Reaction Details
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G-protein coupled bile acid receptor 1
Ligand
BDBM21682
Substrate
BDBM10852
Meas. Tech.
TGR5 Activity Assay
pH
7.2±n/a
Temperature
310.15±n/a K
EC50
>51900±n/a nM
Comments
The efficacy=75% 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 Chem 50:4265-8 (2007) [PubMed] Article More Info.:
Target
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:
MTPNSTGEVPSPIPKGALGLSLALASLIITANLLLALGIAWDRRLRSPPAGCFFLSLLLAGLLTGLALPTLPGLWNQSRRGYWSCLLVYLAPNFSFLSLLANLLLVHGERYMAVLRPLQPPGSIRLALLLTWAGPLLFASLPALGWNHWTPGANCSSQAIFPAPYLYLEVYGLLLPAVGAAAFLSVRVLATAHRQLQDICRLERAVCRDEPSALARALTWRQARAQAGAMLLFGLCWGPYVATLLLSVLAYEQRPPLGPGTLLSLLSLGSASAAAVPVAMGLGDQRYTAPWRAAAQRCLQGLWGRASRDSPGPSIAYHPSSQSSVDLDLN
Inhibitor
Name:
BDBM21682
Synonyms:
(2R,4R)-2-methyl-4-[(1S,2S,5R,7S,9R,10R,11S,14R,15R,16S)-5,9,16-trihydroxy-2,15-dimethyltetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadecan-14-yl]pentanoic acid | 23(R)-methyl-BA derivative, 8d
Type:
Steroid
Emp. Form.:
C25H42O5
Mol. Mass.:
422.598
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])C[C@H](O)[C@]12C)[C@H](C)C[C@@H](C)C(O)=O
Structure:
Substrate