Reaction Details Report a problem with these data
Target
Histamine H1 receptor
Ligand
BDBM24226
Substrate
n/a
Ki
0.8±n/a nM
Comments
PDSP_329
Citation
Schotte, A; Janssen, PF; Gommeren, W; Luyten, WH; Van Gompel, P; Lesage, AS; De Loore, K; Leysen, JE Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding. Psychopharmacology (Berl) 124:57-73 (1996) [PubMed] Article
More Info.:
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:
BDBM24226
Synonyms:
1-[(4-fluorophenyl)methyl]-N-{1-[2-(4-methoxyphenyl)ethyl]piperidin-4-yl}-1H-1,3-benzodiazol-2-amine | ASTEMIZOLE | Astemizole, [O-Methyl-3H] | CHEMBL296419 | Hismanal | Histaminos | [3H]-ASTEMIZOLE | [3H]Astemizole | cid_2247 | med.21724, Compound Astemizole
Type:
Radiolabeled ligand
Emp. Form.:
C28H31FN4O
Mol. Mass.:
458.5703
SMILES:
COc1ccc(CCN2CCC(CC2)Nc2nc3ccccc3n2Cc2ccc(F)cc2)cc1