Reaction Details |
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Target | Substance-P receptor |
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Ligand | BDBM50439326 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_977574 (CHEMBL2423356) |
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Ki | 1.1±n/a nM |
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Citation | Nair, P; Yamamoto, T; Largent-Milnes, TM; Cowell, S; Kulkarni, V; Moye, S; Navratilova, E; Davis, P; Ma, SW; Vanderah, TW; Lai, J; Porreca, F; Hruby, VJ Truncation of the peptide sequence in bifunctional ligands with mu and delta opioid receptor agonist and neurokinin 1 receptor antagonist activities. Bioorg Med Chem Lett23:4975-8 (2013) [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 |
Synonyms: | NK-1 receptor | NK-1R | NK1 Receptor | NK1R_RAT | Neurokinin 1 receptor | Neurokinin NK1 | SPR | Substance-P receptor | Tac1r | Tachykinin receptor 1 | Tacr1 |
Type: | G Protein-Coupled Receptor (GPCR) |
Mol. Mass.: | 46371.54 |
Organism: | Rattus norvegicus (rat) |
Description: | Competition binding assays were carried out using membrane preparations from transfected CHO cells that constitutively expressed the rat NK1 receptor. |
Residue: | 407 |
Sequence: | MDNVLPMDSDLFPNISTNTSESNQFVQPTWQIVLWAAAYTVIVVTSVVGNVVVIWIILAH
KRMRTVTNYFLVNLAFAEACMAAFNTVVNFTYAVHNVWYYGLFYCKFHNFFPIAALFASI
YSMTAVAFDRYMAIIHPLQPRLSATATKVVIFVIWVLALLLAFPQGYYSTTETMPSRVVC
MIEWPEHPNRTYEKAYHICVTVLIYFLPLLVIGYAYTVVGITLWASEIPGDSSDRYHEQV
SAKRKVVKMMIVVVCTFAICWLPFHVFFLLPYINPDLYLKKFIQQVYLASMWLAMSSTMY
NPIIYCCLNDRFRLGFKHAFRCCPFISAGDYEGLEMKSTRYLQTQSSVYKVSRLETTIST
VVGAHEEEPEEGPKATPSSLDLTSNGSSRSNSKTMTESSSFYSNMLA
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BDBM50439326 |
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n/a |
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Name | BDBM50439326 |
Synonyms: | CHEMBL2419537 |
Type | Small organic molecule |
Emp. Form. | C57H67F6N9O10S |
Mol. Mass. | 1184.252 |
SMILES | CSCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)OCc1cc(cc(c1)C(F)(F)F)C(F)(F)F |r| |
Structure |
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