Target
Thyroid hormone receptor beta
Ligand
BDBM50123058
Substrate
n/a
Meas. Tech.
ChEBML_210497
Ki
0.020000±n/a nM
Citation
 Dow, RLSchneider, SRPaight, ESHank, RFChiang, PCornelius, PLee, ENewsome, WPSwick, AGSpitzer, JHargrove, DMPatterson, TAPandit, JChrunyk, BALeMotte, PKDanley, DERosner, MHAmmirati, MJSimons, SPSchulte, GKTate, BFDaSilva-Jardine, P Discovery of a novel series of 6-azauracil-based thyroid hormone receptor ligands: potent, TR beta subtype-selective thyromimetics. Bioorg Med Chem Lett 13:379-82 (2003) [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:
BDBM50123058
Synonyms:
2-(3,5-dichloro-4-(4-hydroxy-3-(piperidin-1-ylsulfonyl)phenoxy)phenyl)-1,2,4-triazine-3,5(2H,4H)-dione | 2-{3,5-Dichloro-4-[4-hydroxy-3-(piperidine-1-sulfonyl)-phenoxy]-phenyl}-2H-[1,2,4]triazine-3,5-dione | CHEMBL124126
Type:
Small organic molecule
Emp. Form.:
C20H18Cl2N4O6S
Mol. Mass.:
513.351
SMILES:
Oc1ccc(Oc2c(Cl)cc(cc2Cl)-n2ncc(=O)[nH]c2=O)cc1S(=O)(=O)N1CCCCC1
Structure:
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