Reaction Details |
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Target | Substance-P receptor |
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Ligand | BDBM50070383 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1467478 (CHEMBL3411101) |
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Ki | 1020±n/a nM |
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Citation | Guillemyn, K; Kleczkowska, P; Lesniak, A; Dyniewicz, J; Van der Poorten, O; Van den Eynde, I; Keresztes, A; Varga, E; Lai, J; Porreca, F; Chung, NN; Lemieux, C; Mika, J; Rojewska, E; Makuch, W; Van Duppen, J; Przewlocka, B; Vanden Broeck, J; Lipkowski, AW; Schiller, PW; Tourwé, D; Ballet, S Synthesis and biological evaluation of compact, conformationally constrained bifunctional opioid agonist - neurokinin-1 antagonist peptidomimetics. Eur J Med Chem92:64-77 (2015) [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 | NK1R_HUMAN | Neurokinin 1 receptor | Neurokinin-1 (NK-1) | Neuromedin-1 receptor (NK-1R) | SPR | TAC1R | TACR1 | Tachykinin receptor 1 | Tachykinin receptor 1 (NK1) | tachykinin |
Type: | G Protein-Coupled Receptor (GPCR) |
Mol. Mass.: | 46254.43 |
Organism: | Homo sapiens (Human) |
Description: | P25103 |
Residue: | 407 |
Sequence: | MDNVLPVDSDLSPNISTNTSEPNQFVQPAWQIVLWAAAYTVIVVTSVVGNVVVMWIILAH
KRMRTVTNYFLVNLAFAEASMAAFNTVVNFTYAVHNEWYYGLFYCKFHNFFPIAAVFASI
YSMTAVAFDRYMAIIHPLQPRLSATATKVVICVIWVLALLLAFPQGYYSTTETMPSRVVC
MIEWPEHPNKIYEKVYHICVTVLIYFLPLLVIGYAYTVVGITLWASEIPGDSSDRYHEQV
SAKRKVVKMMIVVVCTFAICWLPFHIFFLLPYINPDLYLKKFIQQVYLAIMWLAMSSTMY
NPIIYCCLNDRFRLGFKHAFRCCPFISAGDYEGLEMKSTRYLQTQGSVYKVSRLETTIST
VVGAHEEEPEDGPKATPSSLDLTSNCSSRSDSKTMTESFSFSSNVLS
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BDBM50070383 |
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n/a |
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Name | BDBM50070383 |
Synonyms: | CHEMBL3408732 |
Type | Small organic molecule |
Emp. Form. | C40H54N8O5 |
Mol. Mass. | 726.9074 |
SMILES | [H][C@@]1(Cc2ccccc2CN(CC(=O)N(CC(C)C)Cc2ccccc2)C1=O)NC(=O)[C@@H](CCCNC(N)=N)NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C |r| |
Structure |
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