Target
Substance-P receptor
Ligand
BDBM50045033
Substrate
n/a
Meas. Tech.
ChEMBL_141634 (CHEMBL749536)
IC50
6±n/a nM
Citation
 Kucharczyk, NThurieau, CPaladino, JMorris, ADBonnet, JCanet, EKrause, JERegoli, DCouture, RFauchère, JL Tetrapeptide tachykinin antagonists: synthesis and modulation of the physicochemical and pharmacological properties of a new series of partially cyclic analogs. J Med Chem 36:1654-61 (1993) [PubMed]  Article 
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:
Homo sapiens (Human)
Description:
P25103
Residue:
407
Sequence:
MDNVLPVDSDLSPNISTNTSEPNQFVQPAWQIVLWAAAYTVIVVTSVVGNVVVMWIILAHKRMRTVTNYFLVNLAFAEASMAAFNTVVNFTYAVHNEWYYGLFYCKFHNFFPIAAVFASIYSMTAVAFDRYMAIIHPLQPRLSATATKVVICVIWVLALLLAFPQGYYSTTETMPSRVVCMIEWPEHPNKIYEKVYHICVTVLIYFLPLLVIGYAYTVVGITLWASEIPGDSSDRYHEQVSAKRKVVKMMIVVVCTFAICWLPFHIFFLLPYINPDLYLKKFIQQVYLAIMWLAMSSTMYNPIIYCCLNDRFRLGFKHAFRCCPFISAGDYEGLEMKSTRYLQTQGSVYKVSRLETTISTVVGAHEEEPEDGPKATPSSLDLTSNCSSRSDSKTMTESFSFSSNVLS
  
Inhibitor
Name:
BDBM50045033
Synonyms:
1N-[1-[1-benzyl(methyl)carbamoyl-2-phenyl-(1S)-ethylcarbamoyl]-2-(1-formyl-1H-3-indolyl)-(1R)-ethyl]-3-hydroxy-2-methylcarboxamidobutanamide | CHEMBL297776 | FR-113680
Type:
Small organic molecule
Emp. Form.:
C35H39N5O6
Mol. Mass.:
625.7141
SMILES:
CC(O)[C@H](NC(C)=O)C(=O)N[C@H](Cc1cn(C=O)c2ccccc12)C(=O)N[C@@H](Cc1ccccc1)C(=O)N(C)Cc1ccccc1
Structure:
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