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Target
Thyroid hormone receptor alpha
Ligand
BDBM50610163
Substrate
n/a
Meas. Tech.
ChEMBL_2280285
IC50
>5000±n/a nM
Citation
 Orsi, DL; Ferrara, SJ; Siegel, S; Friberg, A; Bouché, L; Pook, E; Lienau, P; Bluck, JP; Lemke, CT; Akcay, G; Stellfeld, T; Meyer, H; Pütter, V; Holton, SJ; Korr, D; Jerchel-Furau, I; Pantelidou, C; Strathdee, CA; Meyerson, M; Eis, K; Goldstein, JT Discovery and characterization of orally bioavailable 4-chloro-6-fluoroisophthalamides as covalent PPARG inverse-agonists. Bioorg Med Chem 78:0 (2023) [PubMed]
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:
BDBM50610163
Synonyms:
CHEMBL5267263
Type:
Small organic molecule
Emp. Form.:
C23H17ClF4N2O3
Mol. Mass.:
480.839
SMILES:
Cc1cc(OC(F)F)ccc1NC(=O)c1cc(C(=O)NCc2ccc(F)cc2)c(F)cc1Cl
Structure:
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