BDBM50238741 CHEBI:31638::Faslodex::Fulvestrant::ICI-182780::ZD-9238
SMILES [H][C@@]12CC[C@H](O)[C@@]1(C)CC[C@]1([H])c3ccc(O)cc3C[C@@H](CCCCCCCCC[S+]([O-])CCCC(F)(F)C(F)(F)F)[C@@]21[H]
InChI Key InChIKey=VWUXBMIQPBEWFH-UHFFFAOYSA-N
Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB
Found 47 hits for monomerid = 50238741
Affinity DataIC50: 0.300nMAssay Description:Antagonist activity at ERbeta expressed in HEK293/Gal4 cells incubated for 24 hrs in presence of di-arylpropionitrile by luciferase reporter gene ass...More data for this Ligand-Target Pair
Affinity DataIC50: 0.300nMAssay Description:Downregulation of human ERalpha in human MCF-7 cells after 24 hrs by in-cell Western immunoassay methodMore data for this Ligand-Target Pair
Affinity DataIC50: 8.5nMAssay Description:Downregulation of ER-alpha expression in human tamoxifen-resistant T47D cells over-expressing PKC-alpha measured after 5 days by Western blot analysi...More data for this Ligand-Target Pair
Affinity DataIC50: 0.320nMAssay Description:Induction of ERalpha degradation in human MCF7 cells after 4 hrs by FITC/Hoechst staining based immunofluorescence imaging analysisMore data for this Ligand-Target Pair
Affinity DataIC50: 0.840nMAssay Description:Induction of ERalpha degradation in human T47D cellsMore data for this Ligand-Target Pair
TargetNAD-dependent protein deacylase sirtuin-5, mitochondrial(Human)
Ludwig-Maximilians University
Curated by ChEMBL
Ludwig-Maximilians University
Curated by ChEMBL
Affinity DataIC50: 2.60E+3nMAssay Description:Inhibition of SIRT5 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 2.90nMAssay Description:Displacement of fluorescent-labelled E2 from recombinant human GST-tagged ERalpha by LanthaScreen TR-FRET assayMore data for this Ligand-Target Pair
Affinity DataIC50: 10nMAssay Description:Displacement of fluorescent-labelled E2 from recombinant human GST-tagged ERbeta by LanthaScreen TR-FRET assayMore data for this Ligand-Target Pair
Affinity DataIC50: 89nMAssay Description:Displacement of fluorescent estradiol from full-length ERalpha (unknown origin) measured after 2 hrs by fluorescence polarization assayMore data for this Ligand-Target Pair
Affinity DataIC50: 0.25nMAssay Description:Antagonist activity at estrogen receptor in human T47D cells incubated for 18 hrs by ultra high sensitivity luminescence reporter gene assayMore data for this Ligand-Target Pair
Affinity DataIC50: 10nMAssay Description:Displacement of fluorescent-labeled E2 from LBD of ERbeta (unknown origin) by TR-FRET assayMore data for this Ligand-Target Pair
Affinity DataIC50: 1nMAssay Description:Antagonist activity at ERalpha expressed in HEK293/Gal4 cells incubated for 24 hrs in presence of estradiol by luciferase reporter gene assayMore data for this Ligand-Target Pair
Affinity DataIC50: 9.30nMAssay Description:Downregulation of ER-alpha expression in human T47D cells measured after 5 days by Western blot analysisMore data for this Ligand-Target Pair
Affinity DataIC50: 2.90nMAssay Description:Displacement of fluorescent-labeled E2 from LBD of ERalpha (unknown origin) by TR-FRET assayMore data for this Ligand-Target Pair
Affinity DataEC50: 4.20nMAssay Description:Antagonist activity against ERalpha in estradiol stimulated HEK293T cells measuring luciferase activity after 24 hrs by luciferase reporter assayMore data for this Ligand-Target Pair
Affinity DataEC50: 6.70nMAssay Description:Antagonist activity against ERbeta in estradiol stimulated HEK293T cells measuring luciferase activity after 24 hrs by luciferase reporter assayMore data for this Ligand-Target Pair
Affinity DataIC50: 1.60nMAssay Description:Binding affinity to human wild type ERalpha ligand binding domainMore data for this Ligand-Target Pair
Affinity DataIC50: 3.30nMAssay Description:Binding affinity to human ERalpha D538G mutant ligand binding domainMore data for this Ligand-Target Pair
Affinity DataIC50: 3.80nMAssay Description:Binding affinity to human ERalpha Y537S mutant ligand binding domainMore data for this Ligand-Target Pair
Affinity DataIC50: 0.5nMAssay Description:Inhibition of ERalpha (246 to 595 residues) in doxycycline-induced human HEK293 cells incubated overnight by luciferase based assayMore data for this Ligand-Target Pair
Affinity DataIC50: 0.900nMAssay Description:Inhibition of ERbeta (261 to 500 residues) in doxycycline-induced human HEK293 cells incubated overnight by luciferase based assayMore data for this Ligand-Target Pair
Affinity DataEC50: 0.200nMAssay Description:Induction of ERalpha degradation in human MCF7 cellsMore data for this Ligand-Target Pair
Affinity DataIC50: 13nMAssay Description:Antagonist activity at ER-alpha (unknown origin) by ER-alpha coactivator assayMore data for this Ligand-Target Pair
Affinity DataIC50: 4nMAssay Description:Inhibition of 10e-9 M E2 stimulated MCF-7 breast cancer cell proliferationMore data for this Ligand-Target Pair
Affinity DataIC50: 1.33E+5nMAssay Description:Inhibition of human BSEP overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-taurocholate in presence of ATP measured after 15 to ...More data for this Ligand-Target Pair
Affinity DataIC50: 1.33E+5nMAssay Description:Inhibition of human MRP2 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and...More data for this Ligand-Target Pair
Affinity DataIC50: 1.33E+5nMAssay Description:Inhibition of human MRP3 overexpressed in Sf9 insect cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ...More data for this Ligand-Target Pair
Affinity DataIC50: 1.33E+5nMAssay Description:Inhibition of human MRP4 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and...More data for this Ligand-Target Pair
Affinity DataIC50: 3.40nMAssay Description:Induction of selective estrogen receptor alpha degradation in human MCF7 cells harboring TK-ERE-Luc assessed as reduction in estradiol-induced transc...More data for this Ligand-Target Pair
Affinity DataIC50: 1.20nMAssay Description:Induction of selective estrogen receptor alpha degradation in human MCF7 cells after 18 to 24 hrs by in-cell Western analysisMore data for this Ligand-Target Pair
Affinity DataIC50: 3.80nMAssay Description:Induction of selective estrogen receptor alpha degradation in human MCF7 cells harboring TK-ERE-Luc assessed as reduction in estradiol-induced GREB1 ...More data for this Ligand-Target Pair
Affinity DataIC50: 5nMAssay Description:Inhibition of 10e-9 M E2 stimulated transcriptional activation in ER+MCF-7/2a breast cancer cellsMore data for this Ligand-Target Pair
Affinity DataIC50: 0.210nMAssay Description:Inhibition of ER-MDA-MB 231 breast cancer cell proliferation over 200 hrMore data for this Ligand-Target Pair
Affinity DataIC50: 3nMAssay Description:Displacement of fluoromone ligand from recombinant ER-alpha (unknown origin) by LanthaScreen TR-FRET assayMore data for this Ligand-Target Pair
Affinity DataIC50: 0.780nMAssay 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
Affinity DataKd: 4.70nMAssay 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
Affinity DataEC50: 1.40nMAssay 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
Affinity DataIC50: 5nMAssay Description:Antagonist activity at ERalpha in human MCF7 cells assessed as inhibition of estradiol-driven cell growth measured after 7 days by SYTOX green-based ...More data for this Ligand-Target Pair
Affinity DataIC50: 1.60nMAssay Description:Inhibition of ERalpha in human MCF7:WS8 cells assessed as increase in degradation of ERalpha incubated for 24 hrs by In-Cell Western assayMore data for this Ligand-Target Pair
Affinity DataEC50: 0.400nMAssay Description:Induction of ERalpha degradation in human MCF7 cells in phenol red free RPMI medium containing 5% charcoal-stripped FBS incubated for 4 hrs by IRDye ...More data for this Ligand-Target Pair
Affinity DataIC50: 5.59E+4nMAssay Description:Inhibition of bacterial wild type Beta-lactamase TEM-1 pre-incubated for 5 mins before addition of chromogenic beta-lactamase substrate CENTA by spec...More data for this Ligand-Target Pair
Affinity DataIC50: 5.59E+4nMAssay Description:Inhibition of bacterial wild type Beta-lactamase TEM-1 pre-incubated for 5 mins before addition of chromogenic beta-lactamase substrate CENTA by spec...More data for this Ligand-Target Pair
Affinity DataKi: 0.668nMAssay Description:Apparent inhibition constant for estrogen receptor in Human uterine cytosol in 2.5%DMFMore data for this Ligand-Target Pair
Affinity DataKi: 0.755nMAssay Description:Apparent inhibition constant for estrogen receptor in Human Breast cancer cytosol in 2.5%DMFMore data for this Ligand-Target Pair
Affinity DataKi: 7.60nMAssay Description:Inhibition of estradiol binding to estrogen receptor in Human Breast cancer cytosol (3.3% ethanol)More data for this Ligand-Target Pair
Affinity DataKi: 40nMAssay Description:Binding affinity to ERalpha (unknown origin) assessed as inhibition constant incubated for 2 hrs by fluorescence polarization assayMore data for this Ligand-Target Pair
Affinity DataKi: 190nMAssay Description:Binding affinity to ERbeta (unknown origin) assessed as inhibition constant incubated for 2 hrs by fluorescence polarization assayMore data for this Ligand-Target Pair