Target
Thyroid hormone receptor beta
Ligand
BDBM50012901
Substrate
n/a
Meas. Tech.
ChEMBL_1351953 (CHEMBL3266217)
EC50
2380±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 Chem 57:3912-23 (2014) [PubMed]  Article 
Target
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:
MTPNSMTENGLTAWDKPKHCPDREHDWKLVGMSEACLHRKSHSERRSTLKNEQSSPHLIQTTWTSSIFHLDHDDVNDQSVSSAQTFQTEEKKCKGYIPSYLDKDELCVVCGDKATGYHYRCITCEGCKGFFRRTIQKNLHPSYSCKYEGKCVIDKVTRNQCQECRFKKCIYVGMATDLVLDDSKRLAKRKLIEENREKRRREELQKSIGHKPEPTDEEWELIKTVTEAHVATNAQGSHWKQKRKFLPEDIGQAPIVNAPEGGKVDLEAFSHFTKIITPAITRVVDFAKKLPMFCELPCEDQIILLKGCCMEIMSLRAAVRYDPESETLTLNGEMAVTRGQLKNGGLGVVSDAIFDLGMSLSSFNLDDTEVALLQAVLLMSSDRPGLACVERIEKYQDSFLLAFEHYINYRKHHVTHFWPKLLMKVTDLRMIGACHASRFLHMKVECPTELFPPLFLEVFED
  
Inhibitor
Name:
BDBM50012901
Synonyms:
CHEMBL3261320 | USRE46024, 4
Type:
Small organic molecule
Emp. Form.:
C15H14Cl2N2O4
Mol. Mass.:
357.189
SMILES:
CC(C)c1cc(Oc2c(Cl)cc(CC(O)=O)cc2Cl)n[nH]c1=O
Structure:
Search PDB for entries with ligand similarity: