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Target
Histamine H3 receptor
Ligand
BDBM50296188
Substrate
n/a
Meas. Tech.
ChEMBL_579538 (CHEMBL1061547)
IC50
0.6±n/a nM
Citation
 Sasaki, T; Takahashi, T; Nagase, T; Mizutani, T; Ito, S; Mitobe, Y; Miyamoto, Y; Kanesaka, M; Yoshimoto, R; Tanaka, T; Takenaga, N; Tokita, S; Sato, N Synthesis, structure-activity relationships, and biological profiles of a dihydrobenzoxathiin class of histamine H(3) receptor inverse agonists. Bioorg Med Chem Lett 19:4232-6 (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:
BDBM50296188
Synonyms:
CHEMBL558248 | trans-1-{3-[4-(3-Methyl-4,4-dioxo-3,4-dihydro-2H-4lambda*6*-benzo[1,4]oxathiin-2-yl)-phenoxy]-propyl}-pyrrolidine
Type:
Small organic molecule
Emp. Form.:
C22H27NO4S
Mol. Mass.:
401.519
SMILES:
C[C@@H]1[C@H](Oc2ccccc2S1(=O)=O)c1ccc(OCCCN2CCCC2)cc1 |r|
Structure:
Search PDB for entries with ligand similarity: