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Target
Histamine H3 receptor
Ligand
BDBM50297366
Substrate
n/a
Meas. Tech.
ChEMBL_583253 (CHEMBL1055808)
Ki
1±n/a nM
Citation
 Covel, JA; Santora, VJ; Smith, JM; Hayashi, R; Gallardo, C; Weinhouse, MI; Ibarra, JB; Schultz, JA; Park, DM; Estrada, SA; Hofilena, BJ; Pulley, MD; Smith, BM; Ren, A; Suarez, M; Frazer, J; Edwards, J; Hauser, EK; Lorea, J; Semple, G; Grottick, AJ Design and evaluation of novel biphenyl sulfonamide derivatives with potent histamine H(3) receptor inverse agonist activity. J Med Chem 52:5603-11 (2009) [PubMed]  Article 
Target
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:
MERAPPDGPLNASGALAGEAAAAGGARGFSAAWTAVLAALMALLIVATVLGNALVMLAFVADSSLRTQNNFFLLNLAISDFLVGAFCIPLYVPYVLTGRWTFGRGLCKLWLVVDYLLCTSSAFNIVLISYDRFLSVTRAVSYRAQQGDTRRAVRKMLLVWVLAFLLYGPAILSWEYLSGGSSIPEGHCYAEFFYNWYFLITASTLEFFTPFLSVTFFNLSIYLNIQRRTRLRLDGAREAAGPEPPPEAQPSPPPPPGCWGCWQKGHGEAMPLHRYGVGEAAVGAEAGEATLGGGGGGGSVASPTSSSGSSSRGTERPRSLKRGSKPSASSASLEKRMKMVSQSFTQRFRLSRDRKVAKSLAVIVSIFGLCWAPYTLLMIIRAACHGHCVPDYWYETSFWLLWANSAVNPVLYPLCHHSFRRAFTKLLCPQKLKIQPHSSLEHCWK
  
Inhibitor
Name:
BDBM50297366
Synonyms:
4'-[2-((R)-2-Methyl-pyrrolidin-1-yl)-ethyl]-biphenyl-4-sulfonic Acid Ethylamide | CHEMBL569832
Type:
Small organic molecule
Emp. Form.:
C21H28N2O2S
Mol. Mass.:
372.524
SMILES:
CCNS(=O)(=O)c1ccc(cc1)-c1ccc(CCN2CCC[C@H]2C)cc1 |r|
Structure:
Search PDB for entries with ligand similarity: