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Target
Bile acid receptor
Ligand
BDBM30333
Substrate
BDBM10852
Meas. Tech.
Scintillation Proximity Assay (IC50) and Cell-Based Transactivation Assay (EC50)
pH
8±n/a
Temperature
295.15±n/a K
IC50
250±n/a nM
EC50
10000±n/a nM
Comments
54.3% efficacy.
Citation
 Feng, S; Yang, M; Zhang, Z; Wang, Z; Hong, D; Richter, H; Benson, GM; Bleicher, K; Grether, U; Martin, RE; Plancher, JM; Kuhn, B; Rudolph, MG; Chen, L Identification of an N-oxide pyridine GW4064 analog as a potent FXR agonist. Bioorg Med Chem Lett 19:2595-8 (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:
BDBM30333
Synonyms:
3-aryl isoxazole analog, 6b
Type:
Small organic molecule
Emp. Form.:
C29H26ClNO5
Mol. Mass.:
503.973
SMILES:
COc1ccccc1-c1noc(C(C)C)c1COc1ccc(\C=C\c2cccc(c2)C(O)=O)c(Cl)c1
Structure:
Search PDB for entries with ligand similarity:
Substrate