Target
Histamine H3 receptor
Ligand
BDBM50268452
Substrate
n/a
Meas. Tech.
ChEMBL_523445 (CHEMBL1008297)
Ki
5±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:
HH3R | HRH3_RAT | Hrh3
Type:
G Protein-Coupled Receptor (GPCR)
Mol. Mass.:
48607.98
Organism:
Rattus norvegicus (rat)
Description:
n/a
Residue:
445
Sequence:
MERAPPDGLMNASGTLAGEAAAAGGARGFSAAWTAVLAALMALLIVATVLGNALVMLAFVADSSLRTQNNFFLLNLAISDFLVGAFCIPLYVPYVLTGRWTFGRGLCKLWLVVDYLLCASSVFNIVLISYDRFLSVTRAVSYRAQQGDTRRAVRKMALVWVLAFLLYGPAILSWEYLSGGSSIPEGHCYAEFFYNWYFLITASTLEFFTPFLSVTFFNLSIYLNIQRRTRLRLDGGREAGPEPPPDAQPSPPPAPPSCWGCWPKGHGEAMPLHRYGVGEAGPGVEAGEAALGGGSGGGAAASPTSSSGSSSRGTERPRSLKRGSKPSASSASLEKRMKMVSQSITQRFRLSRDKKVAKSLAIIVSIFGLCWAPYTLLMIIRAACHGRCIPDYWYETSFWLLWANSAVNPVLYPLCHYSFRRAFTKLLCPQKLKVQPHGSLEQCWK
  
Inhibitor
Name:
BDBM50268452
Synonyms:
(4-cyclobutylpiperazin-1-yl)(2-(morpholine-4-carbonyl)-1-(2,2,2-trifluoroethyl)-1H-indol-5-yl)methanone | CHEMBL522739
Type:
Small organic molecule
Emp. Form.:
C24H29F3N4O3
Mol. Mass.:
478.5073
SMILES:
FC(F)(F)Cn1c(cc2cc(ccc12)C(=O)N1CCN(CC1)C1CCC1)C(=O)N1CCOCC1
Structure:
Search PDB for entries with ligand similarity: