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Found 26 Enz. Inhib. hit(s) for PDB: 4LNW
TargetThyroid hormone receptor alpha(Homo sapiens (Human))
Metabasis Therapeutics

Curated by ChEMBL
LigandPNGBDBM18860((2R)-2-amino-3-[4-(4-hydroxy-3-iodophenoxy)-3,5-di...)
Affinity DataKi:  0.220nMAssay Description:Displacement of [125I]T3 from recombinant thyroid hormone receptor alpha (unknown origin) expressed in sf9 cells by scintillation proximity assayMore data for this Ligand-Target Pair
TargetThyroid hormone receptor alpha(Homo sapiens (Human))
Metabasis Therapeutics

Curated by ChEMBL
LigandPNGBDBM18860((2R)-2-amino-3-[4-(4-hydroxy-3-iodophenoxy)-3,5-di...)
Affinity DataKi:  0.330nMAssay Description:Displacement of [125I]3,5,3'-triiodo-L-thyronine from His-tagged human recombinant TRalpha1 by scintillation proximity assayMore data for this Ligand-Target Pair
TargetThyroid hormone receptor alpha(Homo sapiens (Human))
Metabasis Therapeutics

Curated by ChEMBL
LigandPNGBDBM18860((2R)-2-amino-3-[4-(4-hydroxy-3-iodophenoxy)-3,5-di...)
Affinity DataKi:  2.30nMAssay Description:Displacement of [125I]-T3 from human TRalpha expressed in insect cells after 16 to 48 hrs by gamma-countingMore data for this Ligand-Target Pair
TargetThyroid hormone receptor alpha(Homo sapiens (Human))
Metabasis Therapeutics

Curated by ChEMBL
LigandPNGBDBM18860((2R)-2-amino-3-[4-(4-hydroxy-3-iodophenoxy)-3,5-di...)
Affinity DataKi:  2.33nMAssay Description:Displacement of [125I]T3 from human recombinant thyroid harmone receptor alpha after 16 to 48 hrs by gamma-ray detectionMore data for this Ligand-Target Pair
TargetThyroid hormone receptor alpha(Homo sapiens (Human))
Metabasis Therapeutics

Curated by ChEMBL
LigandPNGBDBM18860((2R)-2-amino-3-[4-(4-hydroxy-3-iodophenoxy)-3,5-di...)
Affinity DataIC50:  0.240nMpH: 7.0 T: 2°CAssay Description:IC50 is the concentration of each compound required to inhibit 50% binding of 125I-T3 to hTRalpha. More data for this Ligand-Target Pair
TargetThyroid hormone receptor alpha(Homo sapiens (Human))
Metabasis Therapeutics

Curated by ChEMBL
LigandPNGBDBM18860((2R)-2-amino-3-[4-(4-hydroxy-3-iodophenoxy)-3,5-di...)
Affinity DataIC50:  0.240nMpH: 7.0 T: 2°CAssay Description:IC50 is the concentration of each compound required to inhibit 50% binding of 125I-T3 to hTRalpha. More data for this Ligand-Target Pair
TargetThyroid hormone receptor alpha(Homo sapiens (Human))
Metabasis Therapeutics

Curated by ChEMBL
LigandPNGBDBM18860((2R)-2-amino-3-[4-(4-hydroxy-3-iodophenoxy)-3,5-di...)
Affinity DataIC50:  0.240nMpH: 7.0 T: 2°CAssay Description:IC50 is the concentration of each compound required to inhibit 50% binding of 125I-T3 to hTRalpha. More data for this Ligand-Target Pair
TargetThyroid hormone receptor alpha(Homo sapiens (Human))
Metabasis Therapeutics

Curated by ChEMBL
LigandPNGBDBM18860((2R)-2-amino-3-[4-(4-hydroxy-3-iodophenoxy)-3,5-di...)
Affinity DataIC50:  0.240nMpH: 7.0 T: 2°CAssay Description:IC50 is the concentration of each compound required to inhibit 50% binding of 125I-T3 to hTRalpha. EC50 is the concentration of compound required to ...More data for this Ligand-Target Pair
TargetThyroid hormone receptor alpha(Homo sapiens (Human))
Metabasis Therapeutics

