| Reaction Details |
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 | Report a problem with these data |
| Target | G-protein coupled bile acid receptor 1 |
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| Ligand | BDBM50428103 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_943955 (CHEMBL2339922) |
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| EC50 | 3.3±n/a nM |
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| Citation |  Piotrowski, DW; Futatsugi, K; Warmus, JS; Orr, ST; Freeman-Cook, KD; Londregan, AT; Wei, L; Jennings, SM; Herr, M; Coffey, SB; Jiao, W; Storer, G; Hepworth, D; Wang, J; Lavergne, SY; Chin, JE; Hadcock, JR; Brenner, MB; Wolford, AC; Janssen, AM; Roush, NS; Buxton, J; Hinchey, T; Kalgutkar, AS; Sharma, R; Flynn, DA Identification of Tetrahydropyrido[4,3-d]pyrimidine Amides as a New Class of Orally Bioavailable TGR5 Agonists. ACS Med Chem Lett4:63-8 (2013) [PubMed] Article |
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| More Info.: | Get all data from this article, Assay Method |
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| G-protein coupled bile acid receptor 1 |
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| Name: | G-protein coupled bile acid receptor 1 |
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| Synonyms: | BG37 | GPBAR1 | GPBAR_HUMAN | M-BAR | TGR5 | hBG37 | hGPCR19 |
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| Type: | G Protein-Coupled Receptor (GPCR) |
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| Mol. Mass.: | 35260.02 |
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| Organism: | Homo sapiens (Human) |
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| Description: | CHO cells transiently transfected with hTGR5. |
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| Residue: | 330 |
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| Sequence: | MTPNSTGEVPSPIPKGALGLSLALASLIITANLLLALGIAWDRRLRSPPAGCFFLSLLLA
GLLTGLALPTLPGLWNQSRRGYWSCLLVYLAPNFSFLSLLANLLLVHGERYMAVLRPLQP
PGSIRLALLLTWAGPLLFASLPALGWNHWTPGANCSSQAIFPAPYLYLEVYGLLLPAVGA
AAFLSVRVLATAHRQLQDICRLERAVCRDEPSALARALTWRQARAQAGAMLLFGLCWGPY
VATLLLSVLAYEQRPPLGPGTLLSLLSLGSASAAAVPVAMGLGDQRYTAPWRAAAQRCLQ
GLWGRASRDSPGPSIAYHPSSQSSVDLDLN
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| BDBM50428103 |
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| n/a |
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| Name | BDBM50428103 |
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| Synonyms: | CHEMBL2331654 |
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| Type | Small organic molecule |
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| Emp. Form. | C20H21F3N4O4 |
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| Mol. Mass. | 438.4003 |
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| SMILES | CCOc1nc2CCN(Cc2c(n1)C(N)=O)C(=O)CCc1ccc(OC(F)(F)F)cc1 |
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| Structure | 
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