Target
Histamine H3 receptor
Ligand
BDBM50209688
Substrate
n/a
Meas. Tech.
ChEMBL_675954 (CHEMBL1272820)
Ki
548±n/a nM
Citation
 Cirauqui, NSchrey, AKGaliano, SCeras, JPérez-Silanes, SAldana, IMonge, AKühne, R Building a MCHR1 homology model provides insight into the receptor-antagonist contacts that are important for the development of new anti-obesity agents. Bioorg Med Chem 18:7365-79 (2010) [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:
BDBM50209688
Synonyms:
3-[1,1-di(acetyloxymethyl)propyl]-1-(4'-fluoro-4-biphenylmethyl)-1-{2-[1-(4-methylbenzyl)-4-piperidinyl]ethyl}urea | CHEMBL392015
Type:
Small organic molecule
Emp. Form.:
C38H48FN3O5
Mol. Mass.:
645.8032
SMILES:
CCC(COC(C)=O)(COC(C)=O)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(cc1)-c1ccc(F)cc1
Structure:
Search PDB for entries with ligand similarity: