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Target
Histamine H3 receptor
Ligand
BDBM50318106
Substrate
n/a
Meas. Tech.
ChEMBL_631946 (CHEMBL1104702)
Ki
6.7±n/a nM
Citation
 Watanabe, M; Hirokawa, T; Kobayashi, T; Yoshida, A; Ito, Y; Yamada, S; Orimoto, N; Yamasaki, Y; Arisawa, M; Shuto, S Investigation of the bioactive conformation of histamine H3 receptor antagonists by the cyclopropylic strain-based conformational restriction strategy. J Med Chem 53:3585-93 (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:
BDBM50318106
Synonyms:
(1S,2R)-2-[(1R)-1-Ethyl-2-(4-chlorobenzylamino)ethyl]-1-(1Himidazol-4-yl)cyclopropane | CHEMBL1097393
Type:
Small organic molecule
Emp. Form.:
C17H22ClN3
Mol. Mass.:
303.83
SMILES:
CC[C@@H](CNCc1ccc(Cl)cc1)[C@H]1C[C@@H]1c1cnc[nH]1 |r|
Structure:
Search PDB for entries with ligand similarity: