC50	0.68 nM	PMID8648595	ChEMBL
EC50	0.68 nM	PMID8648595	BindingDB
EC50	1.0 nM	PMID26216015	BindingDB
EC50	1.0 nM	PMID26854379, PMID26216015	BindingDB,ChEMBL
EC50	3.2 nM	PMID26854379	BindingDB,ChEMBL
IC50	2.6 nM	PMID26216015	BindingDB,ChEMBL
IC50	26.0 nM	PMID26854379	BindingDB,ChEMBL
Ki	10.0 nM	PMID8648595	BindingDB,ChEMBL
Ki	23.0 nM	PMID9873682	BindingDB,ChEMBL

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