Reaction Details Report a problem with these data
Target
Histamine H3 receptor
Ligand
BDBM50448294
Substrate
n/a
Meas. Tech.
ChEMBL_1293783 (CHEMBL3123355)
Ki
12±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:
BDBM50448294
Synonyms:
CHEMBL3121096
Type:
Small organic molecule
Emp. Form.:
C20H25N3O2
Mol. Mass.:
339.4314
SMILES:
O=C1NN=C([C@@H]2C[C@H]12)c1ccc(OC2CCN(CC2)C2CCC2)cc1 |r,c:3|
Structure:
Search PDB for entries with ligand similarity: