Reaction Details |
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Target | 5-hydroxytryptamine receptor 2B |
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Ligand | BDBM50429650 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_946217 (CHEMBL2344541) |
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Ki | 3160±n/a nM |
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Citation | Hao, J; Dehlinger, V; Fivush, AM; Rudyk, HC; Britton, TC; Hollinshead, SP; Vokits, BP; Clark, BP; Henry, SS; Massey, SM; Peng, L; Dressman, BA; Heinz, BA; Roberts, EF; Bracey-Walker, MR; Swanson, S; Catlow, JT; Love, PL; Tepool, AD; Peters, SC; Simmons, RM; Iyengar, S; McKinzie, DL; Monn, JA Discovery of (1R,2R)-N-(4-(6-isopropylpyridin-2-yl)-3-(2-methyl-2H-indazol-5-yl)isothiazol-5-yl)-2-methylcyclopropanecarboxamide, a potent and orally efficacious mGlu5 receptor negative allosteric modulator. Bioorg Med Chem Lett23:1249-52 (2013) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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5-hydroxytryptamine receptor 2B |
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Name: | 5-hydroxytryptamine receptor 2B |
Synonyms: | 5-HT-2B | 5-HT2B | 5-hydroxytryptamine (serotonin) receptor 2B [Homo sapiens] | 5-hydroxytryptamine receptor 2B (5-HT2B) | 5-hydroxytryptamine receptor 2C (5HT2C) | 5HT2B_HUMAN | HTR2B | Serotonin (5-HT3) receptor | Serotonin 2b (5-HT2b) receptor | Serotonin Receptor 2B |
Type: | G Protein-Coupled Receptor (GPCR) |
Mol. Mass.: | 54312.47 |
Organism: | Homo sapiens (Human) |
Description: | Receptor binding assays were performed using human clone stably expressed in CHO cells. |
Residue: | 481 |
Sequence: | MALSYRVSELQSTIPEHILQSTFVHVISSNWSGLQTESIPEEMKQIVEEQGNKLHWAALL
ILMVIIPTIGGNTLVILAVSLEKKLQYATNYFLMSLAVADLLVGLFVMPIALLTIMFEAM
WPLPLVLCPAWLFLDVLFSTASIMHLCAISVDRYIAIKKPIQANQYNSRATAFIKITVVW
LISIGIAIPVPIKGIETDVDNPNNITCVLTKERFGDFMLFGSLAAFFTPLAIMIVTYFLT
IHALQKKAYLVKNKPPQRLTWLTVSTVFQRDETPCSSPEKVAMLDGSRKDKALPNSGDET
LMRRTSTIGKKSVQTISNEQRASKVLGIVFFLFLLMWCPFFITNITLVLCDSCNQTTLQM
LLEIFVWIGYVSSGVNPLVYTLFNKTFRDAFGRYITCNYRATKSVKTLRKRSSKIYFRNP
MAENSKFFKKHGIRNGINPAMYQSPMRLRSSTIQSSSIILLDTLLLTENEGDKTEEQVSY
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BDBM50429650 |
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n/a |
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Name | BDBM50429650 |
Synonyms: | CHEMBL2334981 |
Type | Small organic molecule |
Emp. Form. | C24H25N5OS |
Mol. Mass. | 431.553 |
SMILES | CC(C)c1cccc(n1)-c1c(NC(=O)[C@@H]2C[C@H]2C)snc1-c1ccc2nn(C)cc2c1 |r| |
Structure |
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