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Target
Histamine H3 receptor
Ligand
BDBM50199593
Substrate
n/a
Meas. Tech.
ChEMBL_453434 (CHEMBL885433)
Ki
6.50±n/a nM
Citation
 Letavic, MA; Keith, JM; Jablonowski, JA; Stocking, EM; Gomez, LA; Ly, KS; Miller, JM; Barbier, AJ; Bonaventure, P; Boggs, JD; Wilson, SJ; Miller, KL; Lord, B; McAllister, HM; Tognarelli, DJ; Wu, J; Abad, MC; Schubert, C; Lovenberg, TW; Carruthers, NI Novel tetrahydroisoquinolines are histamine H3 antagonists and serotonin reuptake inhibitors. Bioorg Med Chem Lett 17:1047-51 (2007) [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:
BDBM50199593
Synonyms:
7-(3-(4-fluoropiperidin-1-yl)propoxy)-2-methyl-4-(4-(methylthio)phenyl)-1,2,3,4-tetrahydroisoquinoline | CHEMBL395368
Type:
Small organic molecule
Emp. Form.:
C25H33FN2OS
Mol. Mass.:
428.606
SMILES:
CSc1ccc(cc1)C1CN(C)Cc2cc(OCCCN3CCC(F)CC3)ccc12 |w:8.8|
Structure:
Search PDB for entries with ligand similarity: