General Information of the Protein
Protein ID
PT00870
Protein Name
Glucocorticoid receptor
Secondarily
Protein Name
Nuclear receptor subfamily 3 group C member 1
Gene Name
NR3C1
Secondarily
Gene Name
Grl
Sequence
MDSKESLAPPGRDEVPGSLLGQGRGSVMDFYKSLRGGATVKVSASSPSVAAASQADSKQQRILLDFSKGSTSNVQQRQQQQQQQQQQQQQQQQQQQPDLSKAVSLSMGLYMGETETKVMGNDLGYPQQGQLGLSSGETDFRLLEESIANLNRSTSVPENPKSSTSATGCATPTEKEFPKTHSDASSEQQNRKSQTGTNGGSVKLYPTDQSTFDLLKDLEFSAGSPSKDTNESPWRSDLLIDENLLSPLAGEDDPFLLEGNTNEDCKPLILPDTKPKIKDTGDTILSSPSSVALPQVKTEKDDFIELCTPGVIKQEKLGPVYCQASFSGTNIIGNKMSAISVHGVSTSGGQMYHYDMNTASLSQQQDQKPVFNVIPPIPVGSENWNRCQGSGEDSLTSLGALNFPGRSVFSNGYSSPGMRPDVSSPPSSSSAATGPPPKLCLVCSDEASGCHYGVLTCGSCKVFFKRAVEGQHNYLCAGRNDCIIDKIRRKNCPACRYRKCLQAGMNLEARKTKKKIKGIQQATAGVSQDTSENPNKTIVPAALPQLTPTLVSLLEVIEPEVLYAGYDSSVPDSAWRIMTTLNMLGGRQVIAAVKWAKAILGLRNLHLDDQMTLLQYSWMFLMAFALGWRSYRQSSGNLLCFAPDLIINEQRMSLPCMYDQCKHMLFVSSELQRLQVSYEEYLCMKTLLLLSSVPKEGLKSQELFDEIRMTYIKELGKAIVKREGNSSQNWQRFYQLTKLLDSMHEVVENLLTYCFQTFLDKTMSIEFPEMLAEIITNQIPKYSNGNIKKLLFHQK
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Organism
Rattus norvegicus, Rat
Protein Classification
Transcription factor
>
Nuclear receptor
>
Nuclear hormone receptor subfamily 3
>
Nuclear hormone receptor subfamily 3 group C
>
Nuclear hormone receptor subfamily 3 group C member 1
Function
Receptor for glucocorticoids (GC). Has a dual mode of action: as a transcription factor that binds to glucocorticoid response elements (GRE), both for nuclear and mitochondrial DNA, and as a modulator of other transcription factors. Affects inflammatory responses, cellular proliferation and differentiation in target tissues. Involved in chromatin remodeling (PubMed:12917342). Plays a role in rapid mRNA degradation by binding to the 5' UTR of target mRNAs and interacting with PNRC2 in a ligand-dependent manner which recruits the RNA helicase UPF1 and the mRNA-decapping enzyme DCP1A, leading to RNA decay (By similarity). Could act as a coactivator for STAT5-dependent transcription upon growth hormone (GH) stimulation and could reveal an essential role of hepatic GR in the control of body growth (By similarity). In response to induction by transcription factor EGR1/NGFI-A in the hippocampus, may play a role in the behavioral and hypothalamic-pituitary-adrenal responses to stress in offspring (PubMed:15220929).
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Uniprot ID
Primary ID:
P06536

Secondarily ID:
O08624
Q8R463
Q8R5J0
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Ensembl ID
ENSG00000113580
Subcellular Location
Cytoplasm
Nucleus
Mitochondrion
Cytoplasm
Cytoskeleton
Spindle
Cytoplasm
Cytoskeleton
Microtubule organizing center
Centrosome
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000298 , H4-II-E
 Cell Line Info 
Compound ID Compound Name Compound Formula
CP0070809
 Compound Info 
CCI-18781
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C25H31F3O5S
  1
1
EC50 = 0.76 nM
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CP0393622
 Compound Info 
[(8S,9S,10R,11S,13S,14S,17R)-17-[2-(1,3-benzothiazol-2-ylsulfanyl)acetyl]-11-hydroxy-10,13-dimethyl-3-oxo-7,8,9,11,12,14,15,16-octahydro-6H-cyclopenta[a]phenanthren-17-yl] furan-2-carboxylate
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C33H33NO6S2
  1
1
EC50 = 18.7 nM
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CP0238565
 Compound Info 
(6S,8S,9R,10S,11S,13S,14S,16R,17R)-17-[2-(1,3-benzothiazol-2-ylsulfanyl)acetyl]-6,9-difluoro-11,17-dihydroxy-10,13,16-trimethyl-6,7,8,11,12,14,15,16-octahydrocyclopenta[a]phenanthren-3-one
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C29H31F2NO4S2
  1
1
EC50 = 27 nM
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CP0035186
 Compound Info 
(10S,11S,14S,15S,17R)-17-[4-(dimethylamino)phenyl]-14-hydroxy-15-methyl-14-(prop-1-yn-1-yl)tetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadeca-1,6-dien-5-one
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C29H35NO2
  1
1
IC50 = 1.94 nM
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CP0416607
 Compound Info 
1-[(1S,2R,13S,14S,17R,18S,20S)-7-(4-fluorophenyl)-17,20-dihydroxy-2,18-dimethyl-6,7-diazapentacyclo[11.7.0.02,10.04,8.014,18]icosa-4(8),5,9-trien-17-yl]-2-hydroxyethanone
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C28H33FN2O4
  1
1
IC50 = 3.2 nM
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CP0416614
 Compound Info 
1-[(1S,2R,13S,14S,17R,18S,20S)-17,20-dihydroxy-2,18-dimethyl-7-phenyl-6,7-diazapentacyclo[11.7.0.02,10.04,8.014,18]icosa-4(8),5,9-trien-17-yl]-2-hydroxyethanone
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C28H34N2O4
  1
1
IC50 = 3.23 nM
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CP0380981
 Compound Info 
1-[(1S,2R,13S,14S,17R,18S,20S)-7-(4-fluorophenyl)-17,20-dihydroxy-2,18-dimethyl-6,7-diazapentacyclo[11.7.0.02,10.04,8.014,18]icosa-4(8),5,9-trien-17-yl]-2-pyridin-2-ylsulfanylethanone
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C33H36FN3O3S
  1
1
IC50 = 4.5 nM
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CP0444548
 Compound Info 
N-[2-[[benzyl(methyl)amino]methyl]-3-(4-fluoro-2-methoxyphenyl)-5-propan-2-yl-1H-indol-7-yl]methanesulfonamide
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C28H32FN3O3S
  1
1
IC50 = 10.6 nM
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CP0400170
 Compound Info 
1-[(1S,2R,13S,14S,17R,18S,20S)-7-(4-fluorophenyl)-17,20-dihydroxy-2,18-dimethyl-6,7-diazapentacyclo[11.7.0.02,10.04,8.014,18]icosa-4(8),5,9-trien-17-yl]-2-([1,3]oxazolo[4,5-b]pyridin-2-ylsulfanyl)ethanone
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C34H35FN4O4S
  1
1
IC50 = 13.3 nM
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CP0416609
 Compound Info 
1-[(1S,2R,13S,14S,17R,18S,20S)-7-(4-fluorophenyl)-17,20-dihydroxy-2,18-dimethyl-6,7-diazapentacyclo[11.7.0.02,10.04,8.014,18]icosa-4(8),5,9-trien-17-yl]-2-pyrimidin-2-ylsulfanylethanone
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C32H35FN4O3S
  1
1
IC50 = 14.3 nM
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CP0410986
 Compound Info 
N-[2-[[benzyl(methyl)amino]methyl]-5-tert-butyl-3-(4-fluoro-2-methoxyphenyl)-1H-indol-7-yl]methanesulfonamide
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C29H34FN3O3S
  1
1
IC50 = 14.4 nM
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CP0387981
 Compound Info 
(8S,9S,10R,11S,13S,14S,16R,17R)-11,17-dihydroxy-10,13,16-trimethyl-17-(2-quinolin-2-ylsulfanylacetyl)-7,8,9,11,12,14,15,16-octahydro-6H-cyclopenta[a]phenanthren-3-one
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C31H35NO4S
  1
1
IC50 = 19.2 nM
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CP0432716
 Compound Info 
(8S,9S,10R,11S,13S,14S,16R,17R)-11,17-dihydroxy-10,13,16-trimethyl-17-[2-([1,3]thiazolo[5,4-b]pyridin-2-ylsulfanyl)acetyl]-7,8,9,11,12,14,15,16-octahydro-6H-cyclopenta[a]phenanthren-3-one
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C28H32N2O4S2
  1
1
IC50 = 24.1 nM
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CP0400172
 Compound Info 
2-(1,3-benzothiazol-2-ylsulfanyl)-1-[(1S,2R,13S,14S,17R,18S,20S)-7-(4-fluorophenyl)-17,20-dihydroxy-2,18-dimethyl-6,7-diazapentacyclo[11.7.0.02,10.04,8.014,18]icosa-4(8),5,9-trien-17-yl]ethanone
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C35H36FN3O3S2
  1
1
IC50 = 24.1 nM
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CP0400173
 Compound Info 
1-[(1S,2R,13S,14S,17R,18S,20S)-7-(4-fluorophenyl)-17,20-dihydroxy-2,18-dimethyl-6,7-diazapentacyclo[11.7.0.02,10.04,8.014,18]icosa-4(8),5,9-trien-17-yl]-2-quinolin-2-ylsulfanylethanone
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C37H38FN3O3S
  1
1
IC50 = 24.3 nM
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CP0428604
 Compound Info 
2-(1,3-benzoxazol-2-ylsulfanyl)-1-[(1S,2R,13S,14S,17R,18S,20S)-7-cyclohexyl-17,20-dihydroxy-2,18-dimethyl-6,7-diazapentacyclo[11.7.0.02,10.04,8.014,18]icosa-4(8),5,9-trien-17-yl]ethanone
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C35H43N3O4S
  1
1
IC50 = 31.6 nM
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CP0400175
 Compound Info 
1-[(1S,2R,13S,14S,17R,18S,20S)-17,20-dihydroxy-2,18-dimethyl-7-phenyl-6,7-diazapentacyclo[11.7.0.02,10.04,8.014,18]icosa-4(8),5,9-trien-17-yl]-2-([1,3]oxazolo[4,5-b]pyridin-2-ylsulfanyl)ethanone
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C34H36N4O4S
  1
1
IC50 = 33.8 nM
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CP0432419
 Compound Info 
1-[(1S,2R,13S,14S,17R,18S,20S)-7-(4-fluorophenyl)-17,20-dihydroxy-2,18-dimethyl-6,7-diazapentacyclo[11.7.0.02,10.04,8.014,18]icosa-4(8),5,9-trien-17-yl]-2-quinolin-2-yloxyethanone
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C37H38FN3O4
  1
1
IC50 = 44.7 nM
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CP0400160
 Compound Info 
1-[(1S,2R,13S,14S,17R,18S,20S)-7-(4-fluorophenyl)-17,20-dihydroxy-2,18-dimethyl-6,7-diazapentacyclo[11.7.0.02,10.04,8.014,18]icosa-4(8),5,9-trien-17-yl]-2-naphthalen-2-ylsulfanylethanone
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C38H39FN2O3S
  1
1
IC50 = 52.5 nM
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CP0400171
 Compound Info 
2-(1,3-benzothiazol-2-ylsulfanyl)-1-[(1S,2R,13S,14S,17R,18S,20S)-7-cyclohexyl-17,20-dihydroxy-2,18-dimethyl-6,7-diazapentacyclo[11.7.0.02,10.04,8.014,18]icosa-4(8),5,9-trien-17-yl]ethanone
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C35H43N3O3S2
  1
1
IC50 = 54.7 nM
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CP0380940
 Compound Info 
2-(1,3-benzothiazol-2-ylsulfanyl)-1-[(1S,2R,13S,14S,17R,18S,20S)-17,20-dihydroxy-2,18-dimethyl-7-phenyl-6,7-diazapentacyclo[11.7.0.02,10.04,8.014,18]icosa-4(8),5,9-trien-17-yl]ethanone
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C35H37N3O3S2
  1
1
IC50 = 57.3 nM
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CP0416608
 Compound Info 
1-[(1S,2R,13S,14S,17R,18S,20S)-7-(4-fluorophenyl)-17,20-dihydroxy-2,18-dimethyl-6,7-diazapentacyclo[11.7.0.02,10.04,8.014,18]icosa-4(8),5,9-trien-17-yl]-2-naphthalen-2-yloxyethanone
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C38H39FN2O4
  1
1
IC50 = 58 nM
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CP0413727
 Compound Info 
N-[5-fluoro-3-(4-fluoro-2-methoxyphenyl)-2-methyl-1H-indol-7-yl]methanesulfonamide
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C17H16F2N2O3S
  1
1
IC50 = 63.4 nM
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CP0047174
 Compound Info 
(1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-14-(2-hydroxyacetyl)-2,15-dimethyltetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadeca-3,6-dien-5-one
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C21H28O5
  1
1
IC50 = 65.4 nM
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CP0380980
 Compound Info 
1-[(1S,2R,13S,14S,17R,18S,20S)-7-(4-fluorophenyl)-17,20-dihydroxy-2,18-dimethyl-6,7-diazapentacyclo[11.7.0.02,10.04,8.014,18]icosa-4(8),5,9-trien-17-yl]-2-isoquinolin-1-ylsulfanylethanone
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C37H38FN3O3S
  1
1
IC50 = 65.4 nM
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CP0413728
 Compound Info 
N-[3-(3-chlorophenyl)-1H-indol-7-yl]methanesulfonamide
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C15H13ClN2O2S
  1
1
IC50 = 76 nM
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CP0410217
 Compound Info 
1-[(1S,2R,13S,14S,17R,18S,20S)-17,20-dihydroxy-2,18-dimethyl-7-phenyl-6,7-diazapentacyclo[11.7.0.02,10.04,8.014,18]icosa-4(8),5,9-trien-17-yl]-2-(1-methylbenzimidazol-2-yl)sulfanylethanone
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C36H40N4O3S
  1
1
IC50 = 78 nM
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CP0416612
 Compound Info 
1-[(1S,2R,13S,14S,17R,18S,20S)-7-(4-fluorophenyl)-17,20-dihydroxy-2,18-dimethyl-6,7-diazapentacyclo[11.7.0.02,10.04,8.014,18]icosa-4(8),5,9-trien-17-yl]-2-(1-methylbenzimidazol-2-yl)oxyethanone
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C36H39FN4O4
  1
1
IC50 = 78 nM
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CP0400177
 Compound Info 
1-[(1S,2R,13S,14S,17R,18S,20S)-17,20-dihydroxy-2,18-dimethyl-7-phenyl-6,7-diazapentacyclo[11.7.0.02,10.04,8.014,18]icosa-4(8),5,9-trien-17-yl]-2-quinolin-2-ylsulfanylethanone
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C37H39N3O3S
  1
1
IC50 = 82.3 nM
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CP0385331
 Compound Info 
2-(1,3-benzothiazol-2-yloxy)-1-[(1S,2R,13S,14S,17R,18S,20S)-7-(4-fluorophenyl)-17,20-dihydroxy-2,18-dimethyl-6,7-diazapentacyclo[11.7.0.02,10.04,8.014,18]icosa-4(8),5,9-trien-17-yl]ethanone
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C35H36FN3O4S
  1
1
IC50 = 84 nM
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CP0385328
 Compound Info 
