Target
Histamine H3 receptor
Ligand
BDBM50243123
Substrate
n/a
Meas. Tech.
ChEMBL_491618 (CHEMBL945389)
Ki
0.4±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 Lett 18:4133-6 (2008) [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:
BDBM50243123
Synonyms:
CHEMBL488464 | cyclopentyl((3aR,6aR)-6-(4-(2-((R)-2-methylpyrrolidin-1-yl)ethyl)phenyl)-1,3a,4,6a-tetrahydrocyclopenta[c]pyrrol-2(1H)-yl)methanone
Type:
Small organic molecule
Emp. Form.:
C26H36N2O
Mol. Mass.:
392.5768
SMILES:
C[C@@H]1CCCN1CCc1ccc(cc1)C1=CC[C@H]2CN(C[C@@H]12)C(=O)C1CCCC1 |r,t:16|
Structure:
Search PDB for entries with ligand similarity: