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Target
Substance-P receptor
Ligand
BDBM50264407
Substrate
n/a
Meas. Tech.
ChEMBL_539196 (CHEMBL1024700)
Ki
700±n/a nM
Citation
 Yamamoto, T; Nair, P; Jacobsen, NE; Davis, P; Ma, SW; Navratilova, E; Moye, S; Lai, J; Yamamura, HI; Vanderah, TW; Porreca, F; Hruby, 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 Chem 51:6334-47 (2008) [PubMed]  Article 
Target
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:
MDNVLPMDSDLFPNISTNTSESNQFVQPTWQIVLWAAAYTVIVVTSVVGNVVVIWIILAHKRMRTVTNYFLVNLAFAEACMAAFNTVVNFTYAVHNVWYYGLFYCKFHNFFPIAALFASIYSMTAVAFDRYMAIIHPLQPRLSATATKVVIFVIWVLALLLAFPQGYYSTTETMPSRVVCMIEWPEHPNRTYEKAYHICVTVLIYFLPLLVIGYAYTVVGITLWASEIPGDSSDRYHEQVSAKRKVVKMMIVVVCTFAICWLPFHVFFLLPYINPDLYLKKFIQQVYLASMWLAMSSTMYNPIIYCCLNDRFRLGFKHAFRCCPFISAGDYEGLEMKSTRYLQTQSSVYKVSRLETTISTVVGAHEEEPEEGPKATPSSLDLTSNGSSRSNSKTMTESSSFYSNMLA
  
Inhibitor
Name:
BDBM50264407
Synonyms:
CHEMBL448998 | Tyr-D-Ala-Gly-Phe-Met-Pro-Leu-Trp-NH-Bzl
Type:
Small organic molecule
Emp. Form.:
C57H72N10O9S
Mol. Mass.:
1073.308
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)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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