2-[2-[(1S,2R,13S,14S,17R,18S,20S)-7-(4-fluorophenyl)-17,20-dihydroxy-2,18-dimethyl-6,7-diazapentacyclo[11.7.0.02,10.04,8.014,18]icosa-4(8),5,9-trien-17-yl]-2-oxoethyl]sulfanyl-3H-quinazolin-4-one
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C36H37FN4O4S
  1
1
IC50 = 86.5 nM
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CP0416610
 Compound Info 
1-[(1S,2R,13S,14S,17R,18S,20S)-17,20-dihydroxy-2,18-dimethyl-7-phenyl-6,7-diazapentacyclo[11.7.0.02,10.04,8.014,18]icosa-4(8),5,9-trien-17-yl]-2-quinoxalin-2-ylsulfanylethanone
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C36H38N4O3S
  1
1
IC50 = 113 nM
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CP0401463
 Compound Info 
(8S,9S,10R,11S,13S,14S,16R,17R)-11,17-dihydroxy-10,13,16-trimethyl-17-[2-([1,3]oxazolo[4,5-b]pyridin-2-ylsulfanyl)acetyl]-7,8,9,11,12,14,15,16-octahydro-6H-cyclopenta[a]phenanthren-3-one
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C28H32N2O5S
  1
1
IC50 = 135 nM
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CP0446952
 Compound Info 
1-[(1S,2R,13S,14S,17R,18S,20S)-7-cyclohexyl-17,20-dihydroxy-2,18-dimethyl-6,7-diazapentacyclo[11.7.0.02,10.04,8.014,18]icosa-4(8),5,9-trien-17-yl]-2-[(4,5-dimethyl-1,3-thiazol-2-yl)sulfanyl]ethanone
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C33H45N3O3S2
  1
1
IC50 = 135 nM
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CP0410216
 Compound Info 
1-[(1S,2R,13S,14S,17R,18S,20S)-7-(4-fluorophenyl)-17,20-dihydroxy-2,18-dimethyl-6,7-diazapentacyclo[11.7.0.02,10.04,8.014,18]icosa-4(8),5,9-trien-17-yl]-2-(1-methylbenzimidazol-2-yl)sulfanylethanone
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C36H39FN4O3S
  1
1
IC50 = 174 nM
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CP0400174
 Compound Info 
1-[(1S,2R,13S,14S,17R,18S,20S)-17,20-dihydroxy-2,18-dimethyl-7-phenyl-6,7-diazapentacyclo[11.7.0.02,10.04,8.014,18]icosa-4(8),5,9-trien-17-yl]-2-pyridin-2-ylsulfanylethanone
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C33H37N3O3S
  1
1
IC50 = 225 nM
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CP0387984
 Compound Info 
(8S,9S,10R,11S,13S,14S,16R,17R)-17-[2-(1,3-benzothiazol-2-ylsulfanyl)acetyl]-11,17-dihydroxy-10,13,16-trimethyl-7,8,9,11,12,14,15,16-octahydro-6H-cyclopenta[a]phenanthren-3-one
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C29H33NO4S2
  1
1
IC50 = 230 nM
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CP0145473
 Compound Info 
(8S,9S,10R,11S,13S,14S,17R)-11,17-dihydroxy-10,13-dimethyl-17-[2-(1-methylbenzimidazol-2-yl)sulfanylacetyl]-7,8,9,11,12,14,15,16-octahydro-6H-cyclopenta[a]phenanthren-3-one
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C29H34N2O4S
  1
1
IC50 = 235 nM
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CP0434913
 Compound Info 
1-[(1S,2R,13S,14S,17R,18S,20S)-17,20-dihydroxy-2,18-dimethyl-7-phenyl-6,7-diazapentacyclo[11.7.0.02,10.04,8.014,18]icosa-4(8),5,9-trien-17-yl]-2-(1-prop-2-enylbenzimidazol-2-yl)sulfanylethanone
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C38H42N4O3S
  1
1
IC50 = 258 nM
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CP0429171
 Compound Info 
N-[2-benzyl-3-(4-fluoro-2-methoxyphenyl)-5-propan-2-yl-1H-indol-7-yl]methanesulfonamide
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C26H27FN2O3S
  1
1
IC50 = 292 nM
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CP0385432
 Compound Info 
(8S,9S,10R,11S,13S,14S,17R)-11,17-dihydroxy-10,13-dimethyl-17-(2-quinolin-2-ylsulfanylacetyl)-7,8,9,11,12,14,15,16-octahydro-6H-cyclopenta[a]phenanthren-3-one
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C30H33NO4S
  1
1
IC50 = 361 nM
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CP0385431
 Compound Info 
(8S,9S,10R,11S,13S,14S,17R)-11,17-dihydroxy-10,13-dimethyl-17-(2-pyridin-2-ylsulfanylacetyl)-7,8,9,11,12,14,15,16-octahydro-6H-cyclopenta[a]phenanthren-3-one
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C26H31NO4S
  1
1
IC50 = 707 nM
 Bioactivity Info 
   TI
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CP0427353
 Compound Info 
(8S,9S,10R,11S,13S,14S,16R,17R)-11,17-dihydroxy-10,13,16-trimethyl-17-[2-[(5-phenyl-1,3,4-oxadiazol-2-yl)sulfanyl]acetyl]-7,8,9,11,12,14,15,16-octahydro-6H-cyclopenta[a]phenanthren-3-one
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C30H34N2O5S
  1
1
IC50 = 740 nM
 Bioactivity Info 
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CP0409039
 Compound Info 
1-[(1S,2R,13S,14S,17R,18S,20S)-7-cyclohexyl-17,20-dihydroxy-2,18-dimethyl-6,7-diazapentacyclo[11.7.0.02,10.04,8.014,18]icosa-4(8),5,9-trien-17-yl]-2-(1-methylbenzimidazol-2-yl)sulfanylethanone
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C36H46N4O3S
  1
1
IC50 = 1000 nM
 Bioactivity Info 
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CP0513116
 Compound Info 
N-[3-(2-methoxyphenyl)-1H-indol-7-yl]methanesulfonamide
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C16H16N2O3S
  1
1
IC50 = 1180 nM
 Bioactivity Info 
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CP0416932
 Compound Info 
N-[3-(5-chloro-2-methoxyphenyl)-1H-indol-7-yl]methanesulfonamide
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C16H15ClN2O3S
  1
1
IC50 = 1250 nM
 Bioactivity Info 
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CP0424441
 Compound Info 
2-[3,5-dibromo-4-[4-methoxy-2-(3-methylbenzoyl)-5-propan-2-ylphenoxy]phenyl]acetic acid
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C26H24Br2O5
  1
1
IC50 = 2500 nM
 Bioactivity Info 
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Cell Line ID: CL000430 , H4-II-E-C3
 Cell Line Info 
Cell Line ID: CL000230 , INS-1 832/13
 Cell Line Info 
Cell Line ID: CL000752 , PBMC iPSC #1
 Cell Line Info 
Cell Line ID: CL000043 , U2OS
 Cell Line Info 
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0035186
 Compound Info 
(10S,11S,14S,15S,17R)-17-[4-(dimethylamino)phenyl]-14-hydroxy-15-methyl-14-(prop-1-yn-1-yl)tetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadeca-1,6-dien-5-one
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C29H35NO2
  2
1 EC50 = 2.512 nM
2 IC50 = 1.4 nM
CP0070809
 Compound Info 
CCI-18781
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C25H31F3O5S
  2
1 IC50 = 0.14 nM
2 IC50 = 5 nM
CP0008077
 Compound Info 
(1R,2S,10S,11S,13R,14R,15S,17S)-1-fluoro-14,17-dihydroxy-14-(2-hydroxyacetyl)-2,13,15-trimethyltetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadeca-3,6-dien-5-one
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C22H29FO5
  1
1 IC50 = 22 nM
Similar Protein(s) and Bioactivity Statistics
90% Identity
Protein ID Protein Name Protein Organism
PT03331 Glucocorticoid receptor Mus musculus, Mouse
 Protein Info 
50% Identity
Protein ID Protein Name Protein Organism
PT00645 Glucocorticoid receptor Canis lupus familiaris, Dog, Canis familiaris
 Protein Info 
PT00967 Glucocorticoid receptor Homo sapiens, Human
 Protein Info 
PT07390 Glucocorticoid receptor Sus scrofa, Pig
 Protein Info