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Target
Histamine H1 receptor
Ligand
BDBM50010044
Substrate
n/a
Meas. Tech.
ChEBML_84409
Ki
25±n/a nM
Citation
 Malleron, JL; Comte, MT; Gueremy, C; Peyronel, JF; Truchon, A; Blanchard, JC; Doble, A; Piot, O; Zundel, JL; Huon, C Naphthosultam derivatives: a new class of potent and selective 5-HT2 antagonists. J Med Chem 34:2477-83 (1991) [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:
BDBM50010044
Synonyms:
2-{3-[4-(4-Fluoro-phenyl)-piperazin-1-yl]-propyl}-2H-naphtho[1,8-cd]isothiazole 1,1-dioxide | 2-{3-[4-(4-Fluoro-phenyl)-piperazin-1-yl]-propyl}-2H-naphtho[1,8-cd]isothiazole 1,1-dioxide (Fenanserin) | 2-{3-[4-(4-Fluoro-phenyl)-piperazin-1-yl]-propyl}-2H-naphtho[1,8-cd]isothiazole 1,1-dioxide(Fananserin) | CHEMBL83894 | ChEMBL_131689 | FANANSERIN
Type:
Small organic molecule
Emp. Form.:
C23H24FN3O2S
Mol. Mass.:
425.519
SMILES:
Fc1ccc(cc1)N1CCN(CCCN2c3cccc4cccc(c34)S2(=O)=O)CC1
Structure:
Search PDB for entries with ligand similarity: