BDBM18627 (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::Mifeprex::Mifepristone::RU-486::RU486 (tetramethyl-rhodamine conjugated)

SMILES CC#C[C@]1(O)CC[C@H]2[C@@H]3CCC4=CC(=O)CCC4=C3[C@H](C[C@]12C)c1ccc(cc1)N(C)C

InChI Key InChIKey=VKHAHZOOUSRJNA-UHFFFAOYSA-N

Data  44 KI  134 IC50  2 Kd  13 EC50

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
Find this compound or compounds like it in BindingDB:
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Exact match

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 197 hits for monomerid = 18627   

TargetGlucocorticoid receptor(Human)
Ligand Pharmaceuticals

LigandPNGBDBM18627(Mifeprex | (10S,11S,14S,15S,17R)-17-[4-(dimethylam...)
Affinity DataEC50:  0.600nMpH: 7.5Assay Description:GR-Mediated Antagonist Activity Assay- GR-mediated antagonist activity is measured in the presence of a concentration of dexamethasone empirically de...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/17/2007
Entry Details Article
PubMed
TargetGlucocorticoid receptor(Human)
Ligand Pharmaceuticals

LigandPNGBDBM18627(Mifeprex | (10S,11S,14S,15S,17R)-17-[4-(dimethylam...)
Affinity DataIC50: 1.10nM EC50:  4.80nMpH: 8.0 T: 2°CAssay Description:For compounds able to displace the 3(H)-dexamethasone from the receptor an IC50 value (the concentration required to inhibit 50% of the binding of 3(...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/24/2007
Entry Details Article
PubMed
TargetGlucocorticoid receptor(Rat)
Abbott Laboratories

LigandPNGBDBM18627(Mifeprex | (10S,11S,14S,15S,17R)-17-[4-(dimethylam...)
Affinity DataIC50: 1.40nMpH: 8.0 T: 2°CAssay Description:For compounds able to displace the radiolabeled ligand (competitor) from the receptor an IC50 value (the concentration required to inhibit 50% of the...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/24/2007
Entry Details Article
PubMed
TargetProgesterone receptor(Human)
Abbott Laboratories

LigandPNGBDBM18627(Mifeprex | (10S,11S,14S,15S,17R)-17-[4-(dimethylam...)
Affinity DataIC50: 2.90nMpH: 8.0 T: 2°CAssay Description:For compounds able to displace the radiolabeled ligand (competitor) from the receptor an IC50 value (the concentration required to inhibit 50% of the...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/24/2007
Entry Details Article
PubMed
TargetAndrogen receptor(Human)
Abbott Laboratories

LigandPNGBDBM18627(Mifeprex | (10S,11S,14S,15S,17R)-17-[4-(dimethylam...)
Affinity DataIC50: 8.80nMpH: 8.0 T: 2°CAssay Description:For compounds able to displace the radiolabeled ligand (competitor) from the receptor an IC50 value (the concentration required to inhibit 50% of the...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/24/2007
Entry Details Article
PubMed
TargetMineralocorticoid receptor(Human)
Abbott Laboratories

LigandPNGBDBM18627(Mifeprex | (10S,11S,14S,15S,17R)-17-[4-(dimethylam...)
Affinity DataIC50: 6.00E+3nMpH: 8.0 T: 2°CAssay Description:For compounds able to displace the radiolabeled ligand (competitor) from the receptor an IC50 value (the concentration required to inhibit 50% of the...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/24/2007
Entry Details Article
PubMed
LigandPNGBDBM18627(Mifeprex | (10S,11S,14S,15S,17R)-17-[4-(dimethylam...)
Affinity DataIC50: 1.33E+5nMAssay Description:Inhibition of human MRP2 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/3/2019
Entry Details Article
PubMed
LigandