Target
Histamine H1 receptor
Ligand
BDBM50007541
Substrate
n/a
Meas. Tech.
ChEBML_83771
IC50
11900±n/a nM
Citation
 Sleevi, MCCale, ADGero, TWJaques, LWWelstead, WJJohnson, AFKilpatrick, BFDemian, INolan, JCJenkins, H Optical isomers of rocastine and close analogues: synthesis and H1 antihistaminic activity of its enantiomers and their structural relationship to the classical antihistamines. J Med Chem 34:1314-28 (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:
BDBM50007541
Synonyms:
3-Chloro-8-(2-dimethylamino-ethyl)-6-methyl-7,8-dihydro-6H-9-oxa-1,6-diaza-benzocycloheptene-5-thione | CHEMBL283760
Type:
Small organic molecule
Emp. Form.:
C13H18ClN3OS
Mol. Mass.:
299.82
SMILES:
CN(C)CC[C@H]1CN(C)C(=S)c2cc(Cl)cnc2O1
Structure:
Search PDB for entries with ligand similarity: