Reaction Details Report a problem with these data
Target
Histamine H3 receptor
Ligand
BDBM50364959
Substrate
n/a
Meas. Tech.
ChEMBL_804459 (CHEMBL1952469)
EC50
1.6±n/a nM
Citation
 Hudkins, RL; Zulli, AL; Dandu, Rr; Tao, M; Josef, KA; Aimone, LD; Haltiwanger, RC; Huang, Z; Lyons, JA; Mathiasen, JR; Raddatz, R; Gruner, JA 4-phenoxypiperidine pyridazin-3-one histamine H(3) receptor inverse agonists demonstrating potent and robust wake promoting activity. Bioorg Med Chem Lett 22:1504-9 (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:
BDBM50364959
Synonyms:
CHEMBL1950747
Type:
Small organic molecule
Emp. Form.:
C20H27N3O2
Mol. Mass.:
341.4473
SMILES:
C[C@H]1CC(=O)NN=C1c1ccc(OC2CCN(CC2)C2CCC2)cc1 |r,c:6|
Structure:
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