Reaction Details |
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Target | Histamine H3 receptor |
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Ligand | BDBM50139391 |
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Substrate/Competitor | n/a |
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Ki | 4.57±n/a nM |
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Comments | PDSP_4079 |
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Citation | Esbenshade, TA; Fox, GB; Krueger, KM; Miller, TR; Kang, CH; Denny, LI; Witte, DG; Yao, BB; Pan, L; Wetter, J; Marsh, K; Bennani, YL; Cowart, MD; Sullivan, JP; Hancock, AA Pharmacological properties of ABT-239 [4-(2-{2-[(2R)-2-Methylpyrrolidinyl]ethyl}-benzofuran-5-yl)benzonitrile]: I. Potent and selective histamine H3 receptor antagonist with drug-like properties. J Pharmacol Exp Ther313:165-75 (2005) [PubMed] Article |
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More Info.: | Get all data from this article |
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Histamine H3 receptor |
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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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BDBM50139391 |
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n/a |
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Name | BDBM50139391 |
Synonyms: | (R)-4-(2-(2-(2-methylpyrrolidin-1-yl)ethyl)benzofuran-5-yl)benzonitrile | 4-{2-[2-((R)-2-Methyl-pyrrolidin-1-yl)-ethyl]-benzofuran-5-yl}-benzonitrile | ABT-239 | CHEMBL351231 |
Type | Small organic molecule |
Emp. Form. | C22H22N2O |
Mol. Mass. | 330.4229 |
SMILES | C[C@@H]1CCCN1CCc1cc2cc(ccc2o1)-c1ccc(cc1)C#N |r| |
Structure |
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