Target
Histamine H3 receptor
Ligand
BDBM50357273
Substrate
n/a
Meas. Tech.
ChEMBL_788369 (CHEMBL1918050)
Ki
54±n/a nM
Citation
 Masood, MASelby, MDBell, ASMansfield, ACGardner, MSmith, GFLane, CKenyon-Edwards, HOsborne, RJones, RMLiu, WLBrown, CDClarke, NPerrucio, FMowbray, CE Discovery of a series of potent and selective human H4 antagonists using ligand efficiency and libraries to explore structure-activity relationship (SAR). Bioorg Med Chem Lett 21:6591-5 (2011) [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:
BDBM50357273
Synonyms:
CHEMBL1916499
Type:
Small organic molecule
Emp. Form.:
C15H27N5
Mol. Mass.:
277.4084
SMILES:
CN(C)[C@@H]1CCN(C1)c1cc(NCC(C)(C)C)ncn1 |r|
Structure:
Search PDB for entries with ligand similarity: