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Target
Histamine H3 receptor
Ligand
BDBM50401007
Substrate
n/a
Meas. Tech.
ChEMBL_879381 (CHEMBL2208779)
Ki
1.32±n/a nM
Citation
 Wager, TT; Pettersen, BA; Schmidt, AW; Spracklin, DK; Mente, S; Butler, TW; Howard, H; Lettiere, DJ; Rubitski, DM; Wong, DF; Nedza, FM; Nelson, FR; Rollema, H; Raggon, JW; Aubrecht, J; Freeman, JK; Marcek, JM; Cianfrogna, J; Cook, KW; James, LC; Chatman, LA; Iredale, PA; Banker, MJ; Homiski, ML; Munzner, JB; Chandrasekaran, RY Discovery of two clinical histamine H(3) receptor antagonists: trans-N-ethyl-3-fluoro-3-[3-fluoro-4-(pyrrolidinylmethyl)phenyl]cyclobutanecarboxamide (PF-03654746) and trans-3-fluoro-3-[3-fluoro-4-(pyrrolidin-1-ylmethyl)phenyl]-N-(2-methylpropyl)cyclobutanecarboxamide (PF-03654764). J Med Chem 54:7602-20 (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:
BDBM50401007
Synonyms:
CHEMBL209478
Type:
Small organic molecule
Emp. Form.:
C18H24N2
Mol. Mass.:
268.3966
SMILES:
CN(C)Cc1ccc(cc1)-c1ccc(CN(C)C)cc1
Structure:
Search PDB for entries with ligand similarity: