Target
Thyroid hormone receptor alpha
Ligand
BDBM398043
Substrate
n/a
Meas. Tech.
ChEMBL_1995725 (CHEMBL4629620)
EC50
20±n/a nM
Citation
 Gellrich, LHeitel, PHeering, JKilu, WPollinger, JGoebel, TKahnt, AArifi, SPogoda, WPaulke, ASteinhilber, DProschak, EWurglics, MSchubert-Zsilavecz, MChaikuad, AKnapp, SBischoff, IFürst, RMerk, D l-Thyroxin and the Nonclassical Thyroid Hormone TETRAC Are Potent Activators of PPAR?. J Med Chem 63:6727-6740 (2020) [PubMed]  Article 
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:
BDBM398043
Synonyms:
US10322118, Entry 1
Type:
Small organic molecule
Emp. Form.:
C14H8I4O4
Mol. Mass.:
747.8288
SMILES:
OC(=O)Cc1cc(I)c(Oc2cc(I)c(O)c(I)c2)c(I)c1
Structure:
Search PDB for entries with ligand similarity: