Reaction Details Report a problem with these data
Target
Thyroid hormone receptor alpha [148-410]
Ligand
BDBM18839
Substrate
Peptide SRC2-2
Meas. Tech.
Fluorescence Polarization (FP) Competition Assay
IC50
21400±n/a nM
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 Chem 50:5269-5280 (2007) [PubMed]  Article 
Target
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:
EEMIRSLQQRPEPTPEEWDLIHIATEAHRSTNAQGSHWKQRRKFLPDDIGQSPIVSMPDGDKVDLEAFSEFTKIITPAITRVVDFAKKLPMFSELPCEDQIILLKGCCMEIMSLRAAVRYDPESDTLTLSGEMAVKREQLKNGGLGVVSDAIFELGKSLSAFNLDDTEVALLQAVLLMSTDRSGLLCVDKIEKSQEAYLLAFEHYVNHRKHNIPHFWPKLLMKEREVQSSILYKGAAAEGRPGGSLGVHPEGQQLLGMHVVQV
  
Inhibitor
Name:
BDBM18839
Synonyms:
4-octylphenyl prop-2-enoate | Substituted Acrylate, 6g
Type:
Small organic molecule
Emp. Form.:
C17H24O2
Mol. Mass.:
260.3713
SMILES:
CCCCCCCCc1ccc(OC(=O)C=C)cc1
Structure:
Search PDB for entries with ligand similarity:
Substrate
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