Ki Summary BindingDB logo
myBDB logout
Reaction Details
Report a problem with these data
TargetHistamine H3 receptor
LigandBDBM50394703
Substrate/Competitorn/a
Meas. Tech.ChEMBL_858650 (CHEMBL2166532)
EC50 2.88±n/a nM
Citation Birnkammer, TSpickenreither, ABrunskole, ILopuch, MKagermeier, NBernhardt, GDove, SSeifert, RElz, SBuschauer, A The bivalent ligand approach leads to highly potent and selective acylguanidine-type histamine H2 receptor agonists. J Med Chem55:1147-60 (2012) [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:
BDBM50394703
n/a
NameBDBM50394703
Synonyms:CHEMBL2165628
TypeSmall organic molecule
Emp. Form.C25H42N10O2S
Mol. Mass.546.732
SMILESCc1nc(N)sc1CCCN=C(N)NC(=O)CCCCCCCCC(=O)NC(N)=NCCCc1cnc[nH]1 |w:10.10,29.30|
Structure
Search PDB for entries with ligand similarity:Similarity to this molecule at least: