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TargetSubstance-P receptor
LigandBDBM50428792
Substrate/Competitorn/a
Meas. Tech.ChEMBL_948440 (CHEMBL2342730)
IC50 3.0±n/a nM
Citation Gillman, KWParker, MFSilva, MDegnan, APTora, GOLodge, NJLi, YWLelas, STaber, MKrause, RGBertekap, RLNewton, AEPieschl, RLLengyel, KDJohnson, KATaylor, SJBronson, JJMacor, JE Design, optimization, and in vivo evaluation of a series of pyridine derivatives with dual NK1 antagonism and SERT inhibition for the treatment of depression. Bioorg Med Chem Lett23:407-11 (2012) [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 | 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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  Blast E-value cutoff:
BDBM50428792
n/a
NameBDBM50428792
Synonyms:CHEMBL2333620
TypeSmall organic molecule
Emp. Form.C25H33F4N3O
Mol. Mass.467.5426
SMILESCCC(CC)Nc1cc(cc(COCC2(CCN(C)CC2)c2ccc(F)cc2)n1)C(F)(F)F
Structure
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