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Found 43 Enz. Inhib. hit(s) with Target = 'Estrogen receptor beta' and Ligand = 'BDBM19441'
TargetEstrogen receptor beta(Homo sapiens (Human))
Eli Lilly

LigandPNGBDBM19441(2-(4-hydroxyphenyl)-3-({4-[2-(piperidin-1-yl)ethox...)
Affinity DataKi:  2.74nM ΔG°:  -48.4kJ/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 beta(Homo sapiens (Human))
Eli Lilly

LigandPNGBDBM19441(2-(4-hydroxyphenyl)-3-({4-[2-(piperidin-1-yl)ethox...)
Affinity DataKi:  2.74nMAssay Description:Displacement of [3H]estradiol from ERbeta after 4 hrs by scintillation countingMore data for this Ligand-Target Pair
TargetEstrogen receptor beta(Homo sapiens (Human))
Eli Lilly

LigandPNGBDBM19441(2-(4-hydroxyphenyl)-3-({4-[2-(piperidin-1-yl)ethox...)
Affinity DataKi:  4.30nMAssay Description:Binding affinity to ERbeta (unknown origin)More data for this Ligand-Target Pair
TargetEstrogen receptor beta(Homo sapiens (Human))
Eli Lilly

LigandPNGBDBM19441(2-(4-hydroxyphenyl)-3-({4-[2-(piperidin-1-yl)ethox...)
Affinity DataKi:  4.30nMAssay Description:Binding affinity for estrogen receptor betaMore data for this Ligand-Target Pair
TargetEstrogen receptor beta(Homo sapiens (Human))
Eli Lilly

LigandPNGBDBM19441(2-(4-hydroxyphenyl)-3-({4-[2-(piperidin-1-yl)ethox...)
Affinity DataKi:  4.5nMAssay Description:Antagonistic activity against estrogen receptor beta in presence of 0.1 nM estradiolMore data for this Ligand-Target Pair
TargetEstrogen receptor beta(Homo sapiens (Human))
Eli Lilly

LigandPNGBDBM19441(2-(4-hydroxyphenyl)-3-({4-[2-(piperidin-1-yl)ethox...)
Affinity DataKi:  10nMAssay Description:Ability to displace [3H]-17-beta-estradiol from Estrogen receptor beta by scintillation proximity assay.More data for this Ligand-Target Pair
TargetEstrogen receptor beta(Homo sapiens (Human))
Eli Lilly

LigandPNGBDBM19441(2-(4-hydroxyphenyl)-3-({4-[2-(piperidin-1-yl)ethox...)
Affinity DataKi:  23nMAssay Description:Displacement of [3H]estradiol from full length biotinylated human ERbeta 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: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 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:  0.340nMAssay Description:Inhibition of 17-beta-estradiol (10e-11 M) mediated MCF-7 cell proliferationMore data for this Ligand-Target Pair
TargetEstrogen receptor beta(Homo sapiens (Human))
Eli Lilly

LigandPNGBDBM19441(2-(4-hydroxyphenyl)-3-({4-[2-(piperidin-1-yl)ethox...)
Affinity DataIC50:  1.60nMAssay Description:Inhibition of [3H]-17-beta-estradiol binding to human estrogen receptor betaMore 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 beta(Homo sapiens (Human))
Eli Lilly

LigandPNGBDBM19441(2-(4-hydroxyphenyl)-3-({4-[2-(piperidin-1-yl)ethox...)
Affinity DataIC50:  1.90nMAssay Description:Inhibition of human estrogen receptor 2 using tritiated estradiol incubated for 3 hrMore data for this Ligand-Target Pair
TargetEstrogen receptor beta(Rattus norvegicus)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM19441(2-(4-hydroxyphenyl)-3-({4-[2-(piperidin-1-yl)ethox...)
Affinity DataIC50:  3.40nMAssay Description:Binding affinity foor Rat Estrogen receptor-betaMore 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 beta(Homo sapiens (Human))
Eli Lilly

LigandPNGBDBM19441(2-(4-hydroxyphenyl)-3-({4-[2-(piperidin-1-yl)ethox...)
Affinity DataIC50:  6.90nMAssay Description:Antagonist activity at human wild type ERbeta expressed in HEK293T cells co-expressing ERE assessed as inhibition of estradiol-induced transactivatio...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:  7.70nMAssay Description:Displacement of [3H]17-beta-estradiol from Estrogen receptor of rabbit uterine tissueMore data for this Ligand-Target Pair
TargetEstrogen receptor beta(Homo sapiens (Human))
Eli Lilly

LigandPNGBDBM19441(2-(4-hydroxyphenyl)-3-({4-[2-(piperidin-1-yl)ethox...)
Affinity DataIC50:  8.20nMAssay Description:Inhibition of fluormone ES2 binding to estrogen receptor beta after 1 hr by fluorescence polarization assayMore data for this Ligand-Target Pair
TargetEstrogen receptor beta(Homo sapiens (Human))
Eli Lilly

LigandPNGBDBM19441(2-(4-hydroxyphenyl)-3-({4-[2-(piperidin-1-yl)ethox...)
Affinity DataIC50:  8.20nMAssay Description:Binding affinity to ERbetaMore data for this Ligand-Target Pair
TargetEstrogen receptor beta(Homo sapiens (Human))
Eli Lilly

LigandPNGBDBM19441(2-(4-hydroxyphenyl)-3-({4-[2-(piperidin-1-yl)ethox...)
Affinity DataIC50:  12nMAssay Description:Inhibition of binding to recombinant human ERbeta by scintillation proximity assayMore data for this Ligand-Target Pair
TargetEstrogen receptor beta(Homo sapiens (Human))
Eli Lilly

LigandPNGBDBM19441(2-(4-hydroxyphenyl)-3-({4-[2-(piperidin-1-yl)ethox...)
Affinity DataIC50:  12nMAssay Description:Binding affinity for Human Estrogen receptor-betaMore data for this Ligand-Target Pair
TargetEstrogen receptor beta(Homo sapiens (Human))
Eli Lilly

LigandPNGBDBM19441(2-(4-hydroxyphenyl)-3-({4-[2-(piperidin-1-yl)ethox...)
Affinity DataIC50:  12nMAssay Description:Inhibition of binding to recombinant human estrogen receptor betaMore data for this Ligand-Target Pair
TargetEstrogen receptor beta(Homo sapiens (Human))
Eli Lilly

LigandPNGBDBM19441(2-(4-hydroxyphenyl)-3-({4-[2-(piperidin-1-yl)ethox...)
Affinity DataIC50:  12nMAssay Description:Displacement of [3H]-17-beta-estradiol from full length human estrogen receptor betaMore data for this Ligand-Target Pair
TargetEstrogen receptor beta(Homo sapiens (Human))
Eli Lilly

LigandPNGBDBM19441(2-(4-hydroxyphenyl)-3-({4-[2-(piperidin-1-yl)ethox...)
Affinity DataIC50:  12nMAssay Description:Binding affinity towards human estrogen receptor beta (ERbeta)More data for this Ligand-Target Pair
TargetEstrogen receptor beta(Homo sapiens (Human))
Eli Lilly

LigandPNGBDBM19441(2-(4-hydroxyphenyl)-3-({4-[2-(piperidin-1-yl)ethox...)
Affinity DataIC50:  12nMAssay Description:Binding potency for human ER betaMore data for this Ligand-Target Pair
TargetEstrogen receptor beta(Homo sapiens (Human))
Eli Lilly

LigandPNGBDBM19441(2-(4-hydroxyphenyl)-3-({4-[2-(piperidin-1-yl)ethox...)
Affinity DataIC50:  12nMAssay Description:Binding affinity towards human recombinant Estrogen receptor beta was determinedMore data for this Ligand-Target Pair
TargetEstrogen receptor beta(Homo sapiens (Human))
Eli Lilly

LigandPNGBDBM19441(2-(4-hydroxyphenyl)-3-({4-[2-(piperidin-1-yl)ethox...)
Affinity DataIC50:  12nMAssay Description:Binding potency for human ER betaMore data for this Ligand-Target Pair
TargetEstrogen receptor beta(Homo sapiens (Human))
Eli Lilly

LigandPNGBDBM19441(2-(4-hydroxyphenyl)-3-({4-[2-(piperidin-1-yl)ethox...)
Affinity DataIC50:  12nMAssay Description:Binding affinity against human estrogen receptor beta (ER beta) in competitive binding assayMore data for this Ligand-Target Pair
TargetEstrogen receptor beta(Homo sapiens (Human))
Eli Lilly

LigandPNGBDBM19441(2-(4-hydroxyphenyl)-3-({4-[2-(piperidin-1-yl)ethox...)
Affinity DataIC50:  15nMAssay Description:In vitro inhibition of 1 nM 17-beta-estradiol induced transcriptional activation in T47D cells expressing estrogen receptor betaMore data for this Ligand-Target Pair
TargetEstrogen receptor beta(Homo sapiens (Human))
Eli Lilly

LigandPNGBDBM19441(2-(4-hydroxyphenyl)-3-({4-[2-(piperidin-1-yl)ethox...)
Affinity DataIC50:  18.9nMAssay Description:Inhibition of estrogen receptor betaMore data for this Ligand-Target Pair
TargetEstrogen receptor beta(Homo sapiens (Human))
Eli Lilly

LigandPNGBDBM19441(2-(4-hydroxyphenyl)-3-({4-[2-(piperidin-1-yl)ethox...)
Affinity DataIC50:  43nMAssay Description:Displacement of [3H]17-beta-estradiol from human Estrogen receptor betaMore data for this Ligand-Target Pair
TargetEstrogen receptor beta(Homo sapiens (Human))
Eli Lilly

LigandPNGBDBM19441(2-(4-hydroxyphenyl)-3-({4-[2-(piperidin-1-yl)ethox...)
Affinity DataIC50:  43nMAssay Description:In vitro inhibitory concentration against [3H]-17-beta-estradiol binding to human estrogen receptor 2More 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 beta(Homo sapiens (Human))
Eli Lilly

LigandPNGBDBM19441(2-(4-hydroxyphenyl)-3-({4-[2-(piperidin-1-yl)ethox...)
Affinity DataIC50:  260nMpH: 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 beta(Homo sapiens (Human))
Eli Lilly

LigandPNGBDBM19441(2-(4-hydroxyphenyl)-3-({4-[2-(piperidin-1-yl)ethox...)
Affinity DataIC50:  260nM EC50:  341nMT: 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 beta(Homo sapiens (Human))
Eli Lilly

LigandPNGBDBM19441(2-(4-hydroxyphenyl)-3-({4-[2-(piperidin-1-yl)ethox...)
Affinity DataIC50:  260nM EC50:  341nMT: 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 beta(Rattus norvegicus)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM19441(2-(4-hydroxyphenyl)-3-({4-[2-(piperidin-1-yl)ethox...)
Affinity DataIC50:  470nMAssay Description:Binding to Estrogen receptor- beta (ER beta) receptorMore data for this Ligand-Target Pair
TargetEstrogen receptor beta(Homo sapiens (Human))
Eli Lilly

LigandPNGBDBM19441(2-(4-hydroxyphenyl)-3-({4-[2-(piperidin-1-yl)ethox...)
Affinity DataIC50:  470nMAssay Description:In vitro binding affinity for estrogen receptor betaMore data for this Ligand-Target Pair
TargetEstrogen receptor beta(Homo sapiens (Human))
Eli Lilly

LigandPNGBDBM19441(2-(4-hydroxyphenyl)-3-({4-[2-(piperidin-1-yl)ethox...)
Affinity DataIC50:  557nMpH: 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 beta(Homo sapiens (Human))
Eli Lilly

LigandPNGBDBM19441(2-(4-hydroxyphenyl)-3-({4-[2-(piperidin-1-yl)ethox...)
Affinity DataIC50:  1.42E+3nMAssay Description:Binding affinity to human recombinant ERbeta by competitive fluorometric binding assayMore data for this Ligand-Target Pair
TargetEstrogen receptor beta(Homo sapiens (Human))
Eli Lilly

LigandPNGBDBM19441(2-(4-hydroxyphenyl)-3-({4-[2-(piperidin-1-yl)ethox...)
Affinity DataIC50:  7.43E+3nMAssay Description:Antagonist activity at ERbeta (unknown origin)More data for this Ligand-Target Pair