Ki Summary BindingDB logo
myBDB logout
Reaction Details
Report a problem with these data
TargetHistamine H3 receptor
LigandBDBM50243674
Substrate/Competitorn/a
Meas. Tech.ChEMBL_491620 (CHEMBL945391)
Ki 4±n/a nM
Citation Santora, VJCovel, JAHayashi, RHofilena, BJIbarra, JBPulley, MDWeinhouse, MISemple, GRen, APereira, GEdwards, JESuarez, MFrazer, JThomsen, WHauser, ELorea, JGrottick, AJ Novel H3 receptor antagonists with improved pharmacokinetic profiles. Bioorg Med Chem Lett18:4133-6 (2008) [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:
BDBM50243674
n/a
NameBDBM50243674
Synonyms:((3aR,6aR)-6-(4-(2-((R)-2-methylpyrrolidin-1-yl)ethyl)phenyl)-1,3a,4,6a-tetrahydrocyclopenta[c]pyrrol-2(1H)-yl)(tetrahydro-2H-pyran-4-yl)methanone | CHEMBL471555
TypeSmall organic molecule
Emp. Form.C26H36N2O2
Mol. Mass.408.5762
SMILESC[C@@H]1CCCN1CCc1ccc(cc1)C1=CC[C@H]2CN(C[C@@H]12)C(=O)C1CCOCC1 |r,t:16|
Structure
Search PDB for entries with ligand similarity:Similarity to this molecule at least: