Reaction Details |
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Target | Substance-P receptor |
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Ligand | BDBM50243425 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_491574 (CHEMBL944220) |
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Ki | 0.2±n/a nM |
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Citation | Paliwal, S; Reichard, GA; Shah, S; Wrobleski, ML; Wang, C; Stengone, C; Tsui, HC; Xiao, D; Duffy, RA; Lachowicz, JE; Nomeir, AA; Varty, GB; Shih, NY Discovery of a novel, potent and orally active series of gamma-lactams as selective NK1 antagonists. Bioorg Med Chem Lett18:4168-71 (2008) [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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BDBM50243425 |
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n/a |
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Name | BDBM50243425 |
Synonyms: | 1-((3S,5S)-5-(((R)-1-(3,5-bis(trifluoromethyl)phenyl)ethoxy)methyl)-2-oxo-5-phenylpyrrolidin-3-yl)pyrrolidin-2-one | CHEMBL453054 |
Type | Small organic molecule |
Emp. Form. | C25H24F6N2O3 |
Mol. Mass. | 514.4601 |
SMILES | C[C@@H](OC[C@]1(C[C@H](N2CCCC2=O)C(=O)N1)c1ccccc1)c1cc(cc(c1)C(F)(F)F)C(F)(F)F |r| |
Structure |
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