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Target
Substance-P receptor
Ligand
BDBM362855
Substrate
n/a
Meas. Tech.
Binding Assay
Ki
12000±n/a nM
Citation
 Hoveyda, H; Dutheuil, G; Fraser, G N-acyl-(3-substituted)-(8-methyl)-5,6-dihydro-[1,2,4]triazolo[4,3-a] pyrazines as selective NK-3 receptor antagonists, pharmaceutical composition, methods for use in NK-3 receptor-mediated disorders US Patent  US9840508 Publication Date 12/12/2017 
Target
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:
Human
Description:
P25103
Residue:
407
Sequence:
MDNVLPVDSDLSPNISTNTSEPNQFVQPAWQIVLWAAAYTVIVVTSVVGNVVVMWIILAHKRMRTVTNYFLVNLAFAEASMAAFNTVVNFTYAVHNEWYYGLFYCKFHNFFPIAAVFASIYSMTAVAFDRYMAIIHPLQPRLSATATKVVICVIWVLALLLAFPQGYYSTTETMPSRVVCMIEWPEHPNKIYEKVYHICVTVLIYFLPLLVIGYAYTVVGITLWASEIPGDSSDRYHEQVSAKRKVVKMMIVVVCTFAICWLPFHIFFLLPYINPDLYLKKFIQQVYLAIMWLAMSSTMYNPIIYCCLNDRFRLGFKHAFRCCPFISAGDYEGLEMKSTRYLQTQGSVYKVSRLETTISTVVGAHEEEPEDGPKATPSSLDLTSNCSSRSDSKTMTESFSFSSNVLS
  
Inhibitor
Name:
BDBM362855
Synonyms:
(R)-(4-chloro-3- fluorophenyl)(8-methyl-3-(2- (trifluoromethyl)thiazol-4-yl)- 5,6-dihydro- [1,2,4]triazolo[4,3-a]pyrazin- 7(8H)-yl)methanone | US9840508, Compound 17
Type:
Small organic molecule
Emp. Form.:
C17H12ClF4N5OS
Mol. Mass.:
445.822
SMILES:
C[C@H]1N(CCn2c1nnc2-c1csc(n1)C(F)(F)F)C(=O)c1ccc(Cl)c(F)c1 |r|
Structure:
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