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Target
Histamine H1 receptor
Ligand
BDBM50156872
Substrate
n/a
Meas. Tech.
ChEMBL_429751 (CHEMBL914451)
IC50
125±n/a nM
Citation
 Fonquerna, S; Miralpeix, M; Pagès, L; Puig, C; Cardús, A; Antón, F; Cárdenas, A; Vilella, D; Aparici, M; Calaf, E; Prieto, J; Gras, J; Huerta, JM; Warrellow, G; Beleta, J; Ryder, H Synthesis and structure-activity relationships of novel histamine H1 antagonists: indolylpiperidinyl benzoic acid derivatives. J Med Chem 47:6326-37 (2004) [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:
BDBM50156872
Synonyms:
2-methoxy-5-[4-(1-thiophen-2-ylmethyl-1H-indol-3-yl)-piperidin-1-ylmethyl]benzoic acid | CHEMBL376202
Type:
Small organic molecule
Emp. Form.:
C27H28N2O3S
Mol. Mass.:
460.588
SMILES:
COc1ccc(CN2CCC(CC2)c2cn(Cc3cccs3)c3ccccc23)cc1C(O)=O
Structure:
Search PDB for entries with ligand similarity: