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TargetHistamine H3 receptor
LigandBDBM50317687
Substrate/Competitorn/a
Meas. Tech.ChEMBL_629414 (CHEMBL1105767)
Ki 3.7±n/a nM
Citation Stocking, EMAluisio, LAtack, JRBonaventure, PCarruthers, NIDugovic, CEverson, AFraser, IJiang, XLeung, PLord, BLy, KSMorton, KLNepomuceno, DShah, CRShelton, JSoyode-Johnson, ALetavic, MA Novel substituted pyrrolidines are high affinity histamine H3 receptor antagonists. Bioorg Med Chem Lett20:2755-60 (2010) [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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  Blast E-value cutoff:
BDBM50317687
n/a
NameBDBM50317687
Synonyms:1-((2R,4S)-2-(4-cyclobutyl-1,4-diazepane-1-carbonyl)-4-(thiophen-2-yloxy)pyrrolidin-1-yl)ethanone | CHEMBL1098780
TypeSmall organic molecule
Emp. Form.C20H29N3O3S
Mol. Mass.391.528
SMILESCC(=O)N1C[C@H](C[C@@H]1C(=O)N1CCCN(CC1)C1CCC1)Oc1cccs1 |r|
Structure
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