Target
Histamine H1 receptor
Ligand
BDBM50317865
Substrate
n/a
Meas. Tech.
ChEMBL_629975 (CHEMBL1112052)
Ki
>1000±n/a nM
Citation
 Ishikawa, MShinei, RYokoyama, FYamauchi, MOyama, MOkuma, KNagayama, TKato, KKakui, NSato, Y Role of hydrophobic substituents on the terminal nitrogen of histamine in receptor binding and agonist activity: development of an orally active histamine type 3 receptor agonist and evaluation of its antistress activity in mice. J Med Chem 53:3840-4 (2010) [PubMed]  Article 
Target
Name:
Histamine H1 receptor
Synonyms:
H1R | HH1R | HISTAMINE H1 | HRH1 | HRH1_HUMAN
Type:
G Protein-Coupled Receptor (GPCR)
Mol. Mass.:
55808.72
Organism:
Homo sapiens (Human)
Description:
Cell pellets from SK-N-MC cells transfected with human H1 receptor were used in binding assay.
Residue:
487
Sequence:
MSLPNSSCLLEDKMCEGNKTTMASPQLMPLVVVLSTICLVTVGLNLLVLYAVRSERKLHTVGNLYIVSLSVADLIVGAVVMPMNILYLLMSKWSLGRPLCLFWLSMDYVASTASIFSVFILCIDRYRSVQQPLRYLKYRTKTRASATILGAWFLSFLWVIPILGWNHFMQQTSVRREDKCETDFYDVTWFKVMTAIINFYLPTLLMLWFYAKIYKAVRQHCQHRELINRSLPSFSEIKLRPENPKGDAKKPGKESPWEVLKRKPKDAGGGSVLKSPSQTPKEMKSPVVFSQEDDREVDKLYCFPLDIVHMQAAAEGSSRDYVAVNRSHGQLKTDEQGLNTHGASEISEDQMLGDSQSFSRTDSDTTTETAPGKGKLRSGSNTGLDYIKFTWKRLRSHSRQYVSGLHMNRERKAAKQLGFIMAAFILCWIPYFIFFMVIAFCKNCCNEHLHMFTIWLGYINSTLNPLIYPLCNENFKKTFKRILHIRS
  
Inhibitor
Name:
BDBM50317865
Synonyms:
2-(2-(4-tert-Butylphenylthio)ethyl)-1H-imidazole | 4-(2-(4-tert-butylphenylthio)ethyl)-1H-imidazole | CHEMBL1098230
Type:
Small organic molecule
Emp. Form.:
C15H20N2S
Mol. Mass.:
260.398
SMILES:
CC(C)(C)c1ccc(SCCc2cnc[nH]2)cc1
Structure:
Search PDB for entries with ligand similarity: