| Reaction Details |
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 | Report a problem with these data |
| Target | Substance-P receptor |
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| Ligand | BDBM86055 |
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| Substrate/Competitor | n/a |
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| Ki | 1.15±n/a nM |
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| Comments | PDSP_2982 |
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| Citation |  Emonds-Alt, X; Proietto, V; Steinberg, R; Oury-Donat, F; Vigé, X; Vilain, P; Naline, E; Daoui, S; Advenier, C; Le Fur, G; Maffrand, JP; Soubrié, P; Pascal, M SSR240600 [(R)-2-(1-[2-[4-[2-[3,5-bis(trifluoromethyl)phenyl]acetyl]-2-(3,4-dichlorophenyl)-2-morpholinyl]ethyl]- 4-piperidinyl)-2-methylpropanamide], a centrally active nonpeptide antagonist of the tachykinin neurokinin-1 receptor: I. biochemical and pharmacological characterization. J Pharmacol Exp Ther303:1171-9 (2002) [PubMed] Article |
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| More Info.: | Get all data from this article |
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| Substance-P receptor |
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| Name: | Substance-P receptor |
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| Synonyms: | NK-1 receptor | NK-1R | NK1 Receptor | NK1R_RAT | Neurokinin 1 receptor | Neurokinin NK1 | SPR | Substance-P receptor | Tac1r | Tachykinin receptor 1 | Tacr1 |
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| Type: | G Protein-Coupled Receptor (GPCR) |
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| Mol. Mass.: | 46371.54 |
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| Organism: | Rattus norvegicus (rat) |
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| Description: | Competition binding assays were carried out using membrane preparations from transfected CHO cells that constitutively expressed the rat NK1 receptor. |
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| Residue: | 407 |
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| Sequence: | MDNVLPMDSDLFPNISTNTSESNQFVQPTWQIVLWAAAYTVIVVTSVVGNVVVIWIILAH
KRMRTVTNYFLVNLAFAEACMAAFNTVVNFTYAVHNVWYYGLFYCKFHNFFPIAALFASI
YSMTAVAFDRYMAIIHPLQPRLSATATKVVIFVIWVLALLLAFPQGYYSTTETMPSRVVC
MIEWPEHPNRTYEKAYHICVTVLIYFLPLLVIGYAYTVVGITLWASEIPGDSSDRYHEQV
SAKRKVVKMMIVVVCTFAICWLPFHVFFLLPYINPDLYLKKFIQQVYLASMWLAMSSTMY
NPIIYCCLNDRFRLGFKHAFRCCPFISAGDYEGLEMKSTRYLQTQSSVYKVSRLETTIST
VVGAHEEEPEEGPKATPSSLDLTSNGSSRSNSKTMTESSSFYSNMLA
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| BDBM86055 |
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| n/a |
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| Name | BDBM86055 |
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| Synonyms: | SSR240600 |
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| Type | Small organic molecule |
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| Emp. Form. | C31H35Cl2F6N3O3 |
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| Mol. Mass. | 682.524 |
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| SMILES | CC(C)(C1CCN(CCC2(CN(CCO2)C(=O)Cc2cc(cc(c2)C(F)(F)F)C(F)(F)F)c2ccc(Cl)c(Cl)c2)CC1)C(N)=O |
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| Structure | 
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