Reaction Details |
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Target | Thyroid hormone receptor beta |
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Ligand | BDBM18916 |
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Substrate/Competitor | BDBM18860 |
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Meas. Tech. | TRbeta-Binding Assay |
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pH | 7±n/a |
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Temperature | 277.15±n/a K |
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IC50 | 4.3±n/a nM |
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Citation | Li, YL; Litten, C; Koehler, KF; Mellström, K; Garg, N; Garcia Collazo, AM; Färnegård, M; Grynfarb, M; Husman, B; Sandberg, J; Malm, J Thyroid receptor ligands. Part 4: 4'-amido bioisosteric ligands selective for the thyroid hormone receptor beta. Bioorg Med Chem Lett16:884-6 (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 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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BDBM18916 |
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BDBM18860 |
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Name | BDBM18916 |
Synonyms: | 2-{4-[3-bromo-4-(2-methylbutanamido)phenoxy]-3,5-dichlorophenyl}acetic acid | 4-amido bioisosteric ligand, 12c |
Type | Small organic molecule |
Emp. Form. | C19H18BrCl2NO4 |
Mol. Mass. | 475.161 |
SMILES | CCC(C)C(=O)Nc1ccc(Oc2c(Cl)cc(CC(O)=O)cc2Cl)cc1Br |
Structure |
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