Compile Data Set for Download or QSAR
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Found 59 Enz. Inhib. hit(s) for PDB: 1T63
TargetAndrogen receptor(Homo sapiens (Human))
Ligand Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM18161((1S,2S,7S,10R,11S,14S,15S)-14-hydroxy-2,15-dimethy...)
Affinity DataKi:  0.200nMAssay 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))
Ligand Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM18161((1S,2S,7S,10R,11S,14S,15S)-14-hydroxy-2,15-dimethy...)
Affinity DataKi:  0.200nM ΔG°:  -57.6kJ/mole EC50:  5.10nMpH: 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))
Ligand Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM18161((1S,2S,7S,10R,11S,14S,15S)-14-hydroxy-2,15-dimethy...)
Affinity DataKi:  0.200nM EC50:  5.10nMAssay 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))
Ligand Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM18161((1S,2S,7S,10R,11S,14S,15S)-14-hydroxy-2,15-dimethy...)
Affinity DataKi:  0.200nM ΔG°:  -57.6kJ/mole EC50:  5.10nMpH: 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(Rattus norvegicus (Rat))
The Ohio State University

LigandPNGBDBM18161((1S,2S,7S,10R,11S,14S,15S)-14-hydroxy-2,15-dimethy...)
Affinity DataKi:  0.270nM ΔG°:  -50.8kJ/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

LigandPNGBDBM18161((1S,2S,7S,10R,11S,14S,15S)-14-hydroxy-2,15-dimethy...)
Affinity DataKi:  0.280nM ΔG°:  -50.7kJ/mole EC50:  1nMpH: 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

LigandPNGBDBM18161((1S,2S,7S,10R,11S,14S,15S)-14-hydroxy-2,15-dimethy...)
Affinity DataKi:  0.282nMAssay Description:Inhibition of [3H]mibolerone binding to cytosolic androgen receptor of rat ventral prostateMore data for this Ligand-Target Pair
TargetAndrogen receptor(Homo sapiens (Human))
Ligand Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM18161((1S,2S,7S,10R,11S,14S,15S)-14-hydroxy-2,15-dimethy...)
Affinity DataKi:  0.300nM ΔG°:  -53.8kJ/mole EC50:  2.80nMpH: 7.4 T: 2°CAssay Description:Receptor Binding Assay (Ki)-Binding determined through direct displacement of ligand with [3H]-DHT in the MDA-453 cell line. Transactivation Assay (E...More data for this Ligand-Target Pair
TargetAndrogen receptor(Homo sapiens (Human))
Ligand Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM18161((1S,2S,7S,10R,11S,14S,15S)-14-hydroxy-2,15-dimethy...)
Affinity DataKi:  0.300nM ΔG°:  -56.5kJ/mole EC50:  5.70nMpH: 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(Rattus norvegicus (Rat))
The Ohio State University

LigandPNGBDBM18161((1S,2S,7S,10R,11S,14S,15S)-14-hydroxy-2,15-dimethy...)
Affinity DataKi:  0.430nM ΔG°:  -49.7kJ/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

LigandPNGBDBM18161((1S,2S,7S,10R,11S,14S,15S)-14-hydroxy-2,15-dimethy...)
Affinity DataKi:  0.690nMAssay Description:Inhibitory constant against rat prostate cytosol androgen receptor using [3H]miboleroneMore data for this Ligand-Target Pair
TargetAndrogen receptor(Homo sapiens (Human))
Ligand Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM18161((1S,2S,7S,10R,11S,14S,15S)-14-hydroxy-2,15-dimethy...)
Affinity DataKi:  0.900nMAssay 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))
Ligand Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM18161((1S,2S,7S,10R,11S,14S,15S)-14-hydroxy-2,15-dimethy...)
Affinity DataKi:  2nMAssay Description:Binding affinity towards human androgen receptor (hAR), using dihydrotestosterone as radioligand for competitive binding assayMore data for this Ligand-Target Pair
TargetAndrogen receptor(Homo sapiens (Human))
Ligand Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM18161((1S,2S,7S,10R,11S,14S,15S)-14-hydroxy-2,15-dimethy...)
Affinity DataKi:  2nMAssay Description:Agonist activity to the human androgen receptor (hAR) in CV-1 cellsMore data for this Ligand-Target Pair
TargetAndrogen receptor(Homo sapiens (Human))
Ligand Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM18161((1S,2S,7S,10R,11S,14S,15S)-14-hydroxy-2,15-dimethy...)
Affinity DataKi:  2nMAssay Description:Binding affinity against Androgen receptor expressed COS cellsMore data for this Ligand-Target Pair
TargetAndrogen receptor(Homo sapiens (Human))
Ligand Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM18161((1S,2S,7S,10R,11S,14S,15S)-14-hydroxy-2,15-dimethy...)
Affinity DataKi:  3nMAssay Description:Transcriptional repression in HepG2 cells expressing human glucocorticoid receptorMore data for this Ligand-Target Pair
TargetAndrogen receptor(Homo sapiens (Human))
Ligand Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM18161((1S,2S,7S,10R,11S,14S,15S)-14-hydroxy-2,15-dimethy...)
Affinity DataKi:  4.70nMAssay Description:Displacement of [3H]DHT from human androgen receptor after 16 hrs by scintillation countingMore data for this Ligand-Target Pair
TargetAndrogen receptor(Homo sapiens (Human))
Ligand Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM18161((1S,2S,7S,10R,11S,14S,15S)-14-hydroxy-2,15-dimethy...)
Affinity DataKi:  10nMAssay Description:Displacement of fluorescent-tagged R1881 from androgen receptor after 4 hrs by fluorometric assayMore data for this Ligand-Target Pair
TargetAndrogen receptor(Homo sapiens (Human))
Ligand Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM18161((1S,2S,7S,10R,11S,14S,15S)-14-hydroxy-2,15-dimethy...)
Affinity DataIC50:  0.0500nMAssay Description:Binding affinity towards human glucocorticoid receptor (GR) was determined using [3H]-Dexamethasone as radioligand in SF-1 cellsMore data for this Ligand-Target Pair
TargetAndrogen receptor(Homo sapiens (Human))
Ligand Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM18161((1S,2S,7S,10R,11S,14S,15S)-14-hydroxy-2,15-dimethy...)
Affinity DataIC50:  0.0500nMAssay Description:Activity at androgen receptor in human Saos2 cells assessed as IL6 repressionMore data for this Ligand-Target Pair
TargetAndrogen receptor(Homo sapiens (Human))
Ligand Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM18161((1S,2S,7S,10R,11S,14S,15S)-14-hydroxy-2,15-dimethy...)
Affinity DataIC50:  0.670nMAssay Description:Displacement of [3H]mibolerone from human AR after 3 hrsMore data for this Ligand-Target Pair
TargetAndrogen receptor(Homo sapiens (Human))
Ligand Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM18161((1S,2S,7S,10R,11S,14S,15S)-14-hydroxy-2,15-dimethy...)
Affinity DataIC50:  1nMAssay Description:Displacement of [3H]methyltrienolone from androgen receptor in human MDA-MB-453 cellsMore data for this Ligand-Target Pair
TargetAndrogen receptor(Mus musculus)
Chonnam National University

Curated by ChEMBL
LigandPNGBDBM18161((1S,2S,7S,10R,11S,14S,15S)-14-hydroxy-2,15-dimethy...)
Affinity DataIC50:  1nMAssay Description:Displacement of [3H] ]5alpha-DHT from mouse androgen receptor expressed in monkey COS7 cells after 2 hrs by scintillation counting analysisMore data for this Ligand-Target Pair
TargetAndrogen receptor(Homo sapiens (Human))
Ligand Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM18161((1S,2S,7S,10R,11S,14S,15S)-14-hydroxy-2,15-dimethy...)
Affinity DataIC50:  1.82nMAssay Description:Activity against human androgen receptor expressed in HepG2 cells assessed as luciferase reporter gene activationMore data for this Ligand-Target Pair
TargetAndrogen receptor(Rattus norvegicus (Rat))
The Ohio State University

LigandPNGBDBM18161((1S,2S,7S,10R,11S,14S,15S)-14-hydroxy-2,15-dimethy...)
Affinity DataIC50:  2nMAssay 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))
Ligand Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM18161((1S,2S,7S,10R,11S,14S,15S)-14-hydroxy-2,15-dimethy...)
Affinity DataIC50:  2.10nMAssay 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(Homo sapiens (Human))
Ligand Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM18161((1S,2S,7S,10R,11S,14S,15S)-14-hydroxy-2,15-dimethy...)
Affinity DataIC50:  2.10nMAssay Description:Inhibition of wild type Androgen receptor (unknown origin) expressed in Freestyle293F cellsMore data for this Ligand-Target Pair
TargetAndrogen receptor(Rattus norvegicus (Rat))
The Ohio State University

LigandPNGBDBM18161((1S,2S,7S,10R,11S,14S,15S)-14-hydroxy-2,15-dimethy...)
Affinity DataIC50:  2.20nMAssay Description:In vitro antagonist activity against rat prostatic androgen receptor (AR)More data for this Ligand-Target Pair
TargetAndrogen receptor(Rattus norvegicus (Rat))
The Ohio State University

LigandPNGBDBM18161((1S,2S,7S,10R,11S,14S,15S)-14-hydroxy-2,15-dimethy...)
Affinity DataIC50:  3.10nMAssay Description:Displacement of [3H]testosterone from Sprague-Dawley rat AR by liquid scintillation countingMore data for this Ligand-Target Pair
TargetAndrogen receptor(Rattus norvegicus (Rat))
The Ohio State University

LigandPNGBDBM18161((1S,2S,7S,10R,11S,14S,15S)-14-hydroxy-2,15-dimethy...)
Affinity DataIC50:  3.10nMAssay Description:Competitive binding affinity to rat androgen receptorChecked by AuthorMore data for this Ligand-Target Pair
TargetAndrogen receptor(Homo sapiens (Human))
Ligand Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM18161((1S,2S,7S,10R,11S,14S,15S)-14-hydroxy-2,15-dimethy...)
Affinity DataIC50:  4nMAssay Description:In vitro agonistic activity against human androgen receptor using cotransfection assay in CV-1 cells.More data for this Ligand-Target Pair
TargetAndrogen receptor(Homo sapiens (Human))
Ligand Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM18161((1S,2S,7S,10R,11S,14S,15S)-14-hydroxy-2,15-dimethy...)
Affinity DataIC50:  10nMAssay Description:Binding affinity to androgen receptor by fluorescence binding assayMore data for this Ligand-Target Pair
TargetAndrogen receptor(Homo sapiens (Human))
Ligand Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM18161((1S,2S,7S,10R,11S,14S,15S)-14-hydroxy-2,15-dimethy...)
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(Homo sapiens (Human))
Ligand Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM18161((1S,2S,7S,10R,11S,14S,15S)-14-hydroxy-2,15-dimethy...)
Affinity DataIC50:  13nMAssay Description:Competitive inhibition of androgen binding to androgen receptor (unknown origin) by invitrogen polar screen assayMore data for this Ligand-Target Pair
TargetAndrogen receptor(Rattus norvegicus (Rat))
The Ohio State University

LigandPNGBDBM18161((1S,2S,7S,10R,11S,14S,15S)-14-hydroxy-2,15-dimethy...)
Affinity DataIC50:  18.5nMAssay Description:Displacement of androgen fluormone from rat androgen receptorMore data for this Ligand-Target Pair
TargetAndrogen receptor(Rattus norvegicus (Rat))
The Ohio State University

LigandPNGBDBM18161((1S,2S,7S,10R,11S,14S,15S)-14-hydroxy-2,15-dimethy...)
Affinity DataIC50:  3.20E+3nMAssay Description:Ability to inhibit binding of [3H]R-1881 to rat ventral prostrate cytosolic androgen receptor was measured in a radioligand binding assay.More data for this Ligand-Target Pair
TargetAndrogen receptor(Homo sapiens (Human))
Ligand Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM18161((1S,2S,7S,10R,11S,14S,15S)-14-hydroxy-2,15-dimethy...)
Affinity DataIC50: >1.00E+4nMAssay 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))
Ligand Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM18161((1S,2S,7S,10R,11S,14S,15S)-14-hydroxy-2,15-dimethy...)
Affinity DataIC50: >1.00E+4nMAssay Description:Antagonistic activity against human androgen receptor (hAR) in CV-1 cells using cotransfection assayMore data for this Ligand-Target Pair
TargetAndrogen receptor(Homo sapiens (Human))
Ligand Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM18161((1S,2S,7S,10R,11S,14S,15S)-14-hydroxy-2,15-dimethy...)
Affinity DataIC50: >1.00E+4nMAssay Description:Antagonist activity at human androgen receptor expressed in CV1 cells by transcriptional activation assayMore data for this Ligand-Target Pair
TargetAndrogen receptor(Homo sapiens (Human))
Ligand Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM18161((1S,2S,7S,10R,11S,14S,15S)-14-hydroxy-2,15-dimethy...)
Affinity DataIC50: >1.00E+4nMAssay Description:Antagonist activity at human androgen receptor expressed in COS7 cells assessed as inhibition of DHT-induced luciferase activity after 24 hrs by repo...More data for this Ligand-Target Pair
TargetAndrogen receptor(Homo sapiens (Human))
Ligand Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM18161((1S,2S,7S,10R,11S,14S,15S)-14-hydroxy-2,15-dimethy...)
Affinity DataIC50: >1.00E+4nMAssay Description:Agonistic activity against human androgen receptor (hAR) expressed in CV-1 cell linesMore data for this Ligand-Target Pair
TargetAndrogen receptor(Homo sapiens (Human))
Ligand Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM18161((1S,2S,7S,10R,11S,14S,15S)-14-hydroxy-2,15-dimethy...)
Affinity DataIC50: >1.00E+4nMAssay Description:Antagonist activity at wild type Androgen receptor (unknown origin) expressed in human Cos-7 cells co-expressing pGL3-MMTV-luc vector assessed as luc...More data for this Ligand-Target Pair
TargetAndrogen receptor(Homo sapiens (Human))
Ligand Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM18161((1S,2S,7S,10R,11S,14S,15S)-14-hydroxy-2,15-dimethy...)
Affinity DataEC50:  6nMAssay Description:In vitro agonistic activity against human androgen receptor using cotransfection assay in CV-1 cells.More data for this Ligand-Target Pair
TargetAndrogen receptor(Homo sapiens (Human))
Ligand Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM18161((1S,2S,7S,10R,11S,14S,15S)-14-hydroxy-2,15-dimethy...)
Affinity DataEC50:  5.10nMAssay Description:Agonist activity at human androgen receptor african green monkey CV1 cells by cotransfection assayMore data for this Ligand-Target Pair
TargetAndrogen receptor(Homo sapiens (Human))
Ligand Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM18161((1S,2S,7S,10R,11S,14S,15S)-14-hydroxy-2,15-dimethy...)
Affinity DataEC50:  20nMAssay Description:Agonist activity at androgen receptor ligand binding domain expressed in african green monkey COS7 cells co-transfected with Gal4-DBD by luciferase r...More data for this Ligand-Target Pair
TargetAndrogen receptor(Homo sapiens (Human))
Ligand Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM18161((1S,2S,7S,10R,11S,14S,15S)-14-hydroxy-2,15-dimethy...)
Affinity DataEC50:  5.70nMAssay Description:Agonist activity at human androgen receptor in CV1 cells by transcriptional activation assayMore data for this Ligand-Target Pair
TargetAndrogen receptor(Rattus norvegicus (Rat))
The Ohio State University

LigandPNGBDBM18161((1S,2S,7S,10R,11S,14S,15S)-14-hydroxy-2,15-dimethy...)
Affinity DataEC50:  0.970nMAssay Description:Agonist activity at rat androgen receptorChecked by AuthorMore data for this Ligand-Target Pair
TargetAndrogen receptor(Mus musculus)
Chonnam National University

Curated by ChEMBL
LigandPNGBDBM18161((1S,2S,7S,10R,11S,14S,15S)-14-hydroxy-2,15-dimethy...)
Affinity DataEC50:  3.98nMAssay Description:Agonist activity at androgen receptor in mouse NIH3T3 cells transiently transfected with beta-galactosidase reporter gene assessed as cellular transf...More data for this Ligand-Target Pair
TargetAndrogen receptor(Homo sapiens (Human))
Ligand Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM18161((1S,2S,7S,10R,11S,14S,15S)-14-hydroxy-2,15-dimethy...)
Affinity DataEC50:  0.0500nMAssay Description:Agonist activity at androgen receptor expressed in mouse C2C12 cells assessed as osteoblast differentiation after 5 daysMore data for this Ligand-Target Pair
TargetAndrogen receptor(Homo sapiens (Human))
Ligand Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM18161((1S,2S,7S,10R,11S,14S,15S)-14-hydroxy-2,15-dimethy...)
Affinity DataEC50:  2nMAssay Description:Agonist activity at androgen receptor in human MDA-MB-453 cells transfected with MMTV-LUC assessed as induction of MMTV-LTR/promoter linked LUC gene ...More data for this Ligand-Target Pair
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