| Reaction Details |
|---|
 | Report a problem with these data |
| Target | G-protein coupled bile acid receptor 1 |
|---|
| Ligand | BDBM21674 |
|---|
| Substrate/Competitor | BDBM10852 |
|---|
| Meas. Tech. | TGR5 Activity Assay |
|---|
| pH | 7.2±n/a |
|---|
| Temperature | 310.15±n/a K |
|---|
| EC50 | 6710±n/a nM |
|---|
| Comments | The efficacy=105% of 10 uM LCA. |
|---|
| Citation |  Pellicciari, R; Sato, H; Gioiello, A; Costantino, G; Macchiarulo, A; Sadeghpour, BM; Giorgi, G; Schoonjans, K; Auwerx, J Nongenomic actions of bile acids. Synthesis and preliminary characterization of 23- and 6,23-alkyl-substituted bile acid derivatives as selective modulators for the G-protein coupled receptor TGR5. J Med Chem50:4265-8 (2007) [PubMed] Article |
|---|
| More Info.: | Get all data from this article, Solution Info, Assay Method |
|---|
| |
| G-protein coupled bile acid receptor 1 |
|---|
| 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
|
|
|
|---|
| BDBM21674 |
|---|
| BDBM10852 |
|---|
| Name | BDBM21674 |
|---|
| Synonyms: | (4R)-4-[(1S,2S,5R,7S,9R,10R,11S,14R,15R)-5,9-dihydroxy-2,15-dimethyltetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadecan-14-yl]pentanoic acid | CDCA | CHENODIOL | Chenodeoxycholic Acid | US10208081, CDCA |
|---|
| Type | Steroid |
|---|
| Emp. Form. | C24H40O4 |
|---|
| Mol. Mass. | 392.572 |
|---|
| SMILES | [H][C@@]1(CC[C@@]2([H])[C@]3([H])[C@H](O)C[C@]4([H])C[C@H](O)CC[C@]4(C)[C@@]3([H])CC[C@]12C)[C@H](C)CCC(O)=O |
|---|
| Structure | 
|
|---|
Search and Browse
