Reaction Details Report a problem with these data
Target
Bile acid receptor
Ligand
BDBM28530
Substrate
BDBM10852
Meas. Tech.
FXR Co-transfection Assay
pH
7±n/a
Temperature
295.15±n/a K
EC50
500±n/a nM
Comments
120% efficacy.
Citation
 Flatt, B; Martin, R; Wang, TL; Mahaney, P; Murphy, B; Gu, XH; Foster, P; Li, J; Pircher, P; Petrowski, M; Schulman, I; Westin, S; Wrobel, J; Yan, G; Bischoff, E; Daige, C; Mohan, R Discovery of XL335 (WAY-362450), a Highly Potent, Selective, and Orally Active Agonist of the Farnesoid X Receptor (FXR). J Med Chem 52:904-7 (2009) [PubMed]  Article 
Target
Name:
Bile acid receptor
Synonyms:
BAR | Bile acid receptor FXR | FXR | Farnesol receptor HRR-1 | HRR1 | NR1H4 | NR1H4_HUMAN | Nuclear receptor subfamily 1 group H member 4 | RIP14 | RXR-interacting protein 14 | Retinoid X receptor-interacting protein 14 | farnesoid x receptor
Type:
Nuclear Receptor
Mol. Mass.:
55916.24
Organism:
Homo sapiens (Human)
Description:
Q96RI1
Residue:
486
Sequence:
MVMQFQGLENPIQISPHCSCTPSGFFMEMMSMKPAKGVLTEQVAGPLGQNLEVEPYSQYSNVQFPQVQPQISSSSYYSNLGFYPQQPEEWYSPGIYELRRMPAETLYQGETEVAEMPVTKKPRMGASAGRIKGDELCVVCGDRASGYHYNALTCEGCKGFFRRSITKNAVYKCKNGGNCVMDMYMRRKCQECRLRKCKEMGMLAECMYTGLLTEIQCKSKRLRKNVKQHADQTVNEDSEGRDLRQVTSTTKSCREKTELTPDQQTLLHFIMDSYNKQRMPQEITNKILKEEFSAEENFLILTEMATNHVQVLVEFTKKLPGFQTLDHEDQIALLKGSAVEAMFLRSAEIFNKKLPSGHSDLLEERIRNSGISDEYITPMFSFYKSIGELKMTQEEYALLTAIVILSPDRQYIKDREAVEKLQEPLLDVLQKLCKIHQPENPQHFACLLGRLTELRTFNHHHAEMLMSWRVNDHKFTPLLCEIWDVQ
  
Inhibitor
Name:
BDBM28530
Synonyms:
Azepino[4,5-b]indole, 6a | propan-2-yl 3-[(4-fluorophenyl)carbonyl]-1H,2H,3H,6H-azepino[4,5-b]indole-5-carboxylate
Type:
Small organic molecule
Emp. Form.:
C23H21FN2O3
Mol. Mass.:
392.4228
SMILES:
CC(C)OC(=O)C1=CN(CCc2c1[nH]c1ccccc21)C(=O)c1ccc(F)cc1 |t:6|
Structure:
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Substrate