Reaction Details |
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Target | G-protein coupled bile acid receptor 1 |
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Ligand | BDBM18161 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_472949 (CHEMBL949256) |
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EC50 | 4490±n/a nM |
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Citation | Sato, H; Macchiarulo, A; Thomas, C; Gioiello, A; Une, M; Hofmann, AF; Saladin, R; Schoonjans, K; Pellicciari, R; Auwerx, J Novel potent and selective bile acid derivatives as TGR5 agonists: biological screening, structure-activity relationships, and molecular modeling studies. J Med Chem51:1831-41 (2008) [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 |
Synonyms: | BG37 | GPBAR1 | GPBAR_HUMAN | M-BAR | TGR5 | hBG37 | hGPCR19 |
Type: | G Protein-Coupled Receptor (GPCR) |
Mol. Mass.: | 35260.02 |
Organism: | Homo sapiens (Human) |
Description: | CHO cells transiently transfected with hTGR5. |
Residue: | 330 |
Sequence: | MTPNSTGEVPSPIPKGALGLSLALASLIITANLLLALGIAWDRRLRSPPAGCFFLSLLLA
GLLTGLALPTLPGLWNQSRRGYWSCLLVYLAPNFSFLSLLANLLLVHGERYMAVLRPLQP
PGSIRLALLLTWAGPLLFASLPALGWNHWTPGANCSSQAIFPAPYLYLEVYGLLLPAVGA
AAFLSVRVLATAHRQLQDICRLERAVCRDEPSALARALTWRQARAQAGAMLLFGLCWGPY
VATLLLSVLAYEQRPPLGPGTLLSLLSLGSASAAAVPVAMGLGDQRYTAPWRAAAQRCLQ
GLWGRASRDSPGPSIAYHPSSQSSVDLDLN
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BDBM18161 |
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n/a |
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Name | BDBM18161 |
Synonyms: | (1S,2S,7S,10R,11S,14S,15S)-14-hydroxy-2,15-dimethyltetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadecan-5-one | (5alpha,17beta)-17-hydroxyandrostan-3-one | CHEMBL27769 | DHT | Dihydrotestosterone | [3H]DHT |
Type | Steroid |
Emp. Form. | C19H30O2 |
Mol. Mass. | 290.4403 |
SMILES | [H][C@@]12CC[C@H](O)[C@@]1(C)CC[C@@]1([H])[C@@]2([H])CC[C@@]2([H])CC(=O)CC[C@]12C |r| |
Structure |
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