| Reaction Details |
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 | Report a problem with these data |
| Target | Thyroid hormone receptor beta |
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| Ligand | BDBM50012907 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_1351953 (CHEMBL3266217) |
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| EC50 | 90±n/a nM |
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| Citation |  Kelly, MJ; Pietranico-Cole, S; Larigan, JD; Haynes, NE; Reynolds, CH; Scott, N; Vermeulen, J; Dvorozniak, M; Conde-Knape, K; Huang, KS; So, SS; Thakkar, K; Qian, Y; Banner, B; Mennona, F; Danzi, S; Klein, I; Taub, R; Tilley, J Discovery of 2-[3,5-dichloro-4-(5-isopropyl-6-oxo-1,6-dihydropyridazin-3-yloxy)phenyl]-3,5-dioxo-2,3,4,5-tetrahydro[1,2,4]triazine-6-carbonitrile (MGL-3196), a Highly Selective Thyroid Hormone Receptorß agonist in clinical trials for the treatment of dyslipidemia. J Med Chem57:3912-23 (2014) [PubMed] Article |
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| More Info.: | Get all data from this article, Assay Method |
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| Thyroid hormone receptor beta |
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| Name: | Thyroid hormone receptor beta |
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| Synonyms: | ERBA2 | NR1A2 | Nuclear receptor subfamily 1 group A member 2 | THB_HUMAN | THR1 | THRB | c-erbA-2 | c-erbA-beta |
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| Type: | Receptor |
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| Mol. Mass.: | 52793.62 |
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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 ThRbeta 1. |
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| Residue: | 461 |
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| Sequence: | MTPNSMTENGLTAWDKPKHCPDREHDWKLVGMSEACLHRKSHSERRSTLKNEQSSPHLIQ
TTWTSSIFHLDHDDVNDQSVSSAQTFQTEEKKCKGYIPSYLDKDELCVVCGDKATGYHYR
CITCEGCKGFFRRTIQKNLHPSYSCKYEGKCVIDKVTRNQCQECRFKKCIYVGMATDLVL
DDSKRLAKRKLIEENREKRRREELQKSIGHKPEPTDEEWELIKTVTEAHVATNAQGSHWK
QKRKFLPEDIGQAPIVNAPEGGKVDLEAFSHFTKIITPAITRVVDFAKKLPMFCELPCED
QIILLKGCCMEIMSLRAAVRYDPESETLTLNGEMAVTRGQLKNGGLGVVSDAIFDLGMSL
SSFNLDDTEVALLQAVLLMSSDRPGLACVERIEKYQDSFLLAFEHYINYRKHHVTHFWPK
LLMKVTDLRMIGACHASRFLHMKVECPTELFPPLFLEVFED
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| BDBM50012907 |
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| n/a |
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| Name | BDBM50012907 |
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| Synonyms: | CHEMBL3261336 | USRE46024, 13 |
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| Type | Small organic molecule |
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| Emp. Form. | C17H15Cl2N5O3 |
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| Mol. Mass. | 408.239 |
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| SMILES | CC(C)c1cc(Cc2c(Cl)cc(cc2Cl)-n2ncc(=O)[nH]c2=O)n[nH]c1=O |
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| Structure | 
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