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TargetSubstance-P receptor
LigandBDBM50106391
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1506611 (CHEMBL3598468)
IC50 3.8±n/a nM
Citation Degnan, APTora, GOHan, YRajamani, RBertekap, RKrause, RDavis, CDHu, JMorgan, DTaylor, SJKrause, KLi, YWMattson, GCunningham, MATaber, MTLodge, NJBronson, JJGillman, KWMacor, JE Biaryls as potent, tunable dual neurokinin 1 receptor antagonists and serotonin transporter inhibitors. Bioorg Med Chem Lett25:3039-43 (2015) [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:
BDBM50106391
n/a
NameBDBM50106391
Synonyms:CHEMBL3596479
TypeSmall organic molecule
Emp. Form.C26H25F3N2O3
Mol. Mass.470.4835
SMILES[O-][N+](=O)c1ccc(cc1)-c1cc(COCC2(CCNCC2)c2ccccc2)cc(c1)C(F)(F)F
Structure
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