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Target
Thyroid hormone receptor alpha
Ligand
BDBM18627
Substrate
n/a
Meas. Tech.
ChEMBL_302715 (CHEMBL839586)
Ki
>1250±n/a nM
Citation
 von Geldern, TW; Tu, N; Kym, PR; Link, JT; Jae, HS; Lai, C; Apelqvist, T; Rhonnstad, P; Hagberg, L; Koehler, K; Grynfarb, M; Goos-Nilsson, A; Sandberg, J; Osterlund, M; Barkhem, T; Höglund, M; Wang, J; Fung, S; Wilcox, D; Nguyen, P; Jakob, C; Hutchins, C; Färnegårdh, M; Kauppi, B; Ohman, L; Jacobson, PB Liver-selective glucocorticoid antagonists: a novel treatment for type 2 diabetes. J Med Chem 47:4213-30 (2004) [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:
BDBM18627
Synonyms:
(10S,11S,14S,15S,17R)-17-[4-(dimethylamino)phenyl]-14-hydroxy-15-methyl-14-(prop-1-yn-1-yl)tetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadeca-1,6-dien-5-one | Mifeprex | Mifepristone | RU-486 | RU486 (tetramethyl-rhodamine conjugated)
Type:
Small organic molecule
Emp. Form.:
C29H35NO2
Mol. Mass.:
429.5937
SMILES:
[H][C@@]12CC[C@@](O)(C#CC)[C@@]1(C)C[C@@H](C1=C3CCC(=O)C=C3CC[C@@]21[H])c1ccc(cc1)N(C)C |r,c:14,20|
Structure:
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