Reaction Details |
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Target | Thyroid hormone receptor alpha |
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Ligand | BDBM50115668 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1351955 (CHEMBL3266219) |
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EC50 | 3.0±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 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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BDBM50115668 |
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n/a |
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Name | BDBM50115668 |
Synonyms: | 3,5-dimethyl-4-(4'-hydroxy-3'-isopropylbenzyl)phenoxyacetic acid | CHEMBL107400 | GC-1 | US10322118, Entry 7 | US10544075, Compound GC-1 | [4-(4-Hydroxy-3-isopropyl-benzyl)-3,5-dimethyl-phenoxy]-acetic acid | [4-(4-Hydroxy-3-isopropyl-benzyl)-3,5-dimethyl-phenoxy]-acetic acid(GC-1) | {4-[4-hydroxy-3-(1-methylethyl)benzyl]-3,5-dimethylphenoxy}acetic acid |
Type | Small organic molecule |
Emp. Form. | C20H24O4 |
Mol. Mass. | 328.4022 |
SMILES | CC(C)c1cc(Cc2c(C)cc(OCC(O)=O)cc2C)ccc1O |
Structure |
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