Ki Summary BindingDB logo
myBDB logout
Reaction Details
Report a problem with these data
TargetThyroid hormone receptor
LigandBDBM50012910
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1351955
EC50 4290±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 Receptor▀ 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
Name:Thyroid hormone receptor
Synonyms:C-erbA-alpha | EAR-7 | EAR7 | Nuclear receptor subfamily 1 group A member 1 | Thyroid Hormone Receptor (TR-alpha) | Thyroid hormone receptor | Thyroid hormone receptor alpha | 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
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM50012910
NameBDBM50012910
Synonyms:CHEMBL3261326 | USRE46024, 14
TypeSmall organic molecule
Emp. Form.C16H16Cl2N2O3
Mol. Mass.355.216
SMILESCC(C)c1cc(Cc2c(Cl)cc(CC(O)=O)cc2Cl)n[nH]c1=O
Structure
Search PDB for entries with ligand similarity:Similarity to this molecule at least:
n/a