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Found 48 Enz. Inhib. hit(s) for PDB: 1ERR
TargetEstrogen receptor(Homo sapiens (Human))
University Of California

Curated by ChEMBL
LigandPNGBDBM19441(2-(4-hydroxyphenyl)-3-({4-[2-(piperidin-1-yl)ethox...)
Affinity DataKi:  0.0300nMAssay Description:Antagonistic activity against estrogen receptor alpha in presence of 0.1 nM estradiolMore data for this Ligand-Target Pair
TargetEstrogen receptor(Homo sapiens (Human))
University Of California

Curated by ChEMBL
LigandPNGBDBM19441(2-(4-hydroxyphenyl)-3-({4-[2-(piperidin-1-yl)ethox...)
Affinity DataKi:  0.220nMAssay Description:Ability to displace [3H]-17-beta-estradiol from Estrogen receptor alpha by scintillation proximity assay.More data for this Ligand-Target Pair
TargetEstrogen receptor(Homo sapiens (Human))
University Of California

Curated by ChEMBL
LigandPNGBDBM19441(2-(4-hydroxyphenyl)-3-({4-[2-(piperidin-1-yl)ethox...)
Affinity DataKi:  0.370nMAssay Description:Displacement of [3H]estradiol from ERalpha after 4 hrs by scintillation countingMore data for this Ligand-Target Pair
TargetEstrogen receptor(Homo sapiens (Human))
University Of California

Curated by ChEMBL
LigandPNGBDBM19441(2-(4-hydroxyphenyl)-3-({4-[2-(piperidin-1-yl)ethox...)
Affinity DataKi:  0.370nM ΔG°:  -53.3kJ/mole EC50:  4.32nMpH: 7.5 T: 2°CAssay Description:The binding affinities were determined by a competitive radiometric binding assay using [3H]estradiol as tracer. The Kd for 3H-estradiol was determin...More data for this Ligand-Target Pair
TargetEstrogen receptor(Homo sapiens (Human))
University Of California

Curated by ChEMBL
LigandPNGBDBM19441(2-(4-hydroxyphenyl)-3-({4-[2-(piperidin-1-yl)ethox...)
Affinity DataKi:  0.380nMAssay Description:Binding affinity to ERalpha ligand binding domainMore data for this Ligand-Target Pair
TargetEstrogen receptor(Homo sapiens (Human))
University Of California

Curated by ChEMBL
LigandPNGBDBM19441(2-(4-hydroxyphenyl)-3-({4-[2-(piperidin-1-yl)ethox...)
Affinity DataKi:  0.400nMAssay Description:Binding affinity for estrogen receptor alphaMore data for this Ligand-Target Pair
TargetEstrogen receptor(Homo sapiens (Human))
University Of California

Curated by ChEMBL
LigandPNGBDBM19441(2-(4-hydroxyphenyl)-3-({4-[2-(piperidin-1-yl)ethox...)
Affinity DataKi:  0.430nMAssay Description:Binding affinity to ERalpha (unknown origin)More data for this Ligand-Target Pair
TargetEstrogen receptor(Homo sapiens (Human))
University Of California

Curated by ChEMBL
LigandPNGBDBM19441(2-(4-hydroxyphenyl)-3-({4-[2-(piperidin-1-yl)ethox...)
Affinity DataKi:  2nMAssay Description:Displacement of [3H]estradiol from full length biotinylated human ERalpha by scintillation proximity assayMore data for this Ligand-Target Pair
TargetEstrogen receptor beta(Homo sapiens (Human))TBA
LigandPNGBDBM19441(2-(4-hydroxyphenyl)-3-({4-[2-(piperidin-1-yl)ethox...)
Affinity DataIC50:  0.200nMAssay Description:Antagonist effect in breast tissue was assayed by inhibition of estrogen stimulated MCF-7 cell proliferationMore data for this Ligand-Target Pair
In DepthDetails PDB3D3D Structure (crystal)
TargetEstrogen receptor beta(Homo sapiens (Human))TBA
LigandPNGBDBM19441(2-(4-hydroxyphenyl)-3-({4-[2-(piperidin-1-yl)ethox...)
Affinity DataIC50:  0.200nMAssay Description:Inhibition of estradiol-stimulated MCF-7 breast adenocarcinoma cell proliferationMore data for this Ligand-Target Pair
TargetEstrogen receptor beta(Homo sapiens (Human))TBA
LigandPNGBDBM19441(2-(4-hydroxyphenyl)-3-({4-[2-(piperidin-1-yl)ethox...)
Affinity DataIC50:  0.200nMAssay Description:In vitro inhibition of estrogen-stimulated MCF-7 cell proliferationMore data for this Ligand-Target Pair
TargetEstrogen receptor beta(Homo sapiens (Human))TBA
LigandPNGBDBM19441(2-(4-hydroxyphenyl)-3-({4-[2-(piperidin-1-yl)ethox...)
Affinity DataIC50:  0.200nMAssay Description:Antagonism of estrogen action in a mammary tumor cell line was assayed via inhibition of MCF-7 cell proliferation stimulated by 10 e-11 M 17-beta-est...More data for this Ligand-Target Pair
TargetEstrogen receptor(Homo sapiens (Human))
University Of California

Curated by ChEMBL
LigandPNGBDBM19441(2-(4-hydroxyphenyl)-3-({4-[2-(piperidin-1-yl)ethox...)
Affinity DataIC50:  0.300nMAssay Description:Antagonist activity at human wild type ERalpha expressed in HEK293T cells co-expressing ERE assessed as inhibition of estradiol-induced transactivati...More data for this Ligand-Target Pair
TargetEstrogen receptor beta(Homo sapiens (Human))TBA
LigandPNGBDBM19441(2-(4-hydroxyphenyl)-3-({4-[2-(piperidin-1-yl)ethox...)
Affinity DataIC50:  0.340nMAssay Description:Inhibition of 17-beta-estradiol (10e-11 M) mediated MCF-7 cell proliferationMore data for this Ligand-Target Pair
TargetEstrogen receptor(Homo sapiens (Human))
University Of California

Curated by ChEMBL
LigandPNGBDBM19441(2-(4-hydroxyphenyl)-3-({4-[2-(piperidin-1-yl)ethox...)
Affinity DataIC50:  0.460nMAssay Description:Antagonist activity at human ERalpha expressed in african green monkey CV1 cells assessed as inhibition of estrogen like activity after 24 hrs by luc...More data for this Ligand-Target Pair
TargetEstrogen receptor(Homo sapiens (Human))
University Of California

Curated by ChEMBL
LigandPNGBDBM19441(2-(4-hydroxyphenyl)-3-({4-[2-(piperidin-1-yl)ethox...)
Affinity DataIC50:  0.470nMAssay Description:Displacement of Fluormone ES2 from human recombinant full length untagged-ERalpha by fluorescence polarization competition binding assayMore data for this Ligand-Target Pair
TargetEstrogen receptor(RAT)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM19441(2-(4-hydroxyphenyl)-3-({4-[2-(piperidin-1-yl)ethox...)
Affinity DataIC50:  0.700nMAssay Description:Binding affinity for Rat Estrogen receptor-alphaMore data for this Ligand-Target Pair
TargetEstrogen receptor(Homo sapiens (Human))
University Of California

Curated by ChEMBL
LigandPNGBDBM19441(2-(4-hydroxyphenyl)-3-({4-[2-(piperidin-1-yl)ethox...)
Affinity DataIC50:  0.700nMAssay Description:In vitro inhibition of transcriptional activation induced by 1 nM 17-beta estradiol in T47D cells expressing estrogen receptor alphaMore data for this Ligand-Target Pair
TargetEstrogen receptor(Homo sapiens (Human))
University Of California

Curated by ChEMBL
LigandPNGBDBM19441(2-(4-hydroxyphenyl)-3-({4-[2-(piperidin-1-yl)ethox...)
Affinity DataIC50:  0.720nMAssay Description:Antagonist effect on transcriptional activation in MCF-7 cells expressing estrogen receptor alphaMore data for this Ligand-Target Pair
TargetEstrogen receptor(Homo sapiens (Human))
University Of California

Curated by ChEMBL
LigandPNGBDBM19441(2-(4-hydroxyphenyl)-3-({4-[2-(piperidin-1-yl)ethox...)
Affinity DataIC50:  0.720nMAssay Description:In vitro antagonist effect on estrogen receptor alpha transcriptional activation in MCF-7 cells against 10 pM 17-beta-estradiolMore data for this Ligand-Target Pair
TargetEstrogen receptor(Homo sapiens (Human))
University Of California

Curated by ChEMBL
LigandPNGBDBM19441(2-(4-hydroxyphenyl)-3-({4-[2-(piperidin-1-yl)ethox...)
Affinity DataIC50:  0.730nMAssay Description:Inhibition of estrogen receptor alphaMore data for this Ligand-Target Pair
TargetEstrogen receptor(Homo sapiens (Human))
University Of California

Curated by ChEMBL
LigandPNGBDBM19441(2-(4-hydroxyphenyl)-3-({4-[2-(piperidin-1-yl)ethox...)
Affinity DataIC50:  0.890nMAssay Description:Inhibitino of [3H]-17-beta-estradiol binding to human estrogen receptor alphaMore data for this Ligand-Target Pair
TargetEstrogen receptor(Homo sapiens (Human))
University Of California

Curated by ChEMBL
LigandPNGBDBM19441(2-(4-hydroxyphenyl)-3-({4-[2-(piperidin-1-yl)ethox...)
Affinity DataIC50:  1.80nMAssay Description:Inhibition of bindign to recombinant human estrogen receptor alphaMore data for this Ligand-Target Pair
TargetEstrogen receptor(Homo sapiens (Human))
University Of California

Curated by ChEMBL
LigandPNGBDBM19441(2-(4-hydroxyphenyl)-3-({4-[2-(piperidin-1-yl)ethox...)
Affinity DataIC50:  1.80nMAssay Description:Displacement of [3H]-17-beta-estradiol from full length human estrogen receptor alphaMore data for this Ligand-Target Pair
TargetEstrogen receptor(Homo sapiens (Human))
University Of California

Curated by ChEMBL
LigandPNGBDBM19441(2-(4-hydroxyphenyl)-3-({4-[2-(piperidin-1-yl)ethox...)
Affinity DataIC50:  1.80nMAssay Description:Binding affinity for Human Estrogen receptor-alphaMore data for this Ligand-Target Pair
TargetEstrogen receptor(Homo sapiens (Human))
University Of California

Curated by ChEMBL
LigandPNGBDBM19441(2-(4-hydroxyphenyl)-3-({4-[2-(piperidin-1-yl)ethox...)
Affinity DataIC50:  1.80nMAssay Description:Displacement of radiolabeled estrogen from estrogen receptor alpha by scintillation countingMore data for this Ligand-Target Pair
TargetEstrogen receptor(Homo sapiens (Human))
University Of California

Curated by ChEMBL
LigandPNGBDBM19441(2-(4-hydroxyphenyl)-3-({4-[2-(piperidin-1-yl)ethox...)
Affinity DataIC50:  1.80nMAssay Description:Binding affinity against human estrogen receptor alpha in competitive binding assayMore data for this Ligand-Target Pair
TargetEstrogen receptor(Homo sapiens (Human))
University Of California

Curated by ChEMBL
LigandPNGBDBM19441(2-(4-hydroxyphenyl)-3-({4-[2-(piperidin-1-yl)ethox...)
Affinity DataIC50:  1.80nMAssay Description:Binding affinity towards human recombinant Estrogen receptor alpha was determinedMore data for this Ligand-Target Pair
TargetEstrogen receptor(Homo sapiens (Human))
University Of California

Curated by ChEMBL
LigandPNGBDBM19441(2-(4-hydroxyphenyl)-3-({4-[2-(piperidin-1-yl)ethox...)
Affinity DataIC50:  1.80nMAssay Description:Binding affinity to ERalphaMore data for this Ligand-Target Pair
TargetEstrogen receptor(Homo sapiens (Human))
University Of California

Curated by ChEMBL
LigandPNGBDBM19441(2-(4-hydroxyphenyl)-3-({4-[2-(piperidin-1-yl)ethox...)
Affinity DataIC50:  1.80nMAssay Description:Binding potency for human ER alphaMore data for this Ligand-Target Pair
TargetEstrogen receptor(Homo sapiens (Human))
University Of California

Curated by ChEMBL
LigandPNGBDBM19441(2-(4-hydroxyphenyl)-3-({4-[2-(piperidin-1-yl)ethox...)
Affinity DataIC50:  1.80nMAssay Description:Binding affinity towards human estrogen receptor alphaMore data for this Ligand-Target Pair
TargetEstrogen receptor(Homo sapiens (Human))
University Of California

Curated by ChEMBL
LigandPNGBDBM19441(2-(4-hydroxyphenyl)-3-({4-[2-(piperidin-1-yl)ethox...)
Affinity DataIC50:  1.80nMAssay Description:Inhibition of binding to recombinant human ERalpha by scintillation proximity assayMore data for this Ligand-Target Pair
TargetEstrogen receptor(Homo sapiens (Human))
University Of California

Curated by ChEMBL
LigandPNGBDBM19441(2-(4-hydroxyphenyl)-3-({4-[2-(piperidin-1-yl)ethox...)
Affinity DataIC50:  1.80nMAssay Description:Binding potency for human ER alphaMore data for this Ligand-Target Pair
TargetEstrogen receptor beta(RAT)
Pfizer

Curated by ChEMBL
LigandPNGBDBM19441(2-(4-hydroxyphenyl)-3-({4-[2-(piperidin-1-yl)ethox...)
Affinity DataIC50:  1.90nMAssay Description:Inhibition of estradiol binding to estrogen receptorMore data for this Ligand-Target Pair
TargetEstrogen receptor(Homo sapiens (Human))
University Of California

Curated by ChEMBL
LigandPNGBDBM19441(2-(4-hydroxyphenyl)-3-({4-[2-(piperidin-1-yl)ethox...)
Affinity DataIC50:  2nMAssay Description:Displacement of [3H]17-beta-estradiol from human Estrogen receptor alphaMore data for this Ligand-Target Pair
TargetEstrogen receptor beta(Homo sapiens (Human))TBA
LigandPNGBDBM19441(2-(4-hydroxyphenyl)-3-({4-[2-(piperidin-1-yl)ethox...)
Affinity DataIC50:  4nMAssay Description:In vivo inhibition of human ERalpha/ERbeta co-expressed in HEK 293 cells; 4/60More data for this Ligand-Target Pair
TargetEstrogen receptor(Homo sapiens (Human))
University Of California

Curated by ChEMBL
LigandPNGBDBM19441(2-(4-hydroxyphenyl)-3-({4-[2-(piperidin-1-yl)ethox...)
Affinity DataIC50:  4nMAssay Description:In vitro inhibition of [3H]-17-beta-estradiol binding to human estrogen receptor alphaMore data for this Ligand-Target Pair
TargetEstrogen receptor(RAT)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM19441(2-(4-hydroxyphenyl)-3-({4-[2-(piperidin-1-yl)ethox...)
Affinity DataIC50:  7nMAssay Description:Binding to Estrogen receptor- alpha (ER alpha) receptorMore data for this Ligand-Target Pair
TargetEstrogen receptor(Homo sapiens (Human))
University Of California

Curated by ChEMBL
LigandPNGBDBM19441(2-(4-hydroxyphenyl)-3-({4-[2-(piperidin-1-yl)ethox...)
Affinity DataIC50:  7nMAssay Description:In vitro binding affinity for estrogen receptor alphaMore data for this Ligand-Target Pair
TargetEstrogen receptor beta(Homo sapiens (Human))TBA
LigandPNGBDBM19441(2-(4-hydroxyphenyl)-3-({4-[2-(piperidin-1-yl)ethox...)
Affinity DataIC50:  7.70nMAssay Description:Displacement of [3H]17-beta-estradiol from Estrogen receptor of rabbit uterine tissueMore data for this Ligand-Target Pair
TargetEstrogen receptor(Homo sapiens (Human))
University Of California

Curated by ChEMBL
LigandPNGBDBM19441(2-(4-hydroxyphenyl)-3-({4-[2-(piperidin-1-yl)ethox...)
Affinity DataIC50:  20.6nMpH: 7.5 T: 2°CAssay Description:Arzoxifene and its analogues were assayed in the standard ER competitive radioligand binding assay, using full length human recombinant ER-alpha and ...More data for this Ligand-Target Pair
TargetEstrogen receptor(Homo sapiens (Human))
University Of California

Curated by ChEMBL
LigandPNGBDBM19441(2-(4-hydroxyphenyl)-3-({4-[2-(piperidin-1-yl)ethox...)
Affinity DataIC50:  22nM EC50:  2.40nMpH: 7.4 T: 2°CAssay Description:Radioligand binding assay was performed by using 96-well microtiterplates containing ER, 17beta-estradiol, and the test compound to be tested and SPA...More data for this Ligand-Target Pair
TargetEstrogen receptor(Homo sapiens (Human))
University Of California

Curated by ChEMBL
LigandPNGBDBM19441(2-(4-hydroxyphenyl)-3-({4-[2-(piperidin-1-yl)ethox...)
Affinity DataIC50:  22nM EC50:  2.40nMpH: 7.4 T: 2°CAssay Description:Radioligand binding assay was performed by using 96-well microtiterplates containing ER, 17beta-estradiol, and the test compound to be tested and SPA...More data for this Ligand-Target Pair
TargetEstrogen receptor(Homo sapiens (Human))
University Of California

Curated by ChEMBL
LigandPNGBDBM19441(2-(4-hydroxyphenyl)-3-({4-[2-(piperidin-1-yl)ethox...)
Affinity DataIC50:  22nMpH: 7.4 T: 2°CAssay Description:Radioligand binding assay was performed by using 96-well microtiterplates containing ER, 17beta-estradiol, and the test compound to be tested and SPA...More data for this Ligand-Target Pair
TargetEstrogen receptor(Homo sapiens (Human))
University Of California

Curated by ChEMBL
LigandPNGBDBM19441(2-(4-hydroxyphenyl)-3-({4-[2-(piperidin-1-yl)ethox...)
Affinity DataIC50:  24nMAssay Description:Antagonist activity at estrogen receptor in human Ishikawa cells assessed as 17beta-estradiol-induced alkaline phosphatase activity after 3 days by c...More data for this Ligand-Target Pair
TargetEstrogen receptor beta(Homo sapiens (Human))TBA
LigandPNGBDBM19441(2-(4-hydroxyphenyl)-3-({4-[2-(piperidin-1-yl)ethox...)
Affinity DataIC50:  170nMAssay Description:Displacement of [3H]estradiol from Estrogen receptor in MCF-7 cellsMore data for this Ligand-Target Pair
TargetEstrogen receptor(Homo sapiens (Human))
University Of California

Curated by ChEMBL
LigandPNGBDBM19441(2-(4-hydroxyphenyl)-3-({4-[2-(piperidin-1-yl)ethox...)
Affinity DataIC50:  222nMAssay Description:Antagonist activity at estrogen receptor in human MCF7 cells assessed as 17beta-estradiol-induced cell proliferation after 24 hrs by [14C]thymidine i...More data for this Ligand-Target Pair
TargetEstrogen receptor(Homo sapiens (Human))
University Of California

Curated by ChEMBL
LigandPNGBDBM19441(2-(4-hydroxyphenyl)-3-({4-[2-(piperidin-1-yl)ethox...)
Affinity DataEC50:  22nMAssay Description:Activity against estrogen receptor alphaMore data for this Ligand-Target Pair