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Found 83 Enz. Inhib. hit(s) for PDB: 4OKB
TargetAndrogen receptor(Rattus norvegicus (Rat))
The Ohio State University

LigandPNGBDBM18678((2R)-N-[4-cyano-3-(trifluoromethyl)phenyl]-3-[(4-f...)
Affinity DataKi:  11nM ΔG°:  -42.2kJ/molepH: 7.4 T: 2°CAssay Description:The Ki values were determined by the application of the Cheng-Prusoff equation: Ki = (IC50 x Kd)/(Kd+[L]) where [L] is the concentration of [3H]MIB (...More data for this Ligand-Target Pair
TargetAndrogen receptor(Rattus norvegicus (Rat))
The Ohio State University

LigandPNGBDBM18678((2R)-N-[4-cyano-3-(trifluoromethyl)phenyl]-3-[(4-f...)
Affinity DataKi:  11nMAssay Description:Inhibition of [3H]mibolerone binding to cytosolic androgen receptor of rat ventral prostateMore data for this Ligand-Target Pair
TargetAndrogen receptor(Rattus norvegicus (Rat))
The Ohio State University

LigandPNGBDBM18678((2R)-N-[4-cyano-3-(trifluoromethyl)phenyl]-3-[(4-f...)
Affinity DataKi:  11nM ΔG°:  -42.2kJ/molepH: 7.4 T: 2°CAssay Description:The Ki values were determined by the application of the Cheng-Prusoff equation: Ki = (IC50 x Kd)/(Kd+[L]) where [L] is the concentration of [3H]MIB (...More data for this Ligand-Target Pair
TargetAndrogen receptor(Rattus norvegicus (Rat))
The Ohio State University

LigandPNGBDBM18678((2R)-N-[4-cyano-3-(trifluoromethyl)phenyl]-3-[(4-f...)
Affinity DataKi:  11nM ΔG°:  -42.2kJ/molepH: 7.4 T: 2°CAssay Description:The Ki values were determined by the application of the Cheng-Prusoff equation: Ki = (IC50 x Kd)/(Kd+[L]) where [L] is the concentration of [3H]MIB (...More data for this Ligand-Target Pair
TargetAndrogen receptor(Rattus norvegicus (Rat))
The Ohio State University

LigandPNGBDBM18678((2R)-N-[4-cyano-3-(trifluoromethyl)phenyl]-3-[(4-f...)
Affinity DataKi:  11nM ΔG°:  -42.2kJ/mole EC50:  1.00E+3nMpH: 7.4 T: 2°CAssay Description:The Ki values were determined by the application of the Cheng-Prusoff equation: Ki = (IC50 x Kd)/(Kd+[L]) where [L] is the concentration of [3H]MIB (...More data for this Ligand-Target Pair
TargetAndrogen receptor(Rattus norvegicus (Rat))
The Ohio State University

LigandPNGBDBM18525(Bicalutamide | CHEMBL409 | N-[4-cyano-3-(trifluoro...)
Affinity DataKi:  14nMAssay Description:The Ki values were determined by the application of the Cheng-Prusoff equation: Ki=IC50/(1+[L]/Kd] where [L] is the concentration of labeled ligand a...More data for this Ligand-Target Pair
TargetAndrogen receptor(Homo sapiens (Human))
Astellas Pharma

LigandPNGBDBM18525(Bicalutamide | CHEMBL409 | N-[4-cyano-3-(trifluoro...)
Affinity DataKi:  19nMAssay Description:The Ki values were determined by the application of the Cheng-Prusoff equation: Ki=IC50/(1+[L]/Kd] where [L] is the concentration of labeled ligand a...More data for this Ligand-Target Pair
TargetAndrogen receptor(Homo sapiens (Human))
Astellas Pharma

LigandPNGBDBM18525(Bicalutamide | CHEMBL409 | N-[4-cyano-3-(trifluoro...)
Affinity DataKi:  35nMAssay Description:Binding affinity for mutant T877A Androgen receptor in human LNCaP cellsMore data for this Ligand-Target Pair
TargetAndrogen receptor(Homo sapiens (Human))
Astellas Pharma

LigandPNGBDBM18525(Bicalutamide | CHEMBL409 | N-[4-cyano-3-(trifluoro...)
Affinity DataKi:  35nMAssay Description:Inhibition of [3H]-DHT binding to T877A androgen receptor of LNCaP cellsMore data for this Ligand-Target Pair
TargetAndrogen receptor(Homo sapiens (Human))
Astellas Pharma

LigandPNGBDBM18525(Bicalutamide | CHEMBL409 | N-[4-cyano-3-(trifluoro...)
Affinity DataKi:  64nMAssay Description:Displacement of [3H]DHT from AR in human MDA-MB-453 cellsMore data for this Ligand-Target Pair
TargetAndrogen receptor(Homo sapiens (Human))
Astellas Pharma

LigandPNGBDBM18525(Bicalutamide | CHEMBL409 | N-[4-cyano-3-(trifluoro...)
Affinity DataKi:  64nMAssay Description:Displacement of [3H]-DHT from androgen receptor in human MDA-MB-453 cells after 90 mins by TopCount analysisMore data for this Ligand-Target Pair
TargetAndrogen receptor(Homo sapiens (Human))
Astellas Pharma

LigandPNGBDBM18525(Bicalutamide | CHEMBL409 | N-[4-cyano-3-(trifluoro...)
Affinity DataKi:  64nMAssay Description:Binding affinity for androgen receptor in human MDA-453 cellsMore data for this Ligand-Target Pair
TargetAndrogen receptor(Homo sapiens (Human))
Astellas Pharma

LigandPNGBDBM18525(Bicalutamide | CHEMBL409 | N-[4-cyano-3-(trifluoro...)
Affinity DataKi:  64nMAssay Description:Inhibition of [3H]-DHT binding to androgen receptor of MDA-453 cellsMore data for this Ligand-Target Pair
TargetAndrogen receptor(Homo sapiens (Human))
Astellas Pharma

LigandPNGBDBM18525(Bicalutamide | CHEMBL409 | N-[4-cyano-3-(trifluoro...)
Affinity DataKi:  64nMAssay Description:Displacement of [3H]DHT from human androgen receptor in MDA453 cellsMore data for this Ligand-Target Pair
TargetAndrogen receptor(Homo sapiens (Human))
Astellas Pharma

LigandPNGBDBM18525(Bicalutamide | CHEMBL409 | N-[4-cyano-3-(trifluoro...)
Affinity DataKi:  65nMAssay Description:Displacement of [3H]-DHT from androgen receptor of human MDA-453 cellsMore data for this Ligand-Target Pair
TargetAndrogen receptor(Homo sapiens (Human))
Astellas Pharma

LigandPNGBDBM18525(Bicalutamide | CHEMBL409 | N-[4-cyano-3-(trifluoro...)
Affinity DataKi:  70nM ΔG°:  -42.5kJ/mole IC50:  128nMpH: 7.4 T: 2°CAssay Description:The compounds were evaluated in a transcriptional activation assay with hAR in a mammalian cell background (CV-1) as the primary in vitro assay. Rece...More data for this Ligand-Target Pair
TargetAndrogen receptor(Homo sapiens (Human))
Astellas Pharma

LigandPNGBDBM18525(Bicalutamide | CHEMBL409 | N-[4-cyano-3-(trifluoro...)
Affinity DataKi:  82nMAssay Description:Binding affinity against Androgen receptor transfected into COS cellsMore data for this Ligand-Target Pair
TargetAndrogen receptor(Homo sapiens (Human))
Astellas Pharma

LigandPNGBDBM18525(Bicalutamide | CHEMBL409 | N-[4-cyano-3-(trifluoro...)
Affinity DataKi:  117nMAssay Description:Binding affinity for human androgen receptor transfected into mammalian COS-1 cellsMore data for this Ligand-Target Pair
TargetAndrogen receptor(Homo sapiens (Human))
Astellas Pharma

LigandPNGBDBM18525(Bicalutamide | CHEMBL409 | N-[4-cyano-3-(trifluoro...)
Affinity DataKi:  117nMAssay Description:Binding affinity for human androgen receptor in transiently-transfected COS-1 cells.More data for this Ligand-Target Pair
TargetAndrogen receptor(Homo sapiens (Human))
Astellas Pharma

LigandPNGBDBM18525(Bicalutamide | CHEMBL409 | N-[4-cyano-3-(trifluoro...)
Affinity DataKi:  151nM IC50:  162nMAssay Description:The compounds were evaluated in a transcriptional activation assay with hAR in a mammalian cell background (CV-1) as the primary in vitro assay. Rece...More data for this Ligand-Target Pair
TargetAndrogen receptor(Homo sapiens (Human))
Astellas Pharma

LigandPNGBDBM18525(Bicalutamide | CHEMBL409 | N-[4-cyano-3-(trifluoro...)
Affinity DataKi:  151nMAssay Description:Displacement of [3H]DHT from human Androgen receptor in human MDA-MB-453 cellsMore data for this Ligand-Target Pair
TargetAndrogen receptor(Homo sapiens (Human))
Astellas Pharma

LigandPNGBDBM18525(Bicalutamide | CHEMBL409 | N-[4-cyano-3-(trifluoro...)
Affinity DataKi:  151nMAssay Description:Binding affinity to human androgen receptor expressed in monkey COS7 cells by whole cell binding assayMore data for this Ligand-Target Pair
TargetAndrogen receptor(Homo sapiens (Human))
Astellas Pharma

LigandPNGBDBM18525(Bicalutamide | CHEMBL409 | N-[4-cyano-3-(trifluoro...)
Affinity DataKi:  160nMAssay Description:Antagonist activity at androgen receptor (unknown origin)More data for this Ligand-Target Pair
TargetAndrogen receptor(Rattus norvegicus (Rat))
The Ohio State University

LigandPNGBDBM18525(Bicalutamide | CHEMBL409 | N-[4-cyano-3-(trifluoro...)
Affinity DataKi:  330nMAssay Description:In vivo binding affinity for rat ventral prostate androgen receptor by displacement of [3H]R-1881More data for this Ligand-Target Pair
TargetAndrogen receptor(Homo sapiens (Human))
Astellas Pharma

LigandPNGBDBM18525(Bicalutamide | CHEMBL409 | N-[4-cyano-3-(trifluoro...)
Affinity DataKi:  2.46E+3nM IC50:  3.69E+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
TargetAndrogen receptor(Homo sapiens (Human))
Astellas Pharma

LigandPNGBDBM18678((2R)-N-[4-cyano-3-(trifluoromethyl)phenyl]-3-[(4-f...)
Affinity DataKi:  3.70E+3nMAssay Description:Displacement of [3H]testosterone from wild type human androgen receptorMore data for this Ligand-Target Pair
TargetAndrogen receptor(Homo sapiens (Human))
Astellas Pharma

LigandPNGBDBM18525(Bicalutamide | CHEMBL409 | N-[4-cyano-3-(trifluoro...)
Affinity DataIC50: >10nMAssay Description:In vitro binding affinity at human androgen receptor transfected into COS cells.More data for this Ligand-Target Pair
TargetAndrogen receptor(Rattus norvegicus (Rat))
The Ohio State University

LigandPNGBDBM18525(Bicalutamide | CHEMBL409 | N-[4-cyano-3-(trifluoro...)
Affinity DataIC50:  25nMAssay Description:Displacement of [3H]testosterone from androgen receptor in Sprague-Dawley rat prostate gland after 2 hrs by liquid scintillation countingChecked by AuthorMore data for this Ligand-Target Pair
TargetAndrogen receptor(Homo sapiens (Human))
Astellas Pharma

LigandPNGBDBM18525(Bicalutamide | CHEMBL409 | N-[4-cyano-3-(trifluoro...)
Affinity DataIC50:  54nMAssay Description:Inhibition of wild type Androgen receptor (unknown origin) expressed in Freestyle293F cellsMore data for this Ligand-Target Pair
TargetAndrogen receptor(Homo sapiens (Human))
Astellas Pharma

LigandPNGBDBM18525(Bicalutamide | CHEMBL409 | N-[4-cyano-3-(trifluoro...)
Affinity DataIC50:  54nMAssay Description:Displacement of [17-alpha-methyl-3H]mibolerone from androgen receptor expressed in HEK293 cells after 3 hrsMore data for this Ligand-Target Pair
TargetAndrogen receptor(Homo sapiens (Human))
Astellas Pharma

LigandPNGBDBM18525(Bicalutamide | CHEMBL409 | N-[4-cyano-3-(trifluoro...)
Affinity DataIC50:  54nMAssay Description:Displacement of [17-alpha-methyl-3H]-mibolerone from human androgen receptor expressed in HEK293 derived FreeStyle293F cells after 3 hrsMore data for this Ligand-Target Pair
TargetAndrogen receptor(Rattus norvegicus (Rat))
The Ohio State University

LigandPNGBDBM18525(Bicalutamide | CHEMBL409 | N-[4-cyano-3-(trifluoro...)
Affinity DataIC50:  54nMAssay Description:Displacement of [3H]testosterone from Sprague-Dawley rat AR by liquid scintillation countingMore data for this Ligand-Target Pair
TargetAndrogen receptor(Homo sapiens (Human))
Astellas Pharma

LigandPNGBDBM18525(Bicalutamide | CHEMBL409 | N-[4-cyano-3-(trifluoro...)
Affinity DataIC50:  86.9nMAssay Description:Antagonist activity against pSG5-tagged human androgen receptor expressed in COS1 cells assessed as reduction in receptor-mediated transcriptional ac...More data for this Ligand-Target Pair
TargetAndrogen receptor(Homo sapiens (Human))
Astellas Pharma

LigandPNGBDBM18525(Bicalutamide | CHEMBL409 | N-[4-cyano-3-(trifluoro...)
Affinity DataIC50:  87nMAssay Description:Displacement of [3H]R1881 from pSG5-tagged human androgen receptor expressed in COS1 cells assessed as relative binding inhibitionMore data for this Ligand-Target Pair
TargetAndrogen receptor(Homo sapiens (Human))
Astellas Pharma

LigandPNGBDBM18525(Bicalutamide | CHEMBL409 | N-[4-cyano-3-(trifluoro...)
Affinity DataIC50:  117nMAssay Description:In vitro binding affinity at human androgen receptor transfected into COS cells.More data for this Ligand-Target Pair
TargetAndrogen receptor(Homo sapiens (Human))
Astellas Pharma

LigandPNGBDBM18678((2R)-N-[4-cyano-3-(trifluoromethyl)phenyl]-3-[(4-f...)
Affinity DataIC50:  120nMAssay Description:Displacement of [3H]R1881 from wild type human androgen receptor expressed in COS-1 cells co-transfected with pSG5 after 15 mins by scintillation ass...More data for this Ligand-Target Pair
TargetAndrogen receptor(Homo sapiens (Human))
Astellas Pharma

LigandPNGBDBM18525(Bicalutamide | CHEMBL409 | N-[4-cyano-3-(trifluoro...)
Affinity DataIC50:  140nMAssay Description:Antagonist activity at androgen receptor expressed in HeLa cells assessed as inhibition of dihydrotestosterone-induced transcriptional activity by re...More data for this Ligand-Target Pair
TargetAndrogen receptor(Homo sapiens (Human))
Astellas Pharma

LigandPNGBDBM18525(Bicalutamide | CHEMBL409 | N-[4-cyano-3-(trifluoro...)
Affinity DataIC50:  140nMAssay Description:Antagonist activity at human androgen receptor expressed in HeLa cells assessed as inhibition of dihydrotestosterone induced transcriptional activity...More data for this Ligand-Target Pair
TargetAndrogen receptor(Homo sapiens (Human))
Astellas Pharma

LigandPNGBDBM18525(Bicalutamide | CHEMBL409 | N-[4-cyano-3-(trifluoro...)
Affinity DataIC50:  157nMAssay Description:Antagonistic activity (IC50) against human androgen receptor (hAR) in cotransfected CV-1 cellMore data for this Ligand-Target Pair
TargetAndrogen receptor(Homo sapiens (Human))
Astellas Pharma

LigandPNGBDBM18525(Bicalutamide | CHEMBL409 | N-[4-cyano-3-(trifluoro...)
Affinity DataIC50:  157nMAssay Description:Antagonistic activity against human androgen receptor (hAR) in co-transfected CV-1 cells.More data for this Ligand-Target Pair
TargetAndrogen receptor(Homo sapiens (Human))
Astellas Pharma

LigandPNGBDBM18525(Bicalutamide | CHEMBL409 | N-[4-cyano-3-(trifluoro...)
Affinity DataIC50:  162nMAssay Description:Antagonist activity at human androgen receptor in CV1 cells by transcriptional activation assayMore data for this Ligand-Target Pair
TargetAndrogen receptor(Homo sapiens (Human))
Astellas Pharma

LigandPNGBDBM18525(Bicalutamide | CHEMBL409 | N-[4-cyano-3-(trifluoro...)
Affinity DataIC50:  162nMAssay Description:Antagonist activity at human androgen receptor african green monkey CV1 cells by cotransfection assayMore data for this Ligand-Target Pair
TargetAndrogen receptor(Homo sapiens (Human))
Astellas Pharma

LigandPNGBDBM18525(Bicalutamide | CHEMBL409 | N-[4-cyano-3-(trifluoro...)
Affinity DataIC50:  170nMAssay Description:In vitro antagonistic activity against androgen receptor of MDA-453 cellsMore data for this Ligand-Target Pair
TargetAndrogen receptor(Homo sapiens (Human))
Astellas Pharma

LigandPNGBDBM18525(Bicalutamide | CHEMBL409 | N-[4-cyano-3-(trifluoro...)
Affinity DataIC50:  173nMAssay Description:Antagonist activity at human androgen receptor in MDA453 cells by alkaline phosphatase reporter gene assayMore data for this Ligand-Target Pair
TargetAndrogen receptor(Homo sapiens (Human))
Astellas Pharma

LigandPNGBDBM18525(Bicalutamide | CHEMBL409 | N-[4-cyano-3-(trifluoro...)
Affinity DataIC50:  173nMAssay Description:Antagonist activity at androgen receptor in human MDA-MB-453 cells assessed as inhibition of DHT-induced PSA expression by alkaline phosphatase repor...More data for this Ligand-Target Pair
TargetAndrogen receptor(Homo sapiens (Human))
Astellas Pharma

LigandPNGBDBM18525(Bicalutamide | CHEMBL409 | N-[4-cyano-3-(trifluoro...)
Affinity DataIC50:  173nMAssay Description:Inhibition of androgen receptor in human MDA-453 cellsMore data for this Ligand-Target Pair
TargetAndrogen receptor(Homo sapiens (Human))
Astellas Pharma

LigandPNGBDBM18525(Bicalutamide | CHEMBL409 | N-[4-cyano-3-(trifluoro...)
Affinity DataIC50:  173nMAssay Description:Inhibition of human androgen receptor of breast carcinoma MDA-453 cells in reporter gene assayMore data for this Ligand-Target Pair
TargetAndrogen receptor(Homo sapiens (Human))
Astellas Pharma

LigandPNGBDBM18525(Bicalutamide | CHEMBL409 | N-[4-cyano-3-(trifluoro...)
Affinity DataIC50:  173nMAssay Description:Antagonist activity at human wild type AR expressed in human MDA-MB-435 cells by transactivation assayMore data for this Ligand-Target Pair
TargetAndrogen receptor(Mus musculus)
Endorecherche

US Patent
LigandPNGBDBM18525(Bicalutamide | CHEMBL409 | N-[4-cyano-3-(trifluoro...)
Affinity DataIC50:  190nMpH: 7.4 T: 2°CAssay Description:Androgen binding is measured using the hydroxylapatite (HAP) assay. In brief, the radioactive steroid [3H]R1881 solubilized in ethanol is diluted wit...More data for this Ligand-Target Pair
TargetAndrogen receptor(Homo sapiens (Human))
Astellas Pharma

LigandPNGBDBM18525(Bicalutamide | CHEMBL409 | N-[4-cyano-3-(trifluoro...)
Affinity DataIC50:  200nMAssay Description:Displacement of [3H]mibolerone from human androgen receptor expressed in CHOK1 cellsMore data for this Ligand-Target Pair
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