Ki Summary BindingDB logo
myBDB logout
Reaction Details
Report a problem with these data
TargetHistamine H3 receptor
LigandBDBM50079598
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1471679 (CHEMBL3421047)
Ki 19±n/a nM
Citation Hudkins, RLBecknell, NCLyons, JAAimone, LDOlsen, MHaltiwanger, RCMathiasen, JRRaddatz, RGruner, JA 3,4-Diaza-bicyclo[4.1.0]hept-4-en-2-one phenoxypropylamine analogs of irdabisant (CEP-26401) as potent histamine-3 receptor inverse agonists with robust wake-promoting activity. Eur J Med Chem95:349-56 (2015) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Histamine H3 receptor
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:
MERAPPDGPLNASGALAGEAAAAGGARGFSAAWTAVLAALMALLIVATVLGNALVMLAFV
ADSSLRTQNNFFLLNLAISDFLVGAFCIPLYVPYVLTGRWTFGRGLCKLWLVVDYLLCTS
SAFNIVLISYDRFLSVTRAVSYRAQQGDTRRAVRKMLLVWVLAFLLYGPAILSWEYLSGG
SSIPEGHCYAEFFYNWYFLITASTLEFFTPFLSVTFFNLSIYLNIQRRTRLRLDGAREAA
GPEPPPEAQPSPPPPPGCWGCWQKGHGEAMPLHRYGVGEAAVGAEAGEATLGGGGGGGSV
ASPTSSSGSSSRGTERPRSLKRGSKPSASSASLEKRMKMVSQSFTQRFRLSRDRKVAKSL
AVIVSIFGLCWAPYTLLMIIRAACHGHCVPDYWYETSFWLLWANSAVNPVLYPLCHHSFR
RAFTKLLCPQKLKIQPHSSLEHCWK
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM50079598
n/a
NameBDBM50079598
Synonyms:CHEMBL3417507
TypeSmall organic molecule
Emp. Form.C19H25N3O2
Mol. Mass.327.4207
SMILESO=C1NN=C(C2CC12)c1ccc(OCCCN2CCCCC2)cc1 |c:3|
Structure
Search PDB for entries with ligand similarity:Similarity to this molecule at least: