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Target
Histamine H3 receptor
Ligand
BDBM50216250
Substrate
n/a
Meas. Tech.
ChEMBL_456606 (CHEMBL923983)
Ki
0.7±n/a nM
Citation
 Keith, JM; Gomez, LA; Barbier, AJ; Wilson, SJ; Boggs, JD; Lord, B; Mazur, C; Aluisio, L; Lovenberg, TW; Carruthers, NI Pyrrolidino-tetrahydroisoquinolines bearing pendant heterocycles as potent dual H3 antagonist and serotonin transporter inhibitors. Bioorg Med Chem Lett 17:4374-7 (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:
BDBM50216250
Synonyms:
(6R,10bR)-9-(3-(piperidin-1-yl)propoxy)-6-(thiophen-3-yl)-1,2,3,5,6,10b-hexahydropyrrolo[2,1-a]isoquinoline | CHEMBL394928
Type:
Small organic molecule
Emp. Form.:
C24H32N2OS
Mol. Mass.:
396.589
SMILES:
C(COc1ccc2[C@@H](CN3CCC[C@@H]3c2c1)c1ccsc1)CN1CCCCC1
Structure:
Search PDB for entries with ligand similarity: