Reaction Details |
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Target | Thyroid hormone receptor alpha |
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Ligand | BDBM18867 |
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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 | 1.4±0.44 nM |
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EC50 | 0.38±n/a nM |
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Citation | Garg, N; Li, YL; Garcia Collazo, AM; Litten, C; Ryono, DE; Zhang, M; Caringal, Y; Brigance, RP; Meng, W; Washburn, WN; Agback, P; Mellström, K; Rehnmark, S; Rahimi-Ghadim, M; Norin, T; Grynfarb, M; Sandberg, J; Grover, G; Malm, J Thyroid receptor ligands. Part 8: Thyromimetics derived from N-acylated-alpha-amino acid derivatives displaying modulated pharmacological selectivity compared with KB-141. Bioorg Med Chem Lett17:4131-4 (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 |
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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BDBM18867 |
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BDBM18860 |
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Name | BDBM18867 |
Synonyms: | 2-{3,5-dibromo-4-[4-hydroxy-3-(propan-2-yl)phenoxy]phenyl}acetic acid | KB-131092 | dibromo phenylacetic acid, 11a |
Type | Small organic molecule |
Emp. Form. | C17H16Br2O4 |
Mol. Mass. | 444.115 |
SMILES | CC(C)c1cc(Oc2c(Br)cc(CC(O)=O)cc2Br)ccc1O |
Structure |
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