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TargetHistamine H3 receptor
LigandBDBM50274691
Substrate/Competitorn/a
Meas. Tech.ChEMBL_537241 (CHEMBL981856)
IC50 813±n/a nM
Citation Nagase, TMizutani, TSekino, EIshikawa, SIto, SMitobe, YMiyamoto, YYoshimoto, RTanaka, TIshihara, ATakenaga, NTokita, SSato, N Synthesis and evaluation of structurally constrained quinazolinone derivatives as potent and selective histamine H3 receptor inverse agonists. J Med Chem51:6889-901 (2008) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Histamine H3 receptor
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:
MERAPPDGPLNASGALAGEAAAAGGARGFSAAWTAVLAALMALLIVATVLGNALVMLAFV
ADSSLRTQNNFFLLNLAISDFLVGAFCIPLYVPYVLTGRWTFGRGLCKLWLVVDYLLCTS
SAFNIVLISYDRFLSVTRAVSYRAQQGDTRRAVRKMLLVWVLAFLLYGPAILSWEYLSGG
SSIPEGHCYAEFFYNWYFLITASTLEFFTPFLSVTFFNLSIYLNIQRRTRLRLDGAREAA
GPEPPPEAQPSPPPPPGCWGCWQKGHGEAMPLHRYGVGEAAVGAEAGEATLGGGGGGGSV
ASPTSSSGSSSRGTERPRSLKRGSKPSASSASLEKRMKMVSQSFTQRFRLSRDRKVAKSL
AVIVSIFGLCWAPYTLLMIIRAACHGHCVPDYWYETSFWLLWANSAVNPVLYPLCHHSFR
RAFTKLLCPQKLKIQPHSSLEHCWK
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BDBM50274691
n/a
NameBDBM50274691
Synonyms:CHEMBL485604 | trans-2-Methyl-3-(4-([4-(1-pyrrolidinyl)cyclohexyl]oxy)phenyl)-4(3H)-quinazolinone
TypeSmall organic molecule
Emp. Form.C25H29N3O2
Mol. Mass.403.5167
SMILESCc1nc2ccccc2c(=O)n1-c1ccc(O[C@H]2CC[C@@H](CC2)N2CCCC2)cc1 |r,wU:17.18,wD:20.25,(33.03,-37.04,;31.7,-37.81,;30.36,-37.04,;29.03,-37.82,;27.69,-37.06,;26.36,-37.83,;26.36,-39.38,;27.7,-40.15,;29.03,-39.37,;30.37,-40.13,;30.37,-41.67,;31.71,-39.36,;33.04,-40.13,;33.04,-41.67,;34.37,-42.43,;35.71,-41.66,;37.04,-42.42,;38.37,-41.65,;38.35,-40.11,;39.69,-39.34,;41.03,-40.11,;41.03,-41.65,;39.7,-42.42,;42.36,-39.34,;43.76,-39.96,;44.79,-38.82,;44.02,-37.49,;42.52,-37.81,;35.7,-40.11,;34.36,-39.35,)|
Structure
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