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TargetThyroid hormone receptor alpha
LigandBDBM50115668
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1351955 (CHEMBL3266219)
EC50 3.0±n/a nM
Citation Kelly, MJPietranico-Cole, SLarigan, JDHaynes, NEReynolds, CHScott, NVermeulen, JDvorozniak, MConde-Knape, KHuang, KSSo, SSThakkar, KQian, YBanner, BMennona, FDanzi, SKlein, ITaub, RTilley, 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
More Info.:Get all data from this article,  Assay Method
 
Thyroid hormone receptor alpha
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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  Blast E-value cutoff:
BDBM50115668
n/a
NameBDBM50115668
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
TypeSmall organic molecule
Emp. Form.C20H24O4
Mol. Mass.328.4022
SMILESCC(C)c1cc(Cc2c(C)cc(OCC(O)=O)cc2C)ccc1O
Structure
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