Target
Histamine H3 receptor
Ligand
BDBM50212733
Substrate
n/a
Meas. Tech.
ChEMBL_438819 (CHEMBL887977)
EC50
0.2±n/a nM
Citation
 Roche, ORodríguez Sarmiento, RM A new class of histamine H3 receptor antagonists derived from ligand based design. Bioorg Med Chem Lett 17:3670-5 (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:
BDBM50212733
Synonyms:
CHEMBL425994 | N-(2-((dimethylamino)methyl)-4-(3-(piperidin-1-yl)propoxy)phenyl)quinazolin-4-amine
Type:
Small organic molecule
Emp. Form.:
C25H33N5O
Mol. Mass.:
419.5624
SMILES:
CN(C)Cc1cc(OCCCN2CCCCC2)ccc1Nc1ncnc2ccccc12
Structure:
Search PDB for entries with ligand similarity: