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Target
Histamine H3 receptor
Ligand
BDBM50328927
Substrate
n/a
Meas. Tech.
ChEMBL_673999 (CHEMBL1275176)
Ki
23±n/a nM
Citation
 Santillan, A; McClure, KJ; Allison, BD; Lord, B; Boggs, JD; Morton, KL; Everson, AM; Nepomuceno, D; Letavic, MA; Lee-Dutra, A; Lovenberg, TW; Carruthers, NI; Grice, CA Indole- and benzothiophene-based histamine H3 antagonists. Bioorg Med Chem Lett 20:6226-30 (2010) [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:
BDBM50328927
Synonyms:
(4-cyclopropylpiperazin-1-yl)(4-(3,4-dichlorophenoxy)-3-((methylamino)methyl)phenyl)methanone | CHEMBL402644
Type:
Small organic molecule
Emp. Form.:
C22H25Cl2N3O2
Mol. Mass.:
434.359
SMILES:
CNCc1cc(ccc1Oc1ccc(Cl)c(Cl)c1)C(=O)N1CCN(CC1)C1CC1
Structure:
Search PDB for entries with ligand similarity: