Reaction Details |
| Report a problem with these data |
Target | Substance-P receptor |
---|
Ligand | BDBM21016 |
---|
Substrate/Competitor | n/a |
---|
Meas. Tech. | ChEMBL_603837 (CHEMBL1045632) |
---|
Ki | 134±n/a nM |
---|
Citation | Yamamoto, T; Nair, P; Ma, SW; Davis, P; Yamamura, HI; Vanderah, TW; Porreca, F; Lai, J; Hruby, 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
|
|
|
BDBM21016 |
---|
n/a |
---|
Name | BDBM21016 |
Synonyms: | CHEMBL22870 | L 732138 | L-732,138 | L732138 | N-acetyltryptophan 3,5-bis(trifluoromethyl)benzyl ester | [3,5-bis(trifluoromethyl)phenyl]methyl (2S)-2-acetamido-3-(1H-indol-3-yl)propanoate |
Type | Small organic molecule |
Emp. Form. | C22H18F6N2O3 |
Mol. Mass. | 472.3803 |
SMILES | CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)OCc1cc(cc(c1)C(F)(F)F)C(F)(F)F |r| |
Structure |
|