Reaction Details Report a problem with these data
Target
Histamine H3 receptor
Ligand
BDBM50361237
Substrate
n/a
Meas. Tech.
ChEMBL_794859 (CHEMBL1936095)
Ki
0.2±n/a nM
Citation
 Semple, G; Santora, VJ; Smith, JM; Covel, JA; Hayashi, R; Gallardo, C; Ibarra, JB; Schultz, JA; Park, DM; Estrada, SA; Hofilena, BJ; Smith, BM; Ren, A; Suarez, M; Frazer, J; Edwards, JE; Hart, R; Hauser, EK; Lorea, J; Grottick, AJ Identification of biaryl sulfone derivatives as antagonists of the histamine H3 receptor: discovery of (R)-1-(2-(4'-(3-methoxypropylsulfonyl)biphenyl-4-yl)ethyl)-2-methylpyrrolidine (APD916). Bioorg Med Chem Lett 22:71-5 (2011) [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:
BDBM50361237
Synonyms:
CHEMBL1934527
Type:
Small organic molecule
Emp. Form.:
C25H33NO3S
Mol. Mass.:
427.599
SMILES:
C[C@@H]1CCCN1CCc1ccc(cc1)-c1ccc(cc1)S(=O)(=O)CC1CCCCO1 |r|
Structure:
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