Reaction Details Report a problem with these data
Target
Histamine H3 receptor
Ligand
BDBM50327486
Substrate
n/a
Meas. Tech.
ChEMBL_664613 (CHEMBL1260327)
Ki
5±n/a nM
Citation
 Richter, HG; Freichel, C; Huwyler, J; Nakagawa, T; Nettekoven, M; Plancher, JM; Raab, S; Roche, O; Schuler, F; Taylor, S; Ullmer, C; Wiegand, R Discovery of potent and selective histamine H3 receptor inverse agonists based on the 3,4-dihydro-2H-pyrazino[1,2-a]indol-1-one scaffold. Bioorg Med Chem Lett 20:5713-7 (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:
BDBM50327486
Synonyms:
8-(1-isopropylpiperidin-4-yloxy)-2-(pyridin-3-ylmethyl)-3,4-dihydropyrazino[1,2-a]indol-1(2H)-one | CHEMBL1257486
Type:
Small organic molecule
Emp. Form.:
C25H30N4O2
Mol. Mass.:
418.5313
SMILES:
CC(C)N1CCC(CC1)Oc1ccc2n3CCN(Cc4cccnc4)C(=O)c3cc2c1
Structure:
Search PDB for entries with ligand similarity: