| Reaction Details |
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 | Report a problem with these data |
| Target | Thyroid hormone receptor alpha |
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| Ligand | BDBM18886 |
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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 | 36±3 nM |
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| EC50 | 32±n/a nM |
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| Comments | antagonist |
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| Citation |  Koehler, K; Gordon, S; Brandt, P; Carlsson, B; Bäcksbro-Saeidi, A; Apelqvist, T; Agback, P; Grover, GJ; Nelson, W; Grynfarb, M; Färnegård, M; Rehnmark, S; Malm, J Thyroid receptor ligands. 6. A high affinity "direct antagonist" selective for the thyroid hormone receptor. J Med Chem49:6635-7 (2006) [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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| BDBM18886 |
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| BDBM18860 |
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| Name | BDBM18886 |
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| Synonyms: | 3-{3,5-dibromo-4-[4-hydroxy-3-(propan-2-yl)-5-[(E)-2-(pyridin-4-yl)ethenyl]phenoxy]phenyl}propanoic acid | JMC496635 Compound 6 | thyromimetic, 6 |
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| Type | Small organic molecule |
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| Emp. Form. | C25H23Br2NO4 |
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| Mol. Mass. | 561.262 |
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| SMILES | CC(C)c1cc(Oc2c(Br)cc(CCC(O)=O)cc2Br)cc(\C=C\c2ccncc2)c1O |
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| Structure | 
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