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Target
Histamine H3 receptor
Ligand
BDBM50277076
Substrate
n/a
Meas. Tech.
ChEMBL_540492 (CHEMBL1030596)
Ki
1.21±n/a nM
Citation
 von Coburg, Y; Kottke, T; Weizel, L; Ligneau, X; Stark, H Potential utility of histamine H3 receptor antagonist pharmacophore in antipsychotics. Bioorg Med Chem Lett 19:538-42 (2008) [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:
BDBM50277076
Synonyms:
CHEMBL459373 | [3-(2-Chloro-phenothiazin-10-yl)-propyl]-methyl-[4-(3-piperidin-1-yl-propoxy)-benzyl]-amine
Type:
Small organic molecule
Emp. Form.:
C31H38ClN3OS
Mol. Mass.:
536.171
SMILES:
CN(CCCN1c2ccccc2Sc2ccc(Cl)cc12)Cc1ccc(OCCCN2CCCCC2)cc1
Structure:
Search PDB for entries with ligand similarity: