Target
Histamine H3 receptor
Ligand
BDBM50268950
Substrate
n/a
Meas. Tech.
ChEMBL_523444 (CHEMBL1008296)
Ki
6±n/a nM
Citation
 Pierson, PDFettes, AFreichel, CGatti-McArthur, SHertel, CHuwyler, JMohr, PNakagawa, TNettekoven, MPlancher, JMRaab, SRichter, HRoche, ORodríguez Sarmiento, RMSchmitt, MSchuler, FTakahashi, TTaylor, SUllmer, CWiegand, R 5-hydroxyindole-2-carboxylic acid amides: novel histamine-3 receptor inverse agonists for the treatment of obesity. J Med Chem 52:3855-68 (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:
BDBM50268950
Synonyms:
CHEMBL522715 | azepan-1-yl(5-(1-isopropylpiperidin-4-yloxy)-1H-indol-2-yl)methanone
Type:
Small organic molecule
Emp. Form.:
C23H33N3O2
Mol. Mass.:
383.527
SMILES:
CC(C)N1CCC(CC1)Oc1ccc2[nH]c(cc2c1)C(=O)N1CCCCCC1
Structure:
Search PDB for entries with ligand similarity: