Target
Histamine H3 receptor
Ligand
BDBM50224192
Substrate
n/a
Meas. Tech.
ChEMBL_450586 (CHEMBL900873)
Ki
0.24±n/a nM
Citation
 Altenbach, RJLiu, HBanfor, PNBrowman, KEFox, GBFryer, RMKomater, VAKrueger, KMMarsh, KMiller, TRPan, JBPan, LSun, MThiffault, CWetter, JZhao, CZhou, DEsbenshade, TAHancock, AACowart, MD Synthesis, potency, and in vivo profiles of quinoline containing histamine H3 receptor inverse agonists. J Med Chem 50:5439-48 (2007) [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:
BDBM50224192
Synonyms:
(R)-2-(2,7-dimethylpyrazolo[1,5-a]pyrimidin-6-yl)-6-(2-(2-methylpyrrolidin-1-yl)ethyl)quinoline | 2-(2,7-dimethylpyrazolo[1,5-a]pyrimidin-6-yl)-6-{2-[(2R)-2-methylpyrrolidin-1-yl]ethyl}quinoline | CHEMBL392573
Type:
Small organic molecule
Emp. Form.:
C24H27N5
Mol. Mass.:
385.5047
SMILES:
C[C@@H]1CCCN1CCc1ccc2nc(ccc2c1)-c1cnc2cc(C)nn2c1C
Structure:
Search PDB for entries with ligand similarity: