Compile Data Set for Download or QSAR
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Found 30 Enz. Inhib. hit(s) for PDB: 3GWS
TargetThyroid hormone receptor beta(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM18860((2R)-2-amino-3-[4-(4-hydroxy-3-iodophenoxy)-3,5-di...)
Affinity DataKi:  0.0800nMAssay Description:Inhibitory activity against [125I]-T3 binding to human TRbeta1 receptorMore data for this Ligand-Target Pair
TargetThyroid hormone receptor beta(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM18860((2R)-2-amino-3-[4-(4-hydroxy-3-iodophenoxy)-3,5-di...)
Affinity DataKi:  0.550nMAssay Description:Displacement of [125I]T3 from recombinant thyroid hormone receptor beta (unknown origin) expressed in sf9 cells by scintillation proximity assayMore data for this Ligand-Target Pair
TargetThyroid hormone receptor beta(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM18860((2R)-2-amino-3-[4-(4-hydroxy-3-iodophenoxy)-3,5-di...)
Affinity DataKi:  0.680nMAssay Description:Displacement of [125I]3,5,3'-triiodo-L-thyronine His-tagged human recombinant TRbeta1 by scintillation proximity assayMore data for this Ligand-Target Pair
TargetThyroid hormone receptor beta(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM18860((2R)-2-amino-3-[4-(4-hydroxy-3-iodophenoxy)-3,5-di...)
Affinity DataKi:  2.29nMAssay Description:Displacement of [125I]T3 from human recombinant thyroid harmone receptor beta after 16 to 48 hrs by gamma-ray detectionMore data for this Ligand-Target Pair
TargetThyroid hormone receptor beta(Homo sapiens (Human))
Pfizer

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 TRbeta expressed in insect cells after 16 to 48 hrs by gamma-countingMore data for this Ligand-Target Pair
TargetThyroid hormone receptor beta(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM18860((2R)-2-amino-3-[4-(4-hydroxy-3-iodophenoxy)-3,5-di...)
Affinity DataIC50:  0.257nMAssay Description:Inhibition of human thyroid hormone receptor beta 1More data for this Ligand-Target Pair
TargetThyroid hormone receptor beta(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM18860((2R)-2-amino-3-[4-(4-hydroxy-3-iodophenoxy)-3,5-di...)
Affinity DataIC50:  0.260nMAssay Description:IC50 is the concentration of each compound required to inhibit 50% binding of 125I-T3 to hTRbeta.More data for this Ligand-Target Pair
TargetThyroid hormone receptor beta(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM18860((2R)-2-amino-3-[4-(4-hydroxy-3-iodophenoxy)-3,5-di...)
Affinity DataIC50:  0.260nMpH: 7.0 T: 2°CAssay Description:IC50 is the concentration of each compound required to inhibit 50% binding of 125I-T3 to hTRbeta.More data for this Ligand-Target Pair
TargetThyroid hormone receptor beta(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM18860((2R)-2-amino-3-[4-(4-hydroxy-3-iodophenoxy)-3,5-di...)
Affinity DataIC50:  0.260nMpH: 7.0 T: 2°CAssay Description:IC50 is the concentration of each compound required to inhibit 50% binding of 125I-T3 to hTRbeta.More data for this Ligand-Target Pair
TargetThyroid hormone receptor beta(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM18860((2R)-2-amino-3-[4-(4-hydroxy-3-iodophenoxy)-3,5-di...)
Affinity DataIC50:  0.260nMpH: 7.0 T: 2°CAssay Description:IC50 is the concentration of each compound required to inhibit 50% binding of 125I-T3 to hTRbeta. EC50 is the concentration of compound required to r...More data for this Ligand-Target Pair
TargetThyroid hormone receptor beta(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM18860((2R)-2-amino-3-[4-(4-hydroxy-3-iodophenoxy)-3,5-di...)
Affinity DataIC50:  0.260nMAssay Description:Inhibitory concentration against cloned human thyroid hormone receptor beta 1More data for this Ligand-Target Pair
TargetThyroid hormone receptor beta(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM18860((2R)-2-amino-3-[4-(4-hydroxy-3-iodophenoxy)-3,5-di...)
Affinity DataIC50:  2.90nMAssay Description:Displacement of [125I]-Triiodothyronine from human recombinant TRbeta1 ligand binding domain after 2 to 3 hrs by beta countingMore data for this Ligand-Target Pair
TargetThyroid hormone receptor beta(RAT)
Ciba Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM18860((2R)-2-amino-3-[4-(4-hydroxy-3-iodophenoxy)-3,5-di...)
Affinity DataIC50:  4.40nMAssay Description:In vitro inhibition of the bound [125I]L-T3 rat liver nuclear L-triiodothyronine receptorMore data for this Ligand-Target Pair
TargetThyroid hormone receptor beta(RAT)
Ciba Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM18860((2R)-2-amino-3-[4-(4-hydroxy-3-iodophenoxy)-3,5-di...)
Affinity DataIC50:  500nMAssay Description:In vitro inhibition of bound [125I]L-T3 rat plasma membrane 3,5,3'' L-triiodothyronine receptorMore data for this Ligand-Target Pair
TargetThyroid hormone receptor beta(RAT)
Ciba Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM18860((2R)-2-amino-3-[4-(4-hydroxy-3-iodophenoxy)-3,5-di...)
Affinity DataIC50:  500nMAssay Description:In vitro inhibition of bound [125I]L-T3 rat plasma membrane 3,5,3'' L-triiodothyronine receptorMore data for this Ligand-Target Pair
TargetThyroid hormone receptor beta(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM18860((2R)-2-amino-3-[4-(4-hydroxy-3-iodophenoxy)-3,5-di...)
Affinity DataEC50:  1.49nMAssay 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 beta(Homo sapiens (Human))
Pfizer

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 beta(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM18860((2R)-2-amino-3-[4-(4-hydroxy-3-iodophenoxy)-3,5-di...)
Affinity DataKd:  0.0810nMAssay Description:Displacement of [125I]T3 from human TRbeta receptorMore data for this Ligand-Target Pair
TargetThyroid hormone receptor beta(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM18860((2R)-2-amino-3-[4-(4-hydroxy-3-iodophenoxy)-3,5-di...)
Affinity DataEC50:  11nMAssay Description:Effect on human TRbeta transactivation activity in U2OS cells by luciferase reporter assayMore data for this Ligand-Target Pair
TargetThyroid hormone receptor beta(Homo sapiens (Human))
Pfizer

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

Curated by ChEMBL
LigandPNGBDBM18860((2R)-2-amino-3-[4-(4-hydroxy-3-iodophenoxy)-3,5-di...)
Affinity DataEC50:  11nMAssay 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 beta(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM18860((2R)-2-amino-3-[4-(4-hydroxy-3-iodophenoxy)-3,5-di...)
Affinity DataEC50:  2nMAssay Description:Agonist activity at human recombinant TRbeta1 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 beta(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM18860((2R)-2-amino-3-[4-(4-hydroxy-3-iodophenoxy)-3,5-di...)
Affinity DataKd:  0.0810nMAssay 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 beta(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM18860((2R)-2-amino-3-[4-(4-hydroxy-3-iodophenoxy)-3,5-di...)
Affinity DataKd:  0.0810nMAssay 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 beta(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM18860((2R)-2-amino-3-[4-(4-hydroxy-3-iodophenoxy)-3,5-di...)
Affinity DataEC50:  15nMAssay Description:Agonist activity at recombinant His6-tagged THR-beta (unknown origin) expressed in Escherichia coli BL21(DE3) co-expressing RXR preincubated for 30 m...More data for this Ligand-Target Pair
TargetThyroid hormone receptor beta(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM18860((2R)-2-amino-3-[4-(4-hydroxy-3-iodophenoxy)-3,5-di...)
Affinity DataKd:  0.0870nMAssay Description:Binding affinity of compound was determined against thyroid hormone receptor beta 1More data for this Ligand-Target Pair
TargetThyroid hormone receptor beta(Homo sapiens (Human))
Pfizer

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 beta 1 (hTRbeta1)More data for this Ligand-Target Pair
TargetThyroid hormone receptor beta(Homo sapiens (Human))
Pfizer

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 beta 1 (hTRbeta1) using radiolabeled T3More data for this Ligand-Target Pair
TargetThyroid hormone receptor beta(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM18860((2R)-2-amino-3-[4-(4-hydroxy-3-iodophenoxy)-3,5-di...)
Affinity DataKd:  0.140nMAssay Description:Binding affinity of the compound towards thyroid hormone receptor (hTR beta 1)More data for this Ligand-Target Pair
TargetThyroid hormone receptor beta(Homo sapiens (Human))
Pfizer

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 TRbeta1 in E25B2 cells (agonistic activity)More data for this Ligand-Target Pair