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Target
Histamine H3 receptor
Ligand
BDBM50301081
Substrate
n/a
Meas. Tech.
ChEBML_1686321
Ki
517±n/a nM
Citation
 Schaller, D; Hagenow, S; Alpert, G; Naß, A; Schulz, R; Bermudez, M; Stark, H; Wolber, G Systematic Data Mining Reveals Synergistic H3R/MCHR1 Ligands. ACS Med Chem Lett 8:648-653 (2017) [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:
BDBM50301081
Synonyms:
4-(4-fluorobenzyloxy)-1-(4-(2-(pyrrolidin-1-yl)ethoxy)phenyl)pyridin-2(1H)-one | CHEMBL584538
Type:
Small organic molecule
Emp. Form.:
C24H25FN2O3
Mol. Mass.:
408.4653
SMILES:
Fc1ccc(COc2ccn(-c3ccc(OCCN4CCCC4)cc3)c(=O)c2)cc1
Structure:
Search PDB for entries with ligand similarity: