Target
Histamine H3 receptor
Ligand
BDBM50246289
Substrate
n/a
Meas. Tech.
ChEMBL_766669 (CHEMBL1827363)
Ki
0.21875±n/a nM
Citation
 Levoin, NLabeeuw, OCalmels, TPoupardin-Olivier, OBerrebi-Bertrand, ILecomte, JMSchwartz, JCCapet, M Novel and highly potent histamine H3 receptor ligands. Part 1: withdrawing of hERG activity. Bioorg Med Chem Lett 21:5378-83 (2011) [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:
BDBM50246289
Synonyms:
3-methyl-2-(4-(3-(pyrrolidin-1-yl)propoxy)phenyl)quinazolin-4(3H)-one | CHEMBL488248 | CHEMBL557214
Type:
Small organic molecule
Emp. Form.:
C22H25N3O2
Mol. Mass.:
363.4528
SMILES:
Cn1c(nc2ccccc2c1=O)-c1ccc(OCCCN2CCCC2)cc1
Structure:
Search PDB for entries with ligand similarity: