Target
Histamine H1 receptor
Ligand
BDBM50228551
Substrate
n/a
Meas. Tech.
ChEMBL_452856 (CHEMBL903099)
Kd
>1000±n/a nM
Citation
 Procopiou, PAAncliff, RABamford, MJBrowning, CConnor, HDavies, SFogden, YCHodgson, STHolmes, DSLooker, BEMorriss, KMParr, CAPickup, EASehmi, SSWhite, GVWatts, CJWilson, DMWoodrow, MD 4-acyl-1-(4-aminoalkoxyphenyl)-2-ketopiperazines as a novel class of non-brain-penetrant histamine H3 receptor antagonists. J Med Chem 50:6706-17 (2007) [PubMed]  Article 
Target
Name:
Histamine H1 receptor
Synonyms:
HISTAMINE H1 | HRH1 | HRH1_CAVPO
Type:
G Protein-Coupled Receptor (GPCR)
Mol. Mass.:
55641.53
Organism:
Cavia porcellus (domestic guinea pig)
Description:
Guinea pig cerebellum was used in binding assay.
Residue:
488
Sequence:
MSFLPGMTPVTLSNFSWALEDRMLEGNSTTTPTRQLMPLVVVLSSVSLVTVALNLLVLYAVRSERKLHTVGNLYIVSLSVADLIVGAVVMPMSILYLHRSAWILGRPLCLFWLSMDYVASTASIFSVFILCIDRYRSVQQPLRYLRYRTKTRASATILGAWLLSFLWVIPILGWHHFMAPTSEPREKKCETDFYDVTWFKVMTAIINFYLPTLLMLWFYIRIYKAVRRHCQHRQLINSSLPSFSEMKLKLENAKVDTRRMGKESPWEDPKRCSKDASGVHTPMPSSQHLVDMPCAAVLSEDEGGEVGTRQMPMLAVGDGRCCEALNHMHSQLELSGQSRATHSISARPEEWTVVDGQSFPITDSDTSTEAAPMGGQPRSGSNSGLDYIKFTWRRLRSHSRQYTSGLHLNRERKAAKQLGCIMAAFILCWIPYFVFFMVIAFCKSCSNEPVHMFTIWLGYLNSTLNPLIYPLCNENFRKTFKRILRIPP
  
Inhibitor
Name:
BDBM50228551
Synonyms:
4-(4-fluoro-benzoyl)-1-[4-(3-piperidin-1-yl-propoxy)-phenyl]-piperazin-2-one formic acid | CHEMBL239975 | CHEMBL240185
Type:
Small organic molecule
Emp. Form.:
C25H30FN3O3
Mol. Mass.:
439.5224
SMILES:
Fc1ccc(cc1)C(=O)N1CCN(C(=O)C1)c1ccc(OCCCN2CCCCC2)cc1
Structure:
Search PDB for entries with ligand similarity: