Reaction Details |
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Target | Histamine H3 receptor |
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Ligand | BDBM50327477 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_664627 (CHEMBL1260341) |
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EC50 | 18±n/a nM |
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Citation | Richter, HG; Freichel, C; Huwyler, J; Nakagawa, T; Nettekoven, M; Plancher, JM; Raab, S; Roche, O; Schuler, F; Taylor, S; Ullmer, C; Wiegand, R Discovery of potent and selective histamine H3 receptor inverse agonists based on the 3,4-dihydro-2H-pyrazino[1,2-a]indol-1-one scaffold. Bioorg Med Chem Lett20:5713-7 (2010) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Histamine H3 receptor |
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Name: | Histamine H3 receptor |
Synonyms: | HH3R | HRH3_RAT | Hrh3 |
Type: | G Protein-Coupled Receptor (GPCR) |
Mol. Mass.: | 48607.98 |
Organism: | Rattus norvegicus (rat) |
Description: | n/a |
Residue: | 445 |
Sequence: | MERAPPDGLMNASGTLAGEAAAAGGARGFSAAWTAVLAALMALLIVATVLGNALVMLAFV
ADSSLRTQNNFFLLNLAISDFLVGAFCIPLYVPYVLTGRWTFGRGLCKLWLVVDYLLCAS
SVFNIVLISYDRFLSVTRAVSYRAQQGDTRRAVRKMALVWVLAFLLYGPAILSWEYLSGG
SSIPEGHCYAEFFYNWYFLITASTLEFFTPFLSVTFFNLSIYLNIQRRTRLRLDGGREAG
PEPPPDAQPSPPPAPPSCWGCWPKGHGEAMPLHRYGVGEAGPGVEAGEAALGGGSGGGAA
ASPTSSSGSSSRGTERPRSLKRGSKPSASSASLEKRMKMVSQSITQRFRLSRDKKVAKSL
AIIVSIFGLCWAPYTLLMIIRAACHGRCIPDYWYETSFWLLWANSAVNPVLYPLCHYSFR
RAFTKLLCPQKLKVQPHGSLEQCWK
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BDBM50327477 |
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n/a |
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Name | BDBM50327477 |
Synonyms: | (R)-2-(cyclopropylmethyl)-8-(1-isopropylpiperidin-4-yloxy)-3-methyl-3,4-dihydropyrazino[1,2-a]indol-1(2H)-one | CHEMBL1257965 |
Type | Small organic molecule |
Emp. Form. | C24H33N3O2 |
Mol. Mass. | 395.5377 |
SMILES | CC(C)N1CCC(CC1)Oc1ccc2n3C[C@@H](C)N(CC4CC4)C(=O)c3cc2c1 |r| |
Structure |
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