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Target
Histamine H3 receptor
Ligand
BDBM50319565
Substrate
n/a
Meas. Tech.
ChEMBL_766669 (CHEMBL1827363)
Ki
1.1±n/a nM
Citation
 Levoin, N; Labeeuw, O; Calmels, T; Poupardin-Olivier, O; Berrebi-Bertrand, I; Lecomte, JM; Schwartz, JC; Capet, M Novel and highly potent histamine H3 receptor ligands. Part 1: withdrawing of hERG activity. Bioorg Med Chem Lett 21:5378-83 (2011) [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:
BDBM50319565
Synonyms:
(R)-2-(5-methyl-1-(6-methyl-4-(trifluoromethyl)pyridin-2-yl)-1H-pyrazol-4-yl)-6-(2-(2-methylpyrrolidin-1-yl)ethyl)quinoline | CHEMBL1084877
Type:
Small organic molecule
Emp. Form.:
C27H28F3N5
Mol. Mass.:
479.5399
SMILES:
C[C@@H]1CCCN1CCc1ccc2nc(ccc2c1)-c1cnn(c1C)-c1cc(cc(C)n1)C(F)(F)F |r|
Structure:
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