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TargetThyroid hormone receptor alpha
LigandBDBM18867
Substrate/CompetitorBDBM18860
Meas. Tech.TRalpha-Binding Assay and Thyroid Response Element (TRAFalpha1) Reporter Assay.
pH7±n/a
Temperature277.15±n/a K
IC50 1.4±0.44 nM
EC50 0.38±n/a nM
Citation Garg, NLi, YLGarcia Collazo, AMLitten, CRyono, DEZhang, MCaringal, YBrigance, RPMeng, WWashburn, WNAgback, PMellström, KRehnmark, SRahimi-Ghadim, MNorin, TGrynfarb, MSandberg, JGrover, GMalm, J Thyroid receptor ligands. Part 8: Thyromimetics derived from N-acylated-alpha-amino acid derivatives displaying modulated pharmacological selectivity compared with KB-141. Bioorg Med Chem Lett17:4131-4 (2007) [PubMed]  Article
More Info.:Get all data from this article,   Solution Info,  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
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BDBM18867
BDBM18860
NameBDBM18867
Synonyms:2-{3,5-dibromo-4-[4-hydroxy-3-(propan-2-yl)phenoxy]phenyl}acetic acid | KB-131092 | dibromo phenylacetic acid, 11a
TypeSmall organic molecule
Emp. Form.C17H16Br2O4
Mol. Mass.444.115
SMILESCC(C)c1cc(Oc2c(Br)cc(CC(O)=O)cc2Br)ccc1O
Structure
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