BDBM19441 2-(4-hydroxyphenyl)-3-({4-[2-(piperidin-1-yl)ethoxy]phenyl}carbonyl)-1-benzothiophen-6-ol::CHEMBL81::Evista::Keoxifene::RALOXIFENE HYDROCHLORIDE::Raloxifene::Raloxifene (7)::Raloxifene, 6::[6-hydroxy-2-(4-hydroxyphenyl)-1-benzothiophen-3-yl]-[4-(2-piperidin-1-ylethoxy)phenyl]methanone::cid_11071264

SMILES Oc1ccc(cc1)-c1sc2cc(O)ccc2c1C(=O)c1ccc(OCCN2CCCCC2)cc1

InChI Key InChIKey=GZUITABIAKMVPG-UHFFFAOYSA-N

Data  28 KI  100 IC50  2 Kd  11 EC50

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
Find this compound or compounds like it in BindingDB:
   Substructure
Similarity at least:  must be >=0.5
Exact match

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 135 hits for monomerid = 19441   

TargetEstrogen receptor(Human)
University of California

Curated by ChEMBL
LigandPNGBDBM19441(Evista | CHEMBL81 | Keoxifene | Raloxifene, 6 | RA...)
Affinity DataKi:  0.0300nMAssay Description:Antagonistic activity against estrogen receptor alpha in presence of 0.1 nM estradiolMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetEstrogen receptor(Human)
University of California

Curated by ChEMBL
LigandPNGBDBM19441(Evista | CHEMBL81 | Keoxifene | Raloxifene, 6 | RA...)
Affinity DataKi:  0.0700nMAssay Description:Displacement of [3H]estradiol from human ER-alpha expressed in Sf21 cells incubated for 120 mins by scintillation counting analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/16/2024
Entry Details
PubMed
TargetEstrogen receptor(Human)
University of California

Curated by ChEMBL
LigandPNGBDBM19441(Evista | CHEMBL81 | Keoxifene | Raloxifene, 6 | RA...)
Affinity DataIC50: 0.180nMAssay Description:Antagonist activity at FLAG-tagged ERalpha (unknown origin) expressed in HEK293 cells assessed as reduction in E2-induced ER-alpha-mediated transcrip...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/24/2021
Entry Details Article
PubMed
TargetEstrogen receptor beta(Human)
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM19441(Evista | CHEMBL81 | Keoxifene | Raloxifene, 6 | RA...)
Affinity DataIC50: 0.200nMAssay Description:Inhibition of estradiol-stimulated MCF-7 breast adenocarcinoma cell proliferationMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetEstrogen receptor beta(Human)
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM19441(Evista | CHEMBL81 | Keoxifene | Raloxifene, 6 | RA...)
Affinity DataIC50: 0.200nMAssay Description:In vitro inhibition of estrogen-stimulated MCF-7 cell proliferationMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/20/2018
Entry Details Article
PubMed
TargetEstrogen receptor beta(Human)
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM19441(Evista | CHEMBL81 | Keoxifene | Raloxifene, 6 | RA...)
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
In Depth
Date in BDB:
8/21/2020
Entry Details Article
PubMed
TargetEstrogen receptor beta(Human)
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM19441(Evista | CHEMBL81 | Keoxifene | Raloxifene, 6 | RA...)
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 Depth
Date in BDB:
10/6/2018
Entry Details

TargetEstrogen receptor(Human)
University of California

Curated by ChEMBL
LigandPNGBDBM19441(Evista | CHEMBL81 | Keoxifene | Raloxifene, 6 | RA...)
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
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetEstrogen receptor(Human)
University of California

Curated by ChEMBL
LigandPNGBDBM19441(Evista | CHEMBL81 | Keoxifene | Raloxifene, 6 | RA...)
Affinity DataIC50: 0.240nMAssay Description:Displacement of [3H]estradiol from human ER-alpha expressed in Sf21 cells incubated for 120 mins by scintillation counting analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/16/2024
Entry Details
PubMed
TargetEstrogen receptor(Human)
University of California

Curated by ChEMBL
LigandPNGBDBM19441(Evista | CHEMBL81 | Keoxifene | Raloxifene, 6 | RA...)
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
In Depth
Date in BDB:
3/20/2011
Entry Details Article
PubMed
TargetEstrogen receptor beta(Human)
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM19441(Evista | CHEMBL81 | Keoxifene | Raloxifene, 6 | RA...)
Affinity DataIC50: 0.340nMAssay Description:Inhibition of 17-beta-estradiol (10e-11 M) mediated MCF-7 cell proliferationMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/21/2018
Entry Details Article
PubMed
TargetEstrogen receptor(Human)
University of California

Curated by ChEMBL
LigandPNGBDBM19441(Evista | CHEMBL81 | Keoxifene | Raloxifene, 6 | RA...)
Affinity DataKi:  0.370nMAssay Description:Displacement of [3H]estradiol from ERalpha after 4 hrs by scintillation countingMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/7/2013
Entry Details Article
PubMed
TargetEstrogen receptor(Human)
University of California

Curated by ChEMBL
LigandPNGBDBM19441(Evista | CHEMBL81 | Keoxifene | Raloxifene, 6 | RA...)
Affinity DataKi:  0.370nM ΔG°:  -12.7kcal/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
In Depth
Date in BDB:
1/15/2008
Entry Details Article
PubMed
TargetEstrogen receptor(Human)
University of California

Curated by ChEMBL
LigandPNGBDBM19441(Evista | CHEMBL81 | Keoxifene | Raloxifene, 6 | RA...)
Affinity DataKi:  0.380nMAssay Description:Binding affinity to ERalpha ligand binding domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/7/2013
Entry Details Article
PubMed
TargetEstrogen receptor(Human)
University of California

Curated by ChEMBL
LigandPNGBDBM19441(Evista | CHEMBL81 | Keoxifene | Raloxifene, 6 | RA...)
Affinity DataKi:  0.400nMAssay Description:Binding affinity for estrogen receptor alphaMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetEstrogen receptor(Human)
University of California

Curated by ChEMBL
LigandPNGBDBM19441(Evista | CHEMBL81 | Keoxifene | Raloxifene, 6 | RA...)
Affinity DataKi:  0.430nMAssay Description:Binding affinity to ERalpha (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/4/2020
Entry Details Article
PubMed
TargetEstrogen receptor(Human)
University of California

Curated by ChEMBL
LigandPNGBDBM19441(Evista | CHEMBL81 | Keoxifene | Raloxifene, 6 | RA...)
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
In Depth
Date in BDB:
1/11/2010
Entry Details Article
PubMed
TargetEstrogen receptor(Human)
University of California

Curated by ChEMBL
LigandPNGBDBM19441(Evista | CHEMBL81 | Keoxifene | Raloxifene, 6 | RA...)
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
In Depth
Date in BDB:
9/4/2017
Entry Details Article
PubMed
TargetEstrogen receptor(Human)
University of California

Curated by ChEMBL
LigandPNGBDBM19441(Evista | CHEMBL81 | Keoxifene | Raloxifene, 6 | RA...)
Affinity DataEC50:  0.660nMAssay Description:Selective estrogen receptor down-regulator activity at FLAG-tagged ERalpha (unknown origin) expressed in HEK293 cells assessed as induction of ERalph...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/24/2021
Entry Details Article
PubMed
TargetEstrogen receptor(Rat)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM19441(Evista | CHEMBL81 | Keoxifene | Raloxifene, 6 | RA...)
Affinity DataIC50: 0.700nMAssay Description:Binding affinity for Rat Estrogen receptor-alphaMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetEstrogen receptor(Human)
University of California

Curated by ChEMBL
LigandPNGBDBM19441(Evista | CHEMBL81 | Keoxifene | Raloxifene, 6 | RA...)
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
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetEstrogen receptor(Human)
University of California

Curated by ChEMBL
LigandPNGBDBM19441(Evista | CHEMBL81 | Keoxifene | Raloxifene, 6 | RA...)
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
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetEstrogen receptor(Human)
University of California

Curated by ChEMBL
LigandPNGBDBM19441(Evista | CHEMBL81 | Keoxifene | Raloxifene, 6 | RA...)
Affinity DataIC50: 0.720nMAssay Description:Antagonist effect on transcriptional activation in MCF-7 cells expressing estrogen receptor alphaMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/1/2012
Entry Details Article
PubMed
TargetEstrogen receptor(Human)
University of California

Curated by ChEMBL
LigandPNGBDBM19441(Evista | CHEMBL81 | Keoxifene | Raloxifene, 6 | RA...)
Affinity DataIC50: 0.730nMAssay Description:Inhibition of estrogen receptor alphaMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetEstrogen receptor(Human)
University of California

Curated by ChEMBL
LigandPNGBDBM19441(Evista | CHEMBL81 | Keoxifene | Raloxifene, 6 | RA...)
Affinity DataIC50: 0.740nMAssay Description:Antagonist activity at ERalpha (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/21/2023
Entry Details
PubMed
TargetAldehyde oxidase(Human)
Nova University Lisbon

Curated by ChEMBL
LigandPNGBDBM19441(Evista | CHEMBL81 | Keoxifene | Raloxifene, 6 | RA...)
Affinity DataKi:  0.870nMAssay Description:Uncompetitive type inhibition of human AOX assessed as inhibition constant using phthalazine as substrate preincubated for 30 mins followed by substr...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/4/2023
Entry Details Article
PubMed
TargetAldehyde oxidase(Human)
Nova University Lisbon

Curated by ChEMBL
LigandPNGBDBM19441(Evista | CHEMBL81 | Keoxifene | Raloxifene, 6 | RA...)
Affinity DataKi:  0.870nMAssay Description:Uncompetitive type inhibition of human AOX assessed as inhibition constant using vanillin as substrate by HPLC-MS analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/4/2023
Entry Details Article
PubMed
TargetAldehyde oxidase(Human)
Nova University Lisbon

Curated by ChEMBL
LigandPNGBDBM19441(Evista | CHEMBL81 | Keoxifene | Raloxifene, 6 | RA...)
Affinity DataKi:  0.870nMAssay Description:Uncompetitive type inhibition of human AOX assessed as inhibition constant using nicotine-1(S)-iminium ion as substrate incubated for 2 mins by HPLC-...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/4/2023
Entry Details Article
PubMed
TargetAldehyde oxidase(Human)
Nova University Lisbon

Curated by ChEMBL
LigandPNGBDBM19441(Evista | CHEMBL81 | Keoxifene | Raloxifene, 6 | RA...)
Affinity DataKi:  0.870nMAssay Description:Uncompetitive inhibition of human liver cytosolic aldehyde oxidase using phthalazine as substrate assessed as enzyme-substrate complex by Lineweaver-...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/8/2016
Entry Details Article
PubMed
TargetEstrogen receptor(Human)
University of California

Curated by ChEMBL
LigandPNGBDBM19441(Evista | CHEMBL81 | Keoxifene | Raloxifene, 6 | RA...)
Affinity DataIC50: 0.890nMAssay Description:Inhibition of [3H]17-beta-estradiol binding to human estrogen receptor alphaMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
Target3-beta-hydroxysteroid-Delta(8),Delta(7)-isomerase(Human)
University of Innsbruck

Curated by ChEMBL
LigandPNGBDBM19441(Evista | CHEMBL81 | Keoxifene | Raloxifene, 6 | RA...)
Affinity DataKi:  1nMAssay Description:Affinity for human EMP expressed in ERG2 deficient strain of Saccharomyces cerevisiae using [3H]ifenprodil or (+)-[3H]pentazocine as radioligandMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/3/2012
Entry Details Article
PubMed
TargetEstrogen receptor beta(Human)
Chinese Academy of Sciences

Curated by ChEMBL
LigandPNGBDBM19441(Evista | CHEMBL81 | Keoxifene | Raloxifene, 6 | RA...)
Affinity DataIC50: 1.60nMAssay Description:Inhibition of [3H]17-beta-estradiol binding to human estrogen receptor betaMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetEstrogen receptor(Human)
University of California

Curated by ChEMBL
LigandPNGBDBM19441(Evista | CHEMBL81 | Keoxifene | Raloxifene, 6 | RA...)
Affinity DataIC50: 1.80nMAssay Description:Inhibition of binding to recombinant human ERalpha by scintillation proximity assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetEstrogen receptor(Human)
University of California

Curated by ChEMBL
LigandPNGBDBM19441(Evista | CHEMBL81 | Keoxifene | Raloxifene, 6 | RA...)
Affinity DataIC50: 1.80nMAssay Description:Binding potency for human ER alphaMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetEstrogen receptor(Human)
University of California

Curated by ChEMBL
LigandPNGBDBM19441(Evista | CHEMBL81 | Keoxifene | Raloxifene, 6 | RA...)
Affinity DataIC50: 1.80nMAssay Description:Binding affinity towards human estrogen receptor alphaMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetEstrogen receptor(Human)
University of California

Curated by ChEMBL
LigandPNGBDBM19441(Evista | CHEMBL81 | Keoxifene | Raloxifene, 6 | RA...)
Affinity DataIC50: 1.80nMAssay Description:Displacement of [3H]17-beta-estradiol from full length human estrogen receptor alphaMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetEstrogen receptor(Human)
University of California

Curated by ChEMBL
LigandPNGBDBM19441(Evista | CHEMBL81 | Keoxifene | Raloxifene, 6 | RA...)
Affinity DataIC50: 1.80nMAssay Description:Binding affinity for Human Estrogen receptor-alphaMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetEstrogen receptor(Human)
University of California

Curated by ChEMBL
LigandPNGBDBM19441(Evista | CHEMBL81 | Keoxifene | Raloxifene, 6 | RA...)
Affinity DataIC50: 1.80nMAssay Description:Binding affinity towards human recombinant Estrogen receptor alpha was determinedMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetEstrogen receptor(Human)
University of California

Curated by ChEMBL
LigandPNGBDBM19441(Evista | CHEMBL81 | Keoxifene | Raloxifene, 6 | RA...)
Affinity DataIC50: 1.80nMAssay Description:Displacement of radiolabeled estrogen from estrogen receptor alpha by scintillation countingMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/16/2010
Entry Details Article
PubMed
TargetEstrogen receptor(Human)
University of California

Curated by ChEMBL
LigandPNGBDBM19441(Evista | CHEMBL81 | Keoxifene | Raloxifene, 6 | RA...)
Affinity DataIC50: 1.80nMAssay Description:Binding affinity to ERalphaMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetEstrogen receptor(Human)
University of California

Curated by ChEMBL
LigandPNGBDBM19441(Evista | CHEMBL81 | Keoxifene | Raloxifene, 6 | RA...)
Affinity DataIC50: 1.80nMAssay Description:Binding affinity against human estrogen receptor alpha in competitive binding assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetEstrogen receptor(Human)
University of California

Curated by ChEMBL
LigandPNGBDBM19441(Evista | CHEMBL81 | Keoxifene | Raloxifene, 6 | RA...)
Affinity DataIC50: 1.80nMAssay Description:Binding potency for human ER alphaMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetEstrogen receptor(Human)
University of California

Curated by ChEMBL
LigandPNGBDBM19441(Evista | CHEMBL81 | Keoxifene | Raloxifene, 6 | RA...)
Affinity DataIC50: 1.80nMAssay Description:Inhibition of bindign to recombinant human estrogen receptor alphaMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetEstrogen receptor beta(Rat)
Pfizer

Curated by ChEMBL
LigandPNGBDBM19441(Evista | CHEMBL81 | Keoxifene | Raloxifene, 6 | RA...)
Affinity DataIC50: 1.90nMAssay Description:Inhibition of estradiol binding to estrogen receptorMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/21/2020
Entry Details Article
PubMed
TargetEstrogen receptor beta(Human)
Chinese Academy of Sciences

Curated by ChEMBL
LigandPNGBDBM19441(Evista | CHEMBL81 | Keoxifene | Raloxifene, 6 | RA...)
Affinity DataIC50: 1.90nMAssay Description:Inhibition of human estrogen receptor 2 using tritiated estradiol incubated for 3 hrMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetEstrogen receptor(Human)
University of California

Curated by ChEMBL
LigandPNGBDBM19441(Evista | CHEMBL81 | Keoxifene | Raloxifene, 6 | RA...)
Affinity DataKi:  2nMAssay Description:Displacement of [3H]estradiol from full length biotinylated human ERalpha by scintillation proximity assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
1/11/2010
Entry Details Article
PubMed
TargetEstrogen receptor(Human)
University of California

Curated by ChEMBL
LigandPNGBDBM19441(Evista | CHEMBL81 | Keoxifene | Raloxifene, 6 | RA...)
Affinity DataIC50: 2nMAssay Description:Displacement of [3H]17-beta-estradiol from human Estrogen receptor alphaMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/1/2012
Entry Details Article
PubMed
TargetAldehyde oxidase(Human)
Nova University Lisbon

Curated by ChEMBL
LigandPNGBDBM19441(Evista | CHEMBL81 | Keoxifene | Raloxifene, 6 | RA...)
Affinity DataKi:  2.30nMAssay Description:Competitive inhibition of human liver cytosolic aldehyde oxidase using DACA as substrate assessed as free enzyme by Lineweaver-Burk plot analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/8/2016
Entry Details Article
PubMed
TargetEstrogen receptor(Human)
University of California

Curated by ChEMBL
LigandPNGBDBM19441(Evista | CHEMBL81 | Keoxifene | Raloxifene, 6 | RA...)
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
In Depth
Date in BDB:
3/16/2008
Entry Details Article
PubMed
TargetEstrogen receptor(Human)
University of California

Curated by ChEMBL
LigandPNGBDBM19441(Evista | CHEMBL81 | Keoxifene | Raloxifene, 6 | RA...)
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
In Depth
Date in BDB:
3/16/2008
Entry Details Article
PubMed
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