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TargetHistamine receptor (H3)
LigandBDBM50364960
Substrate/Competitorn/a
Meas. Tech.ChEMBL_804459
EC50 1.3±n/a nM
Citation Hudkins, RLZulli, ALDandu, RrTao, MJosef, KAAimone, LDHaltiwanger, RCHuang, ZLyons, JAMathiasen, JRRaddatz, RGruner, JA 4-phenoxypiperidine pyridazin-3-one histamine H(3) receptor inverse agonists demonstrating potent and robust wake promoting activity. Bioorg Med Chem Lett22:1504-9 (2012) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Histamine receptor (H3)
Name:Histamine receptor (H3 and H4)
Synonyms:G-protein coupled receptor 97 | HH3R | HISTAMINE H3 | HRH3 | Histamine H3 Receptor | 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:
MERAPPDGPLNASGALAGEAAAAGGARGFSAAWTAVLAALMALLIVATVLGNALVMLAFV
ADSSLRTQNNFFLLNLAISDFLVGAFCIPLYVPYVLTGRWTFGRGLCKLWLVVDYLLCTS
SAFNIVLISYDRFLSVTRAVSYRAQQGDTRRAVRKMLLVWVLAFLLYGPAILSWEYLSGG
SSIPEGHCYAEFFYNWYFLITASTLEFFTPFLSVTFFNLSIYLNIQRRTRLRLDGAREAA
GPEPPPEAQPSPPPPPGCWGCWQKGHGEAMPLHRYGVGEAAVGAEAGEATLGGGGGGGSV
ASPTSSSGSSSRGTERPRSLKRGSKPSASSASLEKRMKMVSQSFTQRFRLSRDRKVAKSL
AVIVSIFGLCWAPYTLLMIIRAACHGHCVPDYWYETSFWLLWANSAVNPVLYPLCHHSFR
RAFTKLLCPQKLKIQPHSSLEHCWK
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  Blast E-value cutoff:
BDBM50364960
NameBDBM50364960
Synonyms:CHEMBL1950746
TypeSmall organic molecule
Emp. Form.C20H27N3O2
Mol. Mass.341.4473
SMILESC[C@@H]1CC(=O)NN=C1c1ccc(OC2CCN(CC2)C2CCC2)cc1 |r,c:6|
Structure
Search PDB for entries with ligand similarity:Similarity to this molecule at least:
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