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TargetThyroid hormone receptor alpha [148-410]
LigandBDBM18827
Substrate/CompetitorPeptide SRC2-2
Meas. Tech.Fluorescence Polarization (FP) Competition Assay
pH7.2±n/a
Temperature295.15±n/a K
IC50 18900±2500 nM
CommentsViability (LD50) of ARO and U2OS cells in the presence of compound are 1.4 uM and 11.6 uM, respectively. The compound solubility in PBS buffer containing 5% DMSO is 41 uM. Permeability across an artificial membrane (PAMPA) of the compound is 7 x 10-6 cm/s.
Citation Arnold, LA; Kosinski, A; Estebanez-Perpina, E; Fletterick, RJ; Guy, RK Inhibitors of the Interaction of a Thyroid Hormone Receptor and Coactivators: Preliminary Structure-Activity Relationships. J Med Chem50:5269-5280 (2007) [PubMed]  Article
More Info.:Get all data from this article,   Solution Info,  Assay Method
 
Thyroid hormone receptor alpha [148-410]
Name:Thyroid hormone receptor alpha [148-410]
Synonyms:C-erbA-alpha | EAR-7 | EAR7 | ERBA1 | NR1A1 | THA_HUMAN | THRA | THRA1 | THRA2 | Thyroid Hormone Receptor (TR-alpha) | Thyroid hormone receptor alpha | c-erbA-1
Type:Ligand-Binding Domain
Mol. Mass.:29441.97
Organism:Homo sapiens (Human)
Description:The hTRalpha LBD (His6 residues E148 - V410) was cloned and expressed in E. coli.
Residue:263
Sequence:
EEMIRSLQQRPEPTPEEWDLIHIATEAHRSTNAQGSHWKQRRKFLPDDIGQSPIVSMPDG
DKVDLEAFSEFTKIITPAITRVVDFAKKLPMFSELPCEDQIILLKGCCMEIMSLRAAVRY
DPESDTLTLSGEMAVKREQLKNGGLGVVSDAIFELGKSLSAFNLDDTEVALLQAVLLMST
DRSGLLCVDKIEKSQEAYLLAFEHYVNHRKHNIPHFWPKLLMKEREVQSSILYKGAAAEG
RPGGSLGVHPEGQQLLGMHVVQV
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM18827
Peptide SRC2-2
Name:Peptide SRC2-2
Synonyms:n/a
Type:Peptide
Mol. Mass.:2334.76
Organism:n/a
Description:The peptide is labeled with 5-iodoacetamidofluorescien.
Residue:20
Sequence:
CLKEKHKILHRLLQDSSSPV