Target
Thyroid hormone receptor alpha
Ligand
BDBM426634
Substrate
n/a
Meas. Tech.
transactivation assay
EC50
7.96±6.95 nM
Citation
 Scanlan, TDevereaux, JPlaczek, ABanerji, TFerrara, SMeinig, JMBanerji, T Derivatives of sobetirome US Patent  US10544075 Publication Date 1/28/2020 
Target
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:
MEQKPSKVECGSDPEENSARSPDGKRKRKNGQCSLKTSMSGYIPSYLDKDEQCVVCGDKATGYHYRCITCEGCKGFFRRTIQKNLHPTYSCKYDSCCVIDKITRNQCQLCRFKKCIAVGMAMDLVLDDSKRVAKRKLIEQNRERRRKEEMIRSLQQRPEPTPEEWDLIHIATEAHRSTNAQGSHWKQRRKFLPDDIGQSPIVSMPDGDKVDLEAFSEFTKIITPAITRVVDFAKKLPMFSELPCEDQIILLKGCCMEIMSLRAAVRYDPESDTLTLSGEMAVKREQLKNGGLGVVSDAIFELGKSLSAFNLDDTEVALLQAVLLMSTDRSGLLCVDKIEKSQEAYLLAFEHYVNHRKHNIPHFWPKLLMKEREVQSSILYKGAAAEGRPGGSLGVHPEGQQLLGMHVVQGPQVRQLEQQLGEAGSLQGPVLQHQSPKSPQQRLLELLHRSGILHARAVCGEDDSSEADSPSSSEEEPEVCEDLAGNAASP
  
Inhibitor
Name:
BDBM426634
Synonyms:
US10544075, Compound JD-20
Type:
Small organic molecule
Emp. Form.:
C18H18Br2O4
Mol. Mass.:
458.141
SMILES:
CC(C)c1cc(Cc2c(Br)cc(OCC(O)=O)cc2Br)ccc1O
Structure:
Search PDB for entries with ligand similarity: