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TargetSubstance-P receptor
LigandBDBM50264407
Substrate/Competitorn/a
Meas. Tech.ChEMBL_539196 (CHEMBL1024700)
IC50 2512±n/a nM
Citation Yamamoto, TNair, PJacobsen, NEDavis, PMa, SWNavratilova, EMoye, SLai, JYamamura, HIVanderah, TWPorreca, FHruby, VJ The importance of micelle-bound states for the bioactivities of bifunctional peptide derivatives for delta/mu opioid receptor agonists and neurokinin 1 receptor antagonists. J Med Chem51:6334-47 (2008) [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:
BDBM50264407
n/a
NameBDBM50264407
Synonyms:CHEMBL448998 | Tyr-D-Ala-Gly-Phe-Met-Pro-Leu-Trp-NH-Bzl
TypeSmall organic molecule
Emp. Form.C57H72N10O9S
Mol. Mass.1073.308
SMILESCSCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1ccccc1 |r|
Structure
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