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Target
Histamine H3 receptor
Ligand
BDBM50217589
Substrate
n/a
Meas. Tech.
ChEMBL_463175 (CHEMBL948189)
Ki
0.7±n/a nM
Citation
Ly, KS; Letavic, MA; Keith, JM; Miller, JM; Stocking, EM; Barbier, AJ; Bonaventure, P; Lord, B; Jiang, X; Boggs, JD; Dvorak, L; Miller, KL; Nepomuceno, D; Wilson, SJ; Carruthers, NI Synthesis and biological activity of piperazine and diazepane amides that are histamine H3 antagonists and serotonin reuptake inhibitors. Bioorg Med Chem Lett 18:39-43 (2008) [PubMed] Article
More Info.:
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:
BDBM50217589
Synonyms:
(6S,10bR)-6-(4-methoxyphenyl)-9-(3-(piperidin-1-yl)propoxy)-1,2,3,5,6,10b-hexahydropyrrolo[2,1-a]isoquinoline | CHEMBL235614
Type:
Small organic molecule
Emp. Form.:
C27H36N2O2
Mol. Mass.:
420.5869
SMILES:
COc1ccc(cc1)[C@@H]1CN2CCC[C@@H]2c2cc(OCCCN3CCCCC3)ccc12