Target
Histamine H3 receptor
Ligand
BDBM50255759
Substrate
n/a
Meas. Tech.
ChEMBL_515526 (CHEMBL1036547)
Ki
4±n/a nM
Citation
 Jablonowski, JALy, KSBogenstaetter, MDvorak, CABoggs, JDDvorak, LKLord, BMiller, KLMazur, CWilson, SJLovenberg, TWCarruthers, NI Novel imidazole-based histamine H3 antagonists. Bioorg Med Chem Lett 19:903-7 (2009) [PubMed]  Article 
Target
Name:
Histamine H3 receptor
Synonyms:
G-protein coupled receptor 97 | GPCR97 | HH3R | HISTAMINE H3 | HRH3 | HRH3_HUMAN | Histamine H3 receptor (H3) | Histamine H3L | Histamine receptor (H3 and H4)
Type:
G Protein-Coupled Receptor (GPCR)
Mol. Mass.:
48691.47
Organism:
Homo sapiens (Human)
Description:
Binding assays were using CHO cells stably expressing hH3R receptors.
Residue:
445
Sequence:
MERAPPDGPLNASGALAGEAAAAGGARGFSAAWTAVLAALMALLIVATVLGNALVMLAFVADSSLRTQNNFFLLNLAISDFLVGAFCIPLYVPYVLTGRWTFGRGLCKLWLVVDYLLCTSSAFNIVLISYDRFLSVTRAVSYRAQQGDTRRAVRKMLLVWVLAFLLYGPAILSWEYLSGGSSIPEGHCYAEFFYNWYFLITASTLEFFTPFLSVTFFNLSIYLNIQRRTRLRLDGAREAAGPEPPPEAQPSPPPPPGCWGCWQKGHGEAMPLHRYGVGEAAVGAEAGEATLGGGGGGGSVASPTSSSGSSSRGTERPRSLKRGSKPSASSASLEKRMKMVSQSFTQRFRLSRDRKVAKSLAVIVSIFGLCWAPYTLLMIIRAACHGHCVPDYWYETSFWLLWANSAVNPVLYPLCHHSFRRAFTKLLCPQKLKIQPHSSLEHCWK
  
Inhibitor
Name:
BDBM50255759
Synonyms:
(2-((1-isopropylpiperidin-4-yl)methoxy)-1-methyl-1H-imidazol-5-yl)(4-nitrophenyl)methanone | CHEMBL480633
Type:
Small organic molecule
Emp. Form.:
C20H26N4O4
Mol. Mass.:
386.4448
SMILES:
CC(C)N1CCC(COc2ncc(C(=O)c3ccc(cc3)[N+]([O-])=O)n2C)CC1
Structure:
Search PDB for entries with ligand similarity: