Reaction Details Report a problem with these data
Target
Histamine H3 receptor
Ligand
BDBM50496272
Substrate
n/a
Meas. Tech.
ChEMBL_1296757 (CHEMBL3132260)
IC50
8.8±n/a nM
Citation
 Brown, DG; Bernstein, PR; Griffin, A; Wesolowski, S; Labrecque, D; Tremblay, MC; Sylvester, M; Mauger, R; Edwards, PD; Throner, SR; Folmer, JJ; Cacciola, J; Scott, C; Lazor, LA; Pourashraf, M; Santhakumar, V; Potts, WM; Sydserff, S; Giguère, P; Lévesque, C; Dasser, M; Groblewski, T Discovery of spirofused piperazine and diazepane amides as selective histamine-3 antagonists with in vivo efficacy in a mouse model of cognition. J Med Chem 57:733-58 (2014) [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:
BDBM50496272
Synonyms:
CHEMBL3127701
Type:
Small organic molecule
Emp. Form.:
C22H37N3O2
Mol. Mass.:
375.5481
SMILES:
O=C(C1CC11CCN(CC1)C1CCOCC1)N1CCN(CC1)C1CCCC1
Structure:
Search PDB for entries with ligand similarity: