Reaction Details |
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Target | Thyroid hormone receptor beta |
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Ligand | BDBM18913 |
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Substrate/Competitor | BDBM18860 |
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Meas. Tech. | TRalpha-Binding Assay. |
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IC50 | 0.2±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 beta |
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Name: | Thyroid hormone receptor beta |
Synonyms: | ERBA2 | NR1A2 | Nuclear receptor subfamily 1 group A member 2 | THB_HUMAN | THR1 | THRB | c-erbA-2 | c-erbA-beta |
Type: | Receptor |
Mol. Mass.: | 52793.62 |
Organism: | Homo sapiens (Human) |
Description: | Recombinant hThR was obtained from nuclear extracts from SF9 cells infected with baculovirus vectors encoding for ThRbeta 1. |
Residue: | 461 |
Sequence: | MTPNSMTENGLTAWDKPKHCPDREHDWKLVGMSEACLHRKSHSERRSTLKNEQSSPHLIQ
TTWTSSIFHLDHDDVNDQSVSSAQTFQTEEKKCKGYIPSYLDKDELCVVCGDKATGYHYR
CITCEGCKGFFRRTIQKNLHPSYSCKYEGKCVIDKVTRNQCQECRFKKCIYVGMATDLVL
DDSKRLAKRKLIEENREKRRREELQKSIGHKPEPTDEEWELIKTVTEAHVATNAQGSHWK
QKRKFLPEDIGQAPIVNAPEGGKVDLEAFSHFTKIITPAITRVVDFAKKLPMFCELPCED
QIILLKGCCMEIMSLRAAVRYDPESETLTLNGEMAVTRGQLKNGGLGVVSDAIFDLGMSL
SSFNLDDTEVALLQAVLLMSSDRPGLACVERIEKYQDSFLLAFEHYINYRKHHVTHFWPK
LLMKVTDLRMIGACHASRFLHMKVECPTELFPPLFLEVFED
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BDBM18913 |
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BDBM18860 |
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Name | BDBM18913 |
Synonyms: | 2-{3,5-dichloro-4-[3-(3-ethylphenyl)-4-hydroxyphenoxy]phenyl}acetic acid | 4-hydroxy bioisosteric thyromimetics, 3 | 4-hydroxy thyromimetic, 9e |
Type | Small organic molecule |
Emp. Form. | C22H18Cl2O4 |
Mol. Mass. | 417.282 |
SMILES | CCc1cccc(c1)-c1cc(Oc2c(Cl)cc(CC(O)=O)cc2Cl)ccc1O |
Structure |
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