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Target
Thyroid hormone receptor alpha
Ligand
BDBM18887
Substrate
BDBM18860
Meas. Tech.
TRalpha-Binding Assay.
pH
7±n/a
Temperature
277.15±n/a K
IC50
460±n/a nM
Citation
 Malm, J; Gordon, S; Brandt, P; Carlsson, B; Agback, P; Bäckbro Saeidi, A; Sandberg, J Thyroid receptor ligands. Part 7: Indirect antagonists of the thyroid hormone receptor with improved affinity. Bioorg Med Chem Lett 17:2018-21 (2007) [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:
BDBM18887
Synonyms:
3,5-Dibromo-4-alkoxyphenylalkanoic Acid, 9k | 3-[3,5-dibromo-4-(cyclohexylmethoxy)phenyl]propanoic acid | JMC496635 Compound 9 | cyclohexyl derivative, 7
Type:
Small organic molecule
Emp. Form.:
C16H20Br2O3
Mol. Mass.:
420.136
SMILES:
OC(=O)CCc1cc(Br)c(OCC2CCCCC2)c(Br)c1
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
BDBM18860
Synonyms:
(2R)-2-amino-3-[4-(4-hydroxy-3-iodophenoxy)-3,5-diiodophenyl]propanoic acid | (2S)-2-amino-3-[4-(4-hydroxy-3-iodophenoxy)-3,5-diiodophenyl]propanoic acid | 3,5,3'-triiodo-L-thyronine (T3) | CHEMBL1544 | Triiodothyronine | Triiodothyronine (T3) | US10544075, Compound T3 | [125I]T3 | liothyronine | triothyrone
Type:
Hormone
Emp. Form.:
C15H12I3NO4
Mol. Mass.:
650.9735
SMILES:
N[C@@H](Cc1cc(I)c(Oc2ccc(O)c(I)c2)c(I)c1)C(O)=O |r|
Structure:
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