Reaction Details |
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Target | Histamine H3 receptor |
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Ligand | BDBM50274651 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_537241 (CHEMBL981856) |
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IC50 | 37±n/a nM |
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Citation | Nagase, T; Mizutani, T; Sekino, E; Ishikawa, S; Ito, S; Mitobe, Y; Miyamoto, Y; Yoshimoto, R; Tanaka, T; Ishihara, A; Takenaga, N; Tokita, S; Sato, 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 |
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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: | 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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BDBM50274651 |
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n/a |
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Name | BDBM50274651 |
Synonyms: | 3-(4-[(1-Cyclopentyl-3-pyrrolidinyl)oxy]phenyl)-2-methyl-4(3H)-quinazolinone | CHEMBL521503 |
Type | Small organic molecule |
Emp. Form. | C24H27N3O2 |
Mol. Mass. | 389.4901 |
SMILES | Cc1nc2ccccc2c(=O)n1-c1ccc(OC2CCN(C2)C2CCCC2)cc1 |
Structure |
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