Reaction Details Report a problem with these data
Target
Thyroid hormone receptor alpha
Ligand
BDBM50301375
Substrate
n/a
Meas. Tech.
ChEMBL_1995725 (CHEMBL4629620)
EC50
19±n/a nM
Citation
Gellrich, L; Heitel, P; Heering, J; Kilu, W; Pollinger, J; Goebel, T; Kahnt, A; Arifi, S; Pogoda, W; Paulke, A; Steinhilber, D; Proschak, E; Wurglics, M; Schubert-Zsilavecz, M; Chaikuad, A; Knapp, S; Bischoff, I; Fürst, R; Merk, D l-Thyroxin and the Nonclassical Thyroid Hormone TETRAC Are Potent Activators of PPAR?. J Med Chem 63:6727-6740 (2020) [PubMed] Article
More Info.:
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:
BDBM50301375
Synonyms:
3,3',5,5'-tetraiodo-L-thyronine | 3,5,3',5'-tetraiodo-L-thyronine | 4-(4-hydroxy-3,5-diiodophenoxy)-3,5-diiodo-L-phenylalanine | CHEMBL1624 | L-T4 | L-thyroxine | O-(4-hydroxy-3,5-diiodophenyl)-3,5-diiodo-L-tyrosine | levothyroxine
Type:
Small organic molecule
Emp. Form.:
C15H11I4NO4
Mol. Mass.:
776.87
SMILES:
N[C@@H](Cc1cc(I)c(Oc2cc(I)c(O)c(I)c2)c(I)c1)C(O)=O |r|