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TargetHistamine H1 receptor
LigandBDBM22567
Substrate/Competitorn/a
Meas. Tech.ChEMBL_714788
IC50 1.5±n/a nM
Citation Hayashi, SNakata, EMorita, AMizuno, KYamamura, KKato, AOhashi, K Discovery of {1-[4-(2-{hexahydropyrrolo[3,4-c]pyrrol-2(1H)-yl}-1H-benzimidazol-1-yl)piperidin-1-yl]cyclooctyl}methanol, systemically potent novel non-peptide agonist of nociceptin/orphanin FQ receptor as analgesic for the treatment of neuropathic pain: design, synthesis, and structure-activity rela Bioorg Med Chem18:7675-99 (2010) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Histamine H1 receptor
Name:Histamine H1 receptor
Synonyms:HISTAMINE H1
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:
MSFLPGMTPVTLSNFSWALEDRMLEGNSTTTPTRQLMPLVVVLSSVSLVTVALNLLVLYA
VRSERKLHTVGNLYIVSLSVADLIVGAVVMPMSILYLHRSAWILGRPLCLFWLSMDYVAS
TASIFSVFILCIDRYRSVQQPLRYLRYRTKTRASATILGAWLLSFLWVIPILGWHHFMAP
TSEPREKKCETDFYDVTWFKVMTAIINFYLPTLLMLWFYIRIYKAVRRHCQHRQLINSSL
PSFSEMKLKLENAKVDTRRMGKESPWEDPKRCSKDASGVHTPMPSSQHLVDMPCAAVLSE
DEGGEVGTRQMPMLAVGDGRCCEALNHMHSQLELSGQSRATHSISARPEEWTVVDGQSFP
ITDSDTSTEAAPMGGQPRSGSNSGLDYIKFTWRRLRSHSRQYTSGLHLNRERKAAKQLGC
IMAAFILCWIPYFVFFMVIAFCKSCSNEPVHMFTIWLGYLNSTLNPLIYPLCNENFRKTF
KRILRIPP
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  Blast E-value cutoff:
BDBM22567
NameBDBM22567
Synonyms:3H]pyrilamine | CHEMBL511 | Dorantamin | MEPYRAMINE | Mepyramine | N-(4-methoxybenzyl)-N ,N -dimethyl-N-pyridin-2-ylethane-1,2-diamine | N-[2-(dimethylamino)ethyl]-N-[(4-methoxyphenyl)methyl]pyridin-2-amine | PYRILAMINE | Pyranisamine | [3H]mepyramine | [3H]pyrilamine
Typeradiolabeled ligand
Emp. Form.C17H23N3O
Mol. Mass.285.384
SMILESCOc1ccc(CN(CCN(C)C)c2ccccn2)cc1
Structure
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n/a