| Reaction Details |
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 | Report a problem with these data |
| Target | Substance-P receptor |
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| Ligand | BDBM50304491 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_603837 (CHEMBL1045632) |
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| Ki | 45±n/a nM |
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| Citation |  Yamamoto, T; Nair, P; Ma, SW; Davis, P; Yamamura, HI; Vanderah, TW; Porreca, F; Lai, J; Hruby, VJ The biological activity and metabolic stability of peptidic bifunctional compounds that are opioid receptor agonists and neurokinin-1 receptor antagonists with a cystine moiety. Bioorg Med Chem17:7337-43 (2009) [PubMed] Article |
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| More Info.: | Get all data from this article, Assay Method |
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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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| BDBM50304491 |
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| n/a |
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| Name | BDBM50304491 |
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| Synonyms: | CHEMBL611925 | H-Tyr-c[D-Cys-Gly-Phe-D-Cys]-Pro-Leu-Trp-NH-[3',5'-(CF3)2Bzl] |
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| Type | Small organic molecule |
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| Emp. Form. | C57H64F6N10O9S2 |
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| Mol. Mass. | 1211.3 |
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| SMILES | CC(C)C[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H]1CSSC[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1cc(cc(c1)C(F)(F)F)C(F)(F)F |r| |
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| Structure | 
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