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Target
Histamine H3 receptor
Ligand
BDBM50519742
Substrate
n/a
Meas. Tech.
ChEMBL_1878294 (CHEMBL4379688)
Ki
40±n/a nM
Citation
 Malek, R; Arribas, RL; Palomino-Antolin, A; Totoson, P; Demougeot, C; Kobrlova, T; Soukup, O; Iriepa, I; Moraleda, I; Diez-Iriepa, D; Gody?, J; Panek, D; Malawska, B; G?uch-Lutwin, M; Mordyl, B; Siwek, A; Chabchoub, F; Marco-Contelles, J; Kiec-Kononowicz, K; Egea, J; de Los Ríos, C; Ismaili, L New Dual Small Molecules for Alzheimer's Disease Therapy Combining Histamine H J Med Chem 62:11416-11422 (2019) [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:
BDBM50519742
Synonyms:
CHEMBL4469017
Type:
Small organic molecule
Emp. Form.:
C27H38N2O5
Mol. Mass.:
470.601
SMILES:
CCOC(=O)C1=C(C)NC(C)=C(C1c1ccc(OCCCN2CCCCC2)cc1)C(=O)OCC |c:5,10|
Structure:
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