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TargetThyroid hormone receptor alpha
LigandBDBM50123052
Substrate/Competitorn/a
Meas. Tech.ChEBML_210487
EC50 1500±n/a nM
Citation Dow, RLSchneider, SRPaight, ESHank, RFChiang, PCornelius, PLee, ENewsome, WPSwick, AGSpitzer, JHargrove, DMPatterson, TAPandit, JChrunyk, BALeMotte, PKDanley, DERosner, MHAmmirati, MJSimons, SPSchulte, GKTate, BFDaSilva-Jardine, P Discovery of a novel series of 6-azauracil-based thyroid hormone receptor ligands: potent, TR beta subtype-selective thyromimetics. Bioorg Med Chem Lett13:379-82 (2003) [PubMed]
More Info.:Get all data from this article,  Assay Method
 
Thyroid hormone receptor alpha
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
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM50123052
n/a
NameBDBM50123052
Synonyms:2-[4-(3-{8-azaspiro[bicyclo[3.2.1]octane-3,2'-oxolane]-8-ylsulfonyl}-4-hydroxyphenoxy)-3,5-dichlorophenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-3,5-dione | 2-{3,5-dichloro-4-[4-hydroxy-3-spiro[8-azabicyclo[3.2.1]octane-3,2'-(tetrahydrofuran)]-8-ylsulfonylphenoxy]phenyl}-2,3,4,5-tetrahydro-1,2,4-triazine-3,5-dione | CHEMBL125946
TypeSmall organic molecule
Emp. Form.C25H24Cl2N4O7S
Mol. Mass.595.452
SMILESOc1ccc(Oc2c(Cl)cc(cc2Cl)-n2ncc(=O)[nH]c2=O)cc1S(=O)(=O)N1C2CCC1CC1(CCCO1)C2 |TLB:34:33:27:29.30,THB:24:27:33.38.32:29.30,37:33:27:29.30|
Structure
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