Reaction Details |
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Target | Bile acid receptor |
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Ligand | BDBM50094268 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1503730 (CHEMBL3592510) |
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EC50 | 2900±n/a nM |
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Citation | Flesch, D; Gabler, M; Lill, A; Gomez, RC; Steri, R; Schneider, G; Stark, H; Schubert-Zsilavecz, M; Merk, D Fragmentation of GW4064 led to a highly potent partial farnesoid X receptor agonist with improved drug-like properties. Bioorg Med Chem23:3490-8 (2015) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Bile acid receptor |
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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: | MVMQFQGLENPIQISPHCSCTPSGFFMEMMSMKPAKGVLTEQVAGPLGQNLEVEPYSQYS
NVQFPQVQPQISSSSYYSNLGFYPQQPEEWYSPGIYELRRMPAETLYQGETEVAEMPVTK
KPRMGASAGRIKGDELCVVCGDRASGYHYNALTCEGCKGFFRRSITKNAVYKCKNGGNCV
MDMYMRRKCQECRLRKCKEMGMLAECMYTGLLTEIQCKSKRLRKNVKQHADQTVNEDSEG
RDLRQVTSTTKSCREKTELTPDQQTLLHFIMDSYNKQRMPQEITNKILKEEFSAEENFLI
LTEMATNHVQVLVEFTKKLPGFQTLDHEDQIALLKGSAVEAMFLRSAEIFNKKLPSGHSD
LLEERIRNSGISDEYITPMFSFYKSIGELKMTQEEYALLTAIVILSPDRQYIKDREAVEK
LQEPLLDVLQKLCKIHQPENPQHFACLLGRLTELRTFNHHHAEMLMSWRVNDHKFTPLLC
EIWDVQ
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BDBM50094268 |
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n/a |
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Name | BDBM50094268 |
Synonyms: | CHEMBL3589969 |
Type | Small organic molecule |
Emp. Form. | C16H11F3N2O2 |
Mol. Mass. | 320.2659 |
SMILES | COc1ccc(cc1)-c1nc(no1)-c1cccc(c1)C(F)(F)F |
Structure |
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