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Target
Histamine H3 receptor
Ligand
BDBM50384401
Substrate
n/a
Meas. Tech.
ChEMBL_818355 (CHEMBL2034492)
EC50
1.7±n/a nM
Citation
 Josef, KA; Aimone, LD; Lyons, J; Raddatz, R; Hudkins, RL Synthesis of constrained benzocinnolinone analogues of CEP-26401 (irdabisant) as potent, selective histamine H3 receptor inverse agonists. Bioorg Med Chem Lett 22:4198-202 (2012) [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:
BDBM50384401
Synonyms:
CHEMBL2031470
Type:
Small organic molecule
Emp. Form.:
C21H27N3O2
Mol. Mass.:
353.458
SMILES:
C[C@@H]1CCCN1CCCOc1ccc-2c(CCc3cc(=O)n(C)nc-23)c1 |r|
Structure:
Search PDB for entries with ligand similarity: