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Target
Histamine H3 receptor
Ligand
BDBM50317698
Substrate
n/a
Meas. Tech.
ChEMBL_629414 (CHEMBL1105767)
Ki
1.6±n/a nM
Citation
 Stocking, EM; Aluisio, L; Atack, JR; Bonaventure, P; Carruthers, NI; Dugovic, C; Everson, A; Fraser, I; Jiang, X; Leung, P; Lord, B; Ly, KS; Morton, KL; Nepomuceno, D; Shah, CR; Shelton, J; Soyode-Johnson, A; Letavic, MA Novel substituted pyrrolidines are high affinity histamine H3 receptor antagonists. Bioorg Med Chem Lett 20:2755-60 (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:
BDBM50317698
Synonyms:
1-((2R,4S)-2-(4-cyclobutyl-1,4-diazepane-1-carbonyl)-4-(3-fluorophenoxy)pyrrolidin-1-yl)ethanone | CHEMBL1096827
Type:
Small organic molecule
Emp. Form.:
C22H30FN3O3
Mol. Mass.:
403.4903
SMILES:
CC(=O)N1C[C@H](C[C@@H]1C(=O)N1CCCN(CC1)C1CCC1)Oc1cccc(F)c1 |r|
Structure:
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