| Reaction Details |
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 | Report a problem with these data |
| Target | Thyroid hormone receptor alpha |
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| Ligand | BDBM18894 |
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| Substrate/Competitor | BDBM18860 |
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| Meas. Tech. | TRalpha-Binding Assay and Thyroid Response Element (TRAFalpha1) Reporter Assay. |
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| pH | 7±n/a |
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| Temperature | 277.15±n/a K |
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| IC50 | 99±n/a nM |
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| EC50 | 380±n/a nM |
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| Comments | 80% antagonism. |
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| Citation |  Malm, J; Gordon, S; Brandt, P; Carlsson, B; Agback, P; Bäckbro Saeidi, A; Sandberg, J Thyroid receptor ligands. Part 7: Indirect antagonists of the thyroid hormone receptor with improved affinity. Bioorg Med Chem Lett17:2018-21 (2007) [PubMed] Article |
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| More Info.: | Get all data from this article, Solution Info, Assay Method |
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| Thyroid hormone receptor alpha |
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| Name: | Thyroid hormone receptor alpha |
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| Synonyms: | C-erbA-alpha | EAR-7 | EAR7 | ERBA1 | NR1A1 | Nuclear receptor subfamily 1 group A member 1 | THA_HUMAN | THRA | THRA1 | THRA2 | Thyroid Hormone Receptor (TR-alpha) | Thyroid hormone receptor | Thyroid hormone receptor alpha | Thyroid hormone receptor apha | c-erbA-1 |
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| Type: | Receptor |
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| Mol. Mass.: | 54818.00 |
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| Organism: | Homo sapiens (Human) |
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| Description: | Recombinant hThR was obtained from nuclear extracts from SF9 cells infected with baculovirus vectors encoding for ThRalpha 1. |
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| Residue: | 490 |
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| Sequence: | MEQKPSKVECGSDPEENSARSPDGKRKRKNGQCSLKTSMSGYIPSYLDKDEQCVVCGDKA
TGYHYRCITCEGCKGFFRRTIQKNLHPTYSCKYDSCCVIDKITRNQCQLCRFKKCIAVGM
AMDLVLDDSKRVAKRKLIEQNRERRRKEEMIRSLQQRPEPTPEEWDLIHIATEAHRSTNA
QGSHWKQRRKFLPDDIGQSPIVSMPDGDKVDLEAFSEFTKIITPAITRVVDFAKKLPMFS
ELPCEDQIILLKGCCMEIMSLRAAVRYDPESDTLTLSGEMAVKREQLKNGGLGVVSDAIF
ELGKSLSAFNLDDTEVALLQAVLLMSTDRSGLLCVDKIEKSQEAYLLAFEHYVNHRKHNI
PHFWPKLLMKEREVQSSILYKGAAAEGRPGGSLGVHPEGQQLLGMHVVQGPQVRQLEQQL
GEAGSLQGPVLQHQSPKSPQQRLLELLHRSGILHARAVCGEDDSSEADSPSSSEEEPEVC
EDLAGNAASP
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| BDBM18894 |
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| BDBM18860 |
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| Name | BDBM18894 |
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| Synonyms: | 3-{3,5-dibromo-4-[(3-bromophenyl)methoxy]phenyl}propanoic acid | benzyl derivative, 11f |
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| Type | Small organic molecule |
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| Emp. Form. | C16H13Br3O3 |
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| Mol. Mass. | 492.985 |
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| SMILES | OC(=O)CCc1cc(Br)c(OCc2cccc(Br)c2)c(Br)c1 |
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| Structure | 
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