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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 | CHEMBL3780802 |
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Molecular formula | C18H24I2N6O4 |
IUPAC name | (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 |
Molecular weight | 642.237 |
Hydrogen bond acceptor | 5 |
Hydrogen bond donor | 3 |
XlogP | -0.8 |
Synonyms | BDBM50158399 |
Inchi Key | MYMJQRIIXGBYRP-DLOVCJGASA-N |
Inchi ID | InChI=1S/C18H24I2N6O4/c1-2-25-14(19)10(24-18(25)20)8-11(23-16(29)9-5-6-13(27)22-9)17(30)26-7-3-4-12(26)15(21)28/h9,11-12H,2-8H2,1H3,(H2,21,28)(H,22,27)(H,23,29)/t9-,11-,12-/m0/s1 |
PubChem CID | 127033191 |
ChEMBL | CHEMBL3780802 |
IUPHAR | N/A |
BindingDB | 50158399 |
DrugBank | N/A |
Structure | |
Lipinski's druglikeness | This ligand is heavier than 500 daltons. |
Parameter | Value | Reference | Database source |
---|---|---|---|
EC50 | 170.0 nM | PMID26854379 | BindingDB,ChEMBL |
EC50 | 249.0 nM | PMID26854379 | BindingDB,ChEMBL |
IC50 | 29340.0 nM | PMID26854379 | BindingDB,ChEMBL |
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