Reaction Details |
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Target | Thyroid hormone receptor alpha |
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Ligand | BDBM18949 |
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Substrate/Competitor | BDBM18860 |
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Meas. Tech. | TRalpha-Binding Assay. |
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IC50 | 203±n/a nM |
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Citation | Hangeland, JJ; Doweyko, AM; Dejneka, T; Friends, TJ; Devasthale, P; Mellström, K; Sandberg, J; Grynfarb, M; Sack, JS; Einspahr, H; Färnegård, M; Husman, B; Ljunggren, J; Koehler, K; Sheppard, C; Malm, J; Ryono, DE Thyroid receptor ligands. Part 2: Thyromimetics with improved selectivity for the thyroid hormone receptor beta. Bioorg Med Chem Lett14:3549-53 (2004) [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 |
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 |
Type: | Receptor |
Mol. Mass.: | 54818.00 |
Organism: | Homo sapiens (Human) |
Description: | Recombinant hThR was obtained from nuclear extracts from SF9 cells infected with baculovirus vectors encoding for ThRalpha 1. |
Residue: | 490 |
Sequence: | MEQKPSKVECGSDPEENSARSPDGKRKRKNGQCSLKTSMSGYIPSYLDKDEQCVVCGDKA
TGYHYRCITCEGCKGFFRRTIQKNLHPTYSCKYDSCCVIDKITRNQCQLCRFKKCIAVGM
AMDLVLDDSKRVAKRKLIEQNRERRRKEEMIRSLQQRPEPTPEEWDLIHIATEAHRSTNA
QGSHWKQRRKFLPDDIGQSPIVSMPDGDKVDLEAFSEFTKIITPAITRVVDFAKKLPMFS
ELPCEDQIILLKGCCMEIMSLRAAVRYDPESDTLTLSGEMAVKREQLKNGGLGVVSDAIF
ELGKSLSAFNLDDTEVALLQAVLLMSTDRSGLLCVDKIEKSQEAYLLAFEHYVNHRKHNI
PHFWPKLLMKEREVQSSILYKGAAAEGRPGGSLGVHPEGQQLLGMHVVQGPQVRQLEQQL
GEAGSLQGPVLQHQSPKSPQQRLLELLHRSGILHARAVCGEDDSSEADSPSSSEEEPEVC
EDLAGNAASP
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BDBM18949 |
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BDBM18860 |
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Name | BDBM18949 |
Synonyms: | 2-(3,5-dibromo-4-{4-hydroxy-3-[(3-phenylpropyl)carbamoyl]phenoxy}phenyl)acetic acid | 4-hydroxy thyromimetic, 15d |
Type | Small organic molecule |
Emp. Form. | C24H21Br2NO5 |
Mol. Mass. | 563.235 |
SMILES | OC(=O)Cc1cc(Br)c(Oc2ccc(O)c(c2)C(=O)NCCCc2ccccc2)c(Br)c1 |
Structure |
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