Reaction Details |
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Target | Thyroid hormone receptor alpha |
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Ligand | BDBM50063750 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1463693 (CHEMBL3399152) |
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Ki | 47±n/a nM |
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Citation | Burkholder, TP; Cunningham, BE; Clayton, JR; Lander, PA; Brown, ML; Doti, RA; Durst, GL; Montrose-Rafizadeh, C; King, C; Osborne, HE; Amos, RM; Zink, RW; Stramm, LE; Burris, TP; Cardona, G; Konkol, DL; Reidy, C; Christe, ME; Genin, MJ Design and synthesis of a novel series of [1-(4-hydroxy-benzyl)-1H-indol-5-yloxy]-acetic acid compounds as potent, selective, thyroid hormone receptorß agonists. Bioorg Med Chem Lett25:1377-80 (2015) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Thyroid hormone receptor alpha |
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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: | MEQKPSKVECGSDPEENSARSPDGKRKRKNGQCSLKTSMSGYIPSYLDKDEQCVVCGDKA
TGYHYRCITCEGCKGFFRRTIQKNLHPTYSCKYDSCCVIDKITRNQCQLCRFKKCIAVGM
AMDLVLDDSKRVAKRKLIEQNRERRRKEEMIRSLQQRPEPTPEEWDLIHIATEAHRSTNA
QGSHWKQRRKFLPDDIGQSPIVSMPDGDKVDLEAFSEFTKIITPAITRVVDFAKKLPMFS
ELPCEDQIILLKGCCMEIMSLRAAVRYDPESDTLTLSGEMAVKREQLKNGGLGVVSDAIF
ELGKSLSAFNLDDTEVALLQAVLLMSTDRSGLLCVDKIEKSQEAYLLAFEHYVNHRKHNI
PHFWPKLLMKEREVQSSILYKGAAAEGRPGGSLGVHPEGQQLLGMHVVQGPQVRQLEQQL
GEAGSLQGPVLQHQSPKSPQQRLLELLHRSGILHARAVCGEDDSSEADSPSSSEEEPEVC
EDLAGNAASP
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BDBM50063750 |
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n/a |
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Name | BDBM50063750 |
Synonyms: | CHEMBL3397345 |
Type | Small organic molecule |
Emp. Form. | C25H29NO4 |
Mol. Mass. | 407.5021 |
SMILES | Cc1cn(Cc2ccc(O)c(CC3CCCCC3)c2)c2ccc(OCC(O)=O)cc12 |
Structure |
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