Target
Bile acid receptor
Ligand
BDBM30326
Substrate
biotin-tagged SRC-1
Meas. Tech.
HTRF Coactivator Recruitment Assay
pH
7±n/a
Temperature
277.15±n/a K
EC50
16.9±n/a nM
Citation
 Soisson, SMParthasarathy, GAdams, ADSahoo, SSitlani, ASparrow, CCui, JBecker, JW Identification of a potent synthetic FXR agonist with an unexpected mode of binding and activation. Proc Natl Acad Sci U S A 105:5337-42 (2008) [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:
BDBM30326
Synonyms:
MFA-1
Type:
Steroid
Emp. Form.:
C27H32O4
Mol. Mass.:
420.5406
SMILES:
C[C@]12CCC3C(CC=C4C=C(CC[C@]34C)C(O)=O)C1CC[C@@H]2C(=O)c1ccc(O)cc1 |r,c:9,t:7|
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
Nuclear receptor coactivator 1 (aa 568-780)
Synonyms:
BHLHE74 | NCOA1 | NCOA1_HUMAN | SRC1 | Steroid receptor coactivator 1 (aa 568-780)
Type:
Other Protein Type
Mol. Mass.:
23127.68
Organism:
Homo sapiens (Human)
Description:
Q15788 aa 568-780
Residue:
213
Sequence:
NSPSRLNIQPAKAESKDNKEIASILNEMIQSDNSSSDGKPLDSGLLHNNDRLSDGDSKYSQTSHKLVQLLTTTAEQQLRHADIDTSCKDVLSCTGTSNSASANSSGGSCPSSHSSLTERHKILHRLLQEGSPSDITTLSVEPDKKDSASTSVSVTGQVQGNSSIKLELDASKKKESKDHQLLRYLLDKDEKDLRSTPNLSLDDVKVKVEKKEQ