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Target
Histamine H3 receptor
Ligand
BDBM50293628
Substrate
n/a
Meas. Tech.
ChEMBL_571442 (CHEMBL1032753)
IC50
390±n/a nM
Citation
 Kennedy, JP; Conn, PJ; Lindsley, CW A novel class of H3 antagonists derived from the natural product guided synthesis of unnatural analogs of the marine bromopyrrole alkaloid dispyrin. Bioorg Med Chem Lett 19:3204-8 (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:
BDBM50293628
Synonyms:
CHEMBL561228 | N-(3-bromo-4-(2-(pyrrolidin-1-yl)ethoxy)phenethyl)-5-bromofuran-2-carboxamide
Type:
Small organic molecule
Emp. Form.:
C19H22Br2N2O3
Mol. Mass.:
486.198
SMILES:
Brc1ccc(o1)C(=O)NCCc1ccc(OCCN2CCCC2)c(Br)c1
Structure:
Search PDB for entries with ligand similarity: