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Target
Thyroid hormone receptor alpha
Ligand
BDBM18883
Substrate
BDBM18860
Meas. Tech.
TRalpha-Binding Assay.
pH
7±n/a
Temperature
277.15±n/a K
IC50
1600±n/a nM
Citation
 Koehler, K; Gordon, S; Brandt, P; Carlsson, B; Bäcksbro-Saeidi, A; Apelqvist, T; Agback, P; Grover, GJ; Nelson, W; Grynfarb, M; Färnegård, M; Rehnmark, S; Malm, J Thyroid receptor ligands. 6. A high affinity "direct antagonist" selective for the thyroid hormone receptor. J Med Chem 49:6635-7 (2006) [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:
BDBM18883
Synonyms:
3,5-dibromo-4-[4-hydroxy-3,5-bis(propan-2-yl)phenoxy]benzoic acid | JMC496635 Compound 3 | thyromimetic, 4
Type:
Small organic molecule
Emp. Form.:
C19H20Br2O4
Mol. Mass.:
472.168
SMILES:
CC(C)c1cc(Oc2c(Br)cc(cc2Br)C(O)=O)cc(C(C)C)c1O
Structure:
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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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