Reaction Details |
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Target | Histamine H3 receptor |
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Ligand | BDBM50317699 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_629414 (CHEMBL1105767) |
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Ki | 3.4±n/a nM |
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Citation | Stocking, EM; Aluisio, L; Atack, JR; Bonaventure, P; Carruthers, NI; Dugovic, C; Everson, A; Fraser, I; Jiang, X; Leung, P; Lord, B; Ly, KS; Morton, KL; Nepomuceno, D; Shah, CR; Shelton, J; Soyode-Johnson, A; Letavic, MA Novel substituted pyrrolidines are high affinity histamine H3 receptor antagonists. Bioorg Med Chem Lett20:2755-60 (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: | 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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BDBM50317699 |
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n/a |
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Name | BDBM50317699 |
Synonyms: | (4-cyclobutyl-1,4-diazepan-1-yl)((2R,4S)-4-(3-fluorophenoxy)pyrrolidin-2-yl)methanone | CHEMBL1095845 |
Type | Small organic molecule |
Emp. Form. | C20H28FN3O2 |
Mol. Mass. | 361.4536 |
SMILES | Fc1cccc(O[C@@H]2CN[C@H](C2)C(=O)N2CCCN(CC2)C2CCC2)c1 |r| |
Structure |
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