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 67 hits for monomerid = 50425732
Affinity DataKi: 17nMAssay Description:Binding affinity to wild-type androgen receptor in human LNCaP cells assessed as inhibition constant incubated for 24 hrs by Cheng-Prusoff equation a...More data for this Ligand-Target Pair
Affinity DataKi: 28nMAssay Description:Antagonist activity at androgen receptor (unknown origin)More data for this Ligand-Target Pair
Affinity DataKi: 86nMAssay Description:Inhibition of androgen receptor (unknown origin)More data for this Ligand-Target Pair
Affinity DataKi: 1.35E+3nM IC50: 2.03E+3nMAssay Description:A series of dilutions of the compounds were prepared with 10% DMSO in HDAC assay buffer, and 5uL of the dilution was added to a 50uL reaction so that...More data for this Ligand-Target Pair
Affinity DataKi: 2.75E+3nMAssay 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
TargetAndrogen receptor(Rattus norvegicus (Rat))
University Of Tennessee Health Science Center
Curated by ChEMBL
University Of Tennessee Health Science Center
Curated by ChEMBL
Affinity DataKi: 3.64E+3nMAssay Description:Displacement of [3H]-MIB from wild-type rat AR LBD measured after 16 hrs by scintillation counting methodMore data for this Ligand-Target Pair
TargetAndrogen receptor [633-919](Homo sapiens (Human))
University Of Tennessee Research Foundation
US Patent
University Of Tennessee Research Foundation
US Patent
Affinity DataKi: 3.64E+3nMAssay 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 DataKi: 3.64E+3nMAssay Description:Displacement of [3H]-mibolerone from GST-tagged human AR-LBD expressed in HEK293 cellsMore data for this Ligand-Target Pair
Affinity DataKi: 3.64E+3nMAssay Description:Displacement of [3H]-mibolerone from recombinant wild-type GST-tagged androgen receptor LBD (unknown origin) after 16 hrs by scintillation counting a...More data for this Ligand-Target Pair
TargetAndrogen receptor [633-919](Homo sapiens (Human))
University Of Tennessee Research Foundation
US Patent
University Of Tennessee Research Foundation
US Patent
Affinity DataKi: 3.64E+3nMAssay Description: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 was combin...More data for this Ligand-Target Pair
TargetAndrogen receptor(Rattus norvegicus (Rat))
University Of Tennessee Health Science Center
Curated by ChEMBL
University Of Tennessee Health Science Center
Curated by ChEMBL
Affinity DataKi: 3.64E+3nMAssay Description:Inhibition of [3H] MIB binding to rat prostate androgen receptor LBD by competitive binding assayMore data for this Ligand-Target Pair
Affinity DataKi: 3.64E+3nMAssay 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 DataKi: 3.64E+3nMAssay Description:Displacement of [3H]-mibolerone from recombinant wild-type GST-tagged androgen receptor LBD (unknown origin) after 16 hrs by scintillation counting a...More data for this Ligand-Target Pair
TargetGlucocorticoid receptor(Homo sapiens (Human))
Janssen Research And Development
Curated by ChEMBL
Janssen Research And Development
Curated by ChEMBL
Affinity DataKi: 1.40E+4nMAssay Description:Binding affinity to glucocorticoid receptor in human IM-9 cells assessed as inhibition constant incubated for 6 hrs by Cheng-Prusoff equation analysi...More data for this Ligand-Target Pair
Affinity DataIC50: 361nMAssay Description:Antagonist activity at GAL4 DBD-fused androgen receptor LBD (unknown origin) transfected in UAS-bla GripTite 293 cells assessed as inhibition of R188...More data for this Ligand-Target Pair
Affinity DataIC50: 5.60E+3nMAssay Description:Displacement of Fluormone AL Green from androgen receptor ligand binding domain (unknown origin) after 4 hrs by fluorescence polarization assayMore data for this Ligand-Target Pair
Affinity DataEC50: 49nMAssay Description:Displacement of [3H]R1881 from AR in human MDA-MB-453 cellsMore data for this Ligand-Target Pair
Affinity DataEC50: 915nMAssay Description:Displacement of [3H]R1881 from AR in human LNCaP cells after 2 hrs by scintillation counting analysisMore data for this Ligand-Target Pair
Affinity DataIC50: >1.00E+5nMAssay Description:Inhibition of BF3 site of androgen receptor in enzalutamide-resistant human LNCAP cells assessed as reduction in PSA level after 3 daysMore data for this Ligand-Target Pair
Affinity DataIC50: 21nMAssay Description:Displacement of [18F]-FDHT from androgen receptor in human LNCAP/AR cellsMore data for this Ligand-Target Pair
TargetAndrogen receptor(Rattus norvegicus (Rat))
University Of Tennessee Health Science Center
Curated by ChEMBL
University Of Tennessee Health Science Center
Curated by ChEMBL
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 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: 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 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
TargetAndrogen receptor(Rattus norvegicus (Rat))
University Of Tennessee Health Science Center
Curated by ChEMBL
University Of Tennessee Health Science Center
Curated by ChEMBL
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
TargetAndrogen receptor(Rattus norvegicus (Rat))
University Of Tennessee Health Science Center
Curated by ChEMBL
University Of Tennessee Health Science Center
Curated by ChEMBL
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
TargetAndrogen receptor(Rattus norvegicus (Rat))
University Of Tennessee Health Science Center
Curated by ChEMBL
University Of Tennessee Health Science Center
Curated by ChEMBL
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: 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
Affinity DataIC50: 216nMAssay Description:Antagonist activity at recombinant human AR expressed in HEK293 cells assessed as inhibition of R1881-induced transcriptional activity measured after...More data for this Ligand-Target Pair
Affinity DataIC50: 3.97E+3nMAssay Description:Displacement of fluormone-AL green from GST-tagged androgen receptor LBD (unknown origin) measured after 4 hrs by fluorescence polarization assayMore data for this Ligand-Target Pair
Affinity DataIC50: 36nMAssay Description:Antagonist activity at androgen receptor in human LNCaP cells transfected with ARR2 PB-eGFP assessed as inhibition of DHT-induced transcriptional act...More data for this Ligand-Target Pair
Affinity DataIC50: 130nMAssay Description:Inhibition of prostate specific antigen in human LNCaP cellsMore 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: 219nMAssay Description:Inhibition of androgen receptor (unknown origin)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
TargetGlucocorticoid receptor(Homo sapiens (Human))
Janssen Research And Development
Curated by ChEMBL
Janssen Research And Development
Curated by ChEMBL
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 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: 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 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 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: 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