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Name | Thyrotropin-releasing hormone receptor |
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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 |
Name | protirelin |
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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 | 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 [ 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 | |
Lipinski's druglikeness | This ligand satisfies Lipinski's rule of five. |
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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