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Target
Histamine H3 receptor
Ligand
BDBM50448293
Substrate
n/a
Meas. Tech.
ChEMBL_1293783 (CHEMBL3123355)
Ki
6.9±n/a nM
Citation
 Hudkins, RL; Josef, KA; Becknell, NC; Aimone, LD; Lyons, JA; Mathiasen, JR; Gruner, JA; Raddatz, R Discovery of (1R,6S)-5-[4-(1-cyclobutyl-piperidin-4-yloxy)-phenyl]-3,4-diaza-bicyclo[4.1.0]hept-4-en-2-one (R,S-4a): histamine H(3) receptor inverse agonist demonstrating potent cognitive enhancing and wake promoting activity. Bioorg Med Chem Lett 24:1303-6 (2014) [PubMed]  Article 
Target
Name:
Histamine H3 receptor
Synonyms:
HH3R | HRH3_RAT | Hrh3
Type:
G Protein-Coupled Receptor (GPCR)
Mol. Mass.:
48607.98
Organism:
Rattus norvegicus (rat)
Description:
n/a
Residue:
445
Sequence:
MERAPPDGLMNASGTLAGEAAAAGGARGFSAAWTAVLAALMALLIVATVLGNALVMLAFVADSSLRTQNNFFLLNLAISDFLVGAFCIPLYVPYVLTGRWTFGRGLCKLWLVVDYLLCASSVFNIVLISYDRFLSVTRAVSYRAQQGDTRRAVRKMALVWVLAFLLYGPAILSWEYLSGGSSIPEGHCYAEFFYNWYFLITASTLEFFTPFLSVTFFNLSIYLNIQRRTRLRLDGGREAGPEPPPDAQPSPPPAPPSCWGCWPKGHGEAMPLHRYGVGEAGPGVEAGEAALGGGSGGGAAASPTSSSGSSSRGTERPRSLKRGSKPSASSASLEKRMKMVSQSITQRFRLSRDKKVAKSLAIIVSIFGLCWAPYTLLMIIRAACHGRCIPDYWYETSFWLLWANSAVNPVLYPLCHYSFRRAFTKLLCPQKLKVQPHGSLEQCWK
  
Inhibitor
Name:
BDBM50448293
Synonyms:
CHEMBL3121097
Type:
Small organic molecule
Emp. Form.:
C21H27N3O2
Mol. Mass.:
353.458
SMILES:
CN1N=C(C2CC2C1=O)c1ccc(OC2CCN(CC2)C2CCC2)cc1 |c:2|
Structure:
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