BDBM50425732 ENZALUTAMIDE::US10053433, FC 4.129::US10806720, Compound Enzalutamide::US11230523, Compound Enzalutamide::US11648234, Compound Enzalutamide::US20230382870, Enzalutamide::Xtandi
SMILES CNC(=O)c1ccc(cc1F)N1C(=S)N(C(=O)C1(C)C)c1ccc(C#N)c(c1)C(F)(F)F
InChI Key InChIKey=WXCXUHSOUPDCQV-UHFFFAOYSA-N
Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB
Found 75 hits for monomerid = 50425732
Affinity DataIC50: 75nMAssay Description:Antagonist activity at androgen receptor in human LNCaP cells harboring eGFP/ARRIPB incubated for 3 days by fluorescence methodMore data for this Ligand-Target Pair
Affinity DataIC50: 25nMAssay Description:Antagonist activity at androgen receptor (unknown origin) in human LNCap-ARR2PB-eGFP cells by measuring fluorescence intensity measured after 3 days ...More data for this Ligand-Target Pair
Affinity DataIC50: 1.00E+4nMAssay Description:Antagonist activity at glucocorticoid receptor in human HeLa cells assessed as reduction in dexamethasone-induced luciferase activity by dual-Glo luc...More data for this Ligand-Target Pair
Affinity DataIC50: 480nMAssay Description:Inhibition of AR transcriptional activity in human LNCaP cells harboring ARR2PB-eGFP assessed as decrease in PSA levelMore data for this Ligand-Target Pair
Affinity DataIC50: 14nMAssay Description:Inhibition of AR transcriptional activity in human LNCaP cells harboring ARR2PB-eGFP incubated for 72 hrs by fluorescence assayMore data for this Ligand-Target Pair
Affinity DataIC50: 80nMAssay Description:Binding affinity to GST-tagged AR ligand binding domain (unknown origin) measured after 4 hrs by fluorescence polarization assayMore data for this Ligand-Target Pair
Affinity DataKd: 2.95E+5nMAssay Description:Binding affinity to human AR LBD (663 to 920 residues) expressed in Escherichia coli BL21 (DE3) assessed as dissociation constant in presence of DHT ...More data for this Ligand-Target Pair
Affinity DataIC50: 70nMAssay Description:Antagonist activity against human androgen receptor expressed in human LNCap cells trasfected with ARR2PB-eGFP cells incubated for 3 days by fluoresc...More data for this Ligand-Target Pair
Affinity DataKd: 4.02E+4nMAssay Description:Binding affinity to human AR LBD (663 to 920 residues) expressed in Escherichia coli BL21 (DE3) assessed as dissociation constant by biolayer interfe...More data for this Ligand-Target Pair
Affinity DataKd: 6.52E+3nMAssay Description:Binding affinity to full length androgen receptor (unknown origin) assessed as dissociation constant at 5 uM measured after 15 mins by biolayer inter...More data for this Ligand-Target Pair
Affinity DataIC50: 117nMAssay Description:Antagonist activity at wild type androgen receptor in castration-resistant human LNCaP cells assessed as inhibition of R1881-stimulated receptor tran...More data for this Ligand-Target Pair
Affinity DataIC50: 216nMAssay Description:Antagonist activity at human androgen receptor expressed in HEK-293 cells harboring GRE-LUC and CMV-renilla luciferase assessed as inhibition of tran...More data for this Ligand-Target Pair
Affinity DataIC50: 117nMAssay Description:Antagonist activity at AR wild-type (unknown origin) transfected in human LNCAP cells cotransfected with ARE-LUC incubated for 20 to 24 hrs in presen...More data for this Ligand-Target Pair
Affinity DataEC50: 62nMAssay Description:Agonist activity at VP16-AR F877L mutant (unknown origin) transfected in human HepG2 cells cotransfected with ARE-LUC incubated for 48 hrs by steady-...More data for this Ligand-Target Pair
Affinity DataIC50: 2.90E+4nMAssay Description:Displacement of [3H]dexamethasone from glucocorticoid receptor in human IM-9 cells incubated for 6 hrs by scintillation counting analysisMore data for this Ligand-Target Pair
Affinity DataIC50: 219nMAssay Description:Inhibition of androgen receptor (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 647nMAssay Description:Antagonist activity at androgen receptor (unknown origin) expressed in HEK293 cells using DHT as substrate preincubated for 30 mins followed by subst...More data for this Ligand-Target Pair
Affinity DataIC50: 38nMAssay Description:Displacement of [3H]methyltrienolone from wild-type androgen receptor in human LNCaP cells incubated for 24 hrs by scintillation counting analysisMore data for this Ligand-Target Pair
Affinity DataEC50: 1.14E+4nMAssay Description:Agonist activity at full length androgen receptor F877L mutant (unknown origin) expressed in PC-3 cells assessed as transcriptional activityMore data for this Ligand-Target Pair
Affinity DataEC50: 1.07E+3nMAssay Description:Agonist activity at full length androgen receptor F876L/T877A mutant (unknown origin) expressed in PC-3 cells assessed as transcriptional activityMore data for this Ligand-Target Pair
Affinity DataIC50: 492nMAssay Description:Antagonist activity at DHT-induced Androgen receptor transcriptional activity in human HEK293 cells measured after 24 hrs by Steady-Glo reagent based...More data for this Ligand-Target Pair
Affinity DataIC50: 112nMAssay Description:Antagonist activity at androgen receptor T877A mutant (unknown origin) expressed in HEK293 cells incubated for 24 hrs by luciferase reporter assayMore data for this Ligand-Target Pair
Affinity DataIC50: 218nMAssay Description:Reagents and instruments: radiolabeled dihydrotestosterone (DHT-d3) and unlabelled dihydrotestosterone (DHT) purchased from Sigma-Aldrich (St. Louis,...More data for this Ligand-Target Pair
Affinity DataIC50: 450nMAssay Description:Anti-androgenic activity at androgen receptor (unknown origin) expressed in HEK293 cells by BRET assayMore data for this Ligand-Target Pair
Affinity DataEC50: 1.10E+3nMAssay Description:Antagonist activity at Androgen receptor in human LNCaP C4-2 cells transfected with PSA6.1-luc and pRL-TK measured by luciferase gene reporter assayMore data for this Ligand-Target Pair
Affinity DataIC50: 216nMAssay Description:Methods: hAR-LBD (633-919) was cloned into pGex4t.1. Large scale GST-tagged AR-LBD was prepared and purified using a GST column. Recombinant AR-LBD w...More data for this Ligand-Target Pair
Affinity DataIC50: 800nMAssay Description:Displacement of Fluormone AL Green from androgen receptor LBD (unknown origin) incubated for 4 hrs by fluorescence polarization assayMore data for this Ligand-Target Pair
Affinity DataIC50: 522nMAssay Description:Antagonist activity at wild type androgen receptor expressed in HEK293 cells assessed as reduction in DHT-induced transcriptional activation of andro...More data for this Ligand-Target Pair
Affinity DataIC50: 1.03E+3nMAssay Description:Antagonist activity at androgen receptor W741L mutant expressed in HEK293 cells assessed as reduction in DHT-induced transcriptional activation of an...More data for this Ligand-Target Pair
Affinity DataIC50: 112nMAssay Description:Antagonist activity at androgen receptor T877A mutant expressed in HEK293 cells assessed as reduction in DHT-induced transcriptional activation of an...More data for this Ligand-Target Pair
Affinity DataIC50: 216nMAssay Description:Antagonist activity at CMV-tagged full length wild type human AR expressed in HEK293 cells co-transfected with GRE-LUC and CMV-renilla LUC assessed a...More data for this Ligand-Target Pair
Affinity DataIC50: 800nMAssay Description:Binding affinity to GST-tagged androgen receptor LBD (unknown origin) incubated for 4 hrs by fluorescence polarization assayMore data for this Ligand-Target Pair
Affinity DataIC50: 340nMAssay Description:Inhibition of androgen receptor in human VCaP cells expressing GRE-2-TATA-Luc co-expressing firefly luciferase incubated for 24 hrs in presence of DH...More data for this Ligand-Target Pair
Affinity DataIC50: 294nMAssay Description:Displacement of fluormone-DHT green from His/GST-tagged rat AR ligand binding domain after 4 to 8 hrs by fluorescence polarization assayMore data for this Ligand-Target Pair
Affinity DataEC50: 420nMAssay Description:Antagonist activity at full length human androgen receptor expressed in mammalian expression system measured after 22 to 24 hrs by luciferase reporte...More data for this Ligand-Target Pair
Affinity DataIC50: 1.26E+3nMAssay Description:Antagonist activity at androgen receptor (unknown origin) expressed in African green monkey COS7 cells assessed as inhibition of R1881-induced protei...More data for this Ligand-Target Pair
Affinity DataIC50: 50nMAssay Description:Inhibition of full length AR transcriptional activity in human LNCAP cells harboring AR2PB-eGFP construct assessed as reduction in R1881-induced secr...More data for this Ligand-Target Pair
Affinity DataIC50: 90nMAssay Description:Inhibition of R1881-induced full length AR transcriptional activity in human LNCAP cells harboring AR2PB-eGFP construct after 72 hrs by fluorescence ...More data for this Ligand-Target Pair
Affinity DataIC50: 1.32E+3nMAssay Description:Displacement of fluormone-AL Green from His-tagged/GST-fused recombinant rat androgen receptor LBD expressed in insect cells measured after 4 hrs by ...More data for this Ligand-Target Pair
Affinity DataEC50: 180nMAssay Description:Inhibition of DHT-induced androgen receptor transactivation in human LNCaP cells after 24 hrs by luciferase reporter gene assay relative to controlMore data for this Ligand-Target Pair
Affinity DataIC50: 5.34E+3nMAssay Description:Competitive displacement of [3H]R1881 from human AR-LBD expressed in LNCaP cells incubated for 24 hrs by scintillation counting method based radiolig...More data for this Ligand-Target Pair
Affinity DataEC50: 1.10E+3nMAssay Description:Antagonist activity at androgen receptor in human C4-2-PSA-rl cells incubated for 24 hrs in presence of androgen R1881 by dual-glo luciferase reporte...More data for this Ligand-Target Pair
Affinity DataIC50: 361nMAssay Description:Antagonist activity at rat androgen receptor fused with DNA-binding domain of GAL4 expressed in AR-UAS-bla GripTite 293 cells assessed as inhibition ...More data for this Ligand-Target Pair
Affinity DataIC50: 1.32E+3nMAssay Description:Displacement of fluormone-AL Green from His-tagged/GST-fused recombinant rat androgen receptor LBD expressed in insect cells measured after 4 hrs by ...More data for this Ligand-Target Pair
Affinity DataIC50: 8.61E+3nMpH: 7.5Assay Description:An AR-response element is contained within the mmTV sequence and drives the expression of luciferase. The effect of antiandrogens (competitive antago...More data for this Ligand-Target Pair
Affinity DataIC50: 1.94E+3nMpH: 7.5Assay Description:Briefly, the AR LBD is expressed as a fusion with the Gal4 transcription factor, which binds to the Gal4 reporter DNA. Upon activation with agonist h...More data for this Ligand-Target Pair
Affinity DataIC50: 216nMAssay Description:Antagonist activity at human androgen receptor expressed in HEK293 cells assessed as inhibition of R1881-induced receptor transactivation after 24 hr...More data for this Ligand-Target Pair
Affinity DataIC50: 216nMAssay Description:Antagonist activity at human androgen receptor expressed in HEK293 cells assessed as inhibition of R1881-induced receptor transactivation after 24 hr...More data for this Ligand-Target Pair
Affinity DataIC50: 216nMAssay Description:Methods: hAR-LBD (633-919) was cloned into pGex4t.1. Large scale GST-tagged AR-LBD was prepared and purified using a GST column. Recombinant AR-LBD w...More data for this Ligand-Target Pair
Affinity DataIC50: 3.03E+3nMAssay Description:Antagonist activity at Androgen receptor (unknown origin) expressed in COS7 cells by dual luciferase reporter gene assay relative to controlMore data for this Ligand-Target Pair