Curated by ChEMBL
LigandPNGBDBM18860((2R)-2-amino-3-[4-(4-hydroxy-3-iodophenoxy)-3,5-di...)
Affinity DataIC50:  0.240nMAssay Description:Inhibitory concentration against cloned human thyroid hormone receptor alpha 1More data for this Ligand-Target Pair
TargetThyroid hormone receptor alpha(Homo sapiens (Human))
Metabasis Therapeutics

Curated by ChEMBL
LigandPNGBDBM18860((2R)-2-amino-3-[4-(4-hydroxy-3-iodophenoxy)-3,5-di...)
Affinity DataIC50:  3.20nMAssay Description:Displacement of [125I]-Triiodothyronine from human recombinant TRalpha1 ligand binding domain after 2 to 3 hrs by beta countingMore data for this Ligand-Target Pair
TargetThyroid hormone receptor alpha(Homo sapiens (Human))
Metabasis Therapeutics

Curated by ChEMBL
LigandPNGBDBM18860((2R)-2-amino-3-[4-(4-hydroxy-3-iodophenoxy)-3,5-di...)
Affinity DataEC50:  2.40nMAssay Description:TRE-driven dual-luciferase reporter assay in human uterine cervical cancer (Hela) cell lineMore data for this Ligand-Target Pair
TargetThyroid hormone receptor alpha(Homo sapiens (Human))
Metabasis Therapeutics

Curated by ChEMBL
LigandPNGBDBM18860((2R)-2-amino-3-[4-(4-hydroxy-3-iodophenoxy)-3,5-di...)
Affinity DataKd:  0.100nMAssay Description:Binding affinity against human Thyroid hormone receptor alpha1 (hTRalpha1) using radiolabeled T3More data for this Ligand-Target Pair
TargetThyroid hormone receptor alpha(Homo sapiens (Human))
Metabasis Therapeutics

Curated by ChEMBL
LigandPNGBDBM18860((2R)-2-amino-3-[4-(4-hydroxy-3-iodophenoxy)-3,5-di...)
Affinity DataEC50:  2nMAssay Description:Half-maximum activation of human Thyroid hormone receptor alpha1 (hTRalpha1)More data for this Ligand-Target Pair
TargetThyroid hormone receptor alpha(Homo sapiens (Human))
Metabasis Therapeutics

Curated by ChEMBL
LigandPNGBDBM18860((2R)-2-amino-3-[4-(4-hydroxy-3-iodophenoxy)-3,5-di...)
Affinity DataKd:  0.0600nMAssay Description:Binding affinity of compound was determined against Thyroid hormone receptor alpha1More data for this Ligand-Target Pair
TargetThyroid hormone receptor alpha(Homo sapiens (Human))
Metabasis Therapeutics

Curated by ChEMBL
LigandPNGBDBM18860((2R)-2-amino-3-[4-(4-hydroxy-3-iodophenoxy)-3,5-di...)
Affinity DataEC50:  0.410nMAssay Description:Agonist activity at human thyroid hormone receptor alpha expressed in HEK293 cells by luciferase reporter gene assayMore data for this Ligand-Target Pair
TargetThyroid hormone receptor alpha(Homo sapiens (Human))
Metabasis Therapeutics

Curated by ChEMBL
LigandPNGBDBM18860((2R)-2-amino-3-[4-(4-hydroxy-3-iodophenoxy)-3,5-di...)
Affinity DataEC50:  1.01nMAssay Description:Human epithelial kidney cells (HEK 293) were grown to 80% confluency in Dubelcco's modified Eagles 4.5 g/L glucose medium (high glucose DMEM) con...More data for this Ligand-Target Pair
TargetThyroid hormone receptor alpha(Homo sapiens (Human))
Metabasis Therapeutics

Curated by ChEMBL
LigandPNGBDBM18860((2R)-2-amino-3-[4-(4-hydroxy-3-iodophenoxy)-3,5-di...)
Affinity DataEC50:  2.40nMAssay Description:TRE-driven dual-luciferase reporter assay in human bone osteosarcoma epithelial (U2OS) cell line.More data for this Ligand-Target Pair
TargetThyroid hormone receptor alpha(Homo sapiens (Human))
Metabasis Therapeutics

Curated by ChEMBL
LigandPNGBDBM18860((2R)-2-amino-3-[4-(4-hydroxy-3-iodophenoxy)-3,5-di...)
Affinity DataKd:  0.0580nMAssay Description:Thyroid hormone competitive binding assay using TNT T7 quick-coupled transcription translation system from promega.More data for this Ligand-Target Pair
TargetThyroid hormone receptor alpha(Homo sapiens (Human))
Metabasis Therapeutics

Curated by ChEMBL
LigandPNGBDBM18860((2R)-2-amino-3-[4-(4-hydroxy-3-iodophenoxy)-3,5-di...)
Affinity DataKd:  0.0580nMAssay Description:Displacement of [125I]T3 from human TRalpha receptorMore data for this Ligand-Target Pair
TargetThyroid hormone receptor alpha(Homo sapiens (Human))
Metabasis Therapeutics

Curated by ChEMBL
LigandPNGBDBM18860((2R)-2-amino-3-[4-(4-hydroxy-3-iodophenoxy)-3,5-di...)
Affinity DataEC50:  2.40nMAssay Description:Effect on human TRalpha transactivation activity in HeLa cells by luciferase reporter assayMore data for this Ligand-Target Pair
TargetThyroid hormone receptor alpha(Homo sapiens (Human))
Metabasis Therapeutics

Curated by ChEMBL
LigandPNGBDBM18860((2R)-2-amino-3-[4-(4-hydroxy-3-iodophenoxy)-3,5-di...)
Affinity DataEC50:  2.40nMAssay Description:Effect on human TRalpha transactivation activity in U2OS cells by luciferase reporter assayMore data for this Ligand-Target Pair
TargetThyroid hormone receptor alpha(Homo sapiens (Human))
Metabasis Therapeutics

Curated by ChEMBL
LigandPNGBDBM18860((2R)-2-amino-3-[4-(4-hydroxy-3-iodophenoxy)-3,5-di...)
Affinity DataKd:  0.0580nMAssay Description:Human thyroid hormone receptor alpha and beta (hTR alpha1) and (hTR beta1) were produced using TNT coupled reticulocyte lysate system from Promega.More data for this Ligand-Target Pair
TargetThyroid hormone receptor alpha(Homo sapiens (Human))
Metabasis Therapeutics

Curated by ChEMBL
LigandPNGBDBM18860((2R)-2-amino-3-[4-(4-hydroxy-3-iodophenoxy)-3,5-di...)
Affinity DataEC50:  2.10nMAssay Description:Agonist activity at human recombinant TRalpha1 transfected in CV-1 cells after 8 to 10 hrs by alkaline phosphatase reporter gene assayMore data for this Ligand-Target Pair
TargetThyroid hormone receptor alpha(Homo sapiens (Human))
Metabasis Therapeutics

Curated by ChEMBL
LigandPNGBDBM18860((2R)-2-amino-3-[4-(4-hydroxy-3-iodophenoxy)-3,5-di...)
Affinity DataEC50:  10nMAssay Description:Agonist activity at recombinant His6-tagged THR-alpha (unknown origin) expressed in Escherichia coli BL21(DE3) co-expressing RXR preincubated for 30 ...More data for this Ligand-Target Pair
TargetThyroid hormone receptor alpha(Homo sapiens (Human))
Metabasis Therapeutics

Curated by ChEMBL
LigandPNGBDBM18860((2R)-2-amino-3-[4-(4-hydroxy-3-iodophenoxy)-3,5-di...)
Affinity DataKd:  0.170nMAssay Description:Binding affinity of the compound towards thyroid hormone receptor (hTR alpha 1)More data for this Ligand-Target Pair
TargetThyroid hormone receptor alpha(Homo sapiens (Human))
Metabasis Therapeutics

Curated by ChEMBL
LigandPNGBDBM18860((2R)-2-amino-3-[4-(4-hydroxy-3-iodophenoxy)-3,5-di...)
Affinity DataEC50:  2nMAssay Description:Effective concentration of the compound binding towards TRalpha in E25B2 cells (agonistic activity)More data for this Ligand-Target Pair