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TargetSubstance-P receptor
LigandBDBM50304489
Substrate/Competitorn/a
Meas. Tech.ChEMBL_603837 (CHEMBL1045632)
Ki 7.1±n/a nM
Citation Yamamoto, TNair, PMa, SWDavis, PYamamura, HIVanderah, TWPorreca, FLai, JHruby, 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
More Info.:Get all data from this article,  Assay Method
 
Substance-P receptor
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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  Blast E-value cutoff:
BDBM50304489
n/a
NameBDBM50304489
Synonyms:CHEMBL592969 | H-Tyr-c[D-Cys-Gly-Phe-Nle-Pro-D-Cys]-Trp-NH-[3',5'-(CF3)2Bzl]
TypeSmall organic molecule
Emp. Form.C57H64F6N10O9S2
Mol. Mass.1211.3
SMILESCCCC[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@@H](CSSC[C@@H](NC(=O)[C@@H]2CCCN2C1=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1cc(cc(c1)C(F)(F)F)C(F)(F)F)NC(=O)[C@@H](N)Cc1ccc(O)cc1 |r|
Structure
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