Target
Histamine H3 receptor
Ligand
BDBM50328812
Substrate
n/a
Meas. Tech.
ChEMBL_673777 (CHEMBL1274954)
IC50
12±n/a nM
Citation
 Anderson, JTCampbell, MWang, JBrunden, KRHarrington, JJStricker-Krongrad, ASong, JDoucette, CMurphy, SBennani, YL Investigation of 4-piperidinols as novel H3 antagonists. Bioorg Med Chem Lett 20:6246-9 (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:
BDBM50328812
Synonyms:
CHEMBL1270264 | rac-1,2,5-trimethyl-4-(quinolin-5-ylethynyl)piperidin-4-ol
Type:
Small organic molecule
Emp. Form.:
C19H22N2O
Mol. Mass.:
294.3908
SMILES:
CC1CC(O)(C#Cc2cccc3ncccc23)C(C)CN1C
Structure:
Search PDB for entries with ligand similarity: