Reaction Details |
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Target | Thyroid hormone receptor beta |
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Ligand | BDBM50610163 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_2280286 |
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IC50 | >5000±n/a nM |
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Citation | Orsi, DL; Ferrara, SJ; Siegel, S; Friberg, A; Bouché, L; Pook, E; Lienau, P; Bluck, JP; Lemke, CT; Akcay, G; Stellfeld, T; Meyer, H; Pütter, V; Holton, SJ; Korr, D; Jerchel-Furau, I; Pantelidou, C; Strathdee, CA; Meyerson, M; Eis, K; Goldstein, JT Discovery and characterization of orally bioavailable 4-chloro-6-fluoroisophthalamides as covalent PPARG inverse-agonists. Bioorg Med Chem78:0 (2023) [PubMed] |
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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 |
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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BDBM50610163 |
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n/a |
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Name | BDBM50610163 |
Synonyms: | CHEMBL5267263 |
Type | Small organic molecule |
Emp. Form. | C23H17ClF4N2O3 |
Mol. Mass. | 480.839 |
SMILES | Cc1cc(OC(F)F)ccc1NC(=O)c1cc(C(=O)NCc2ccc(F)cc2)c(F)cc1Cl |
Structure |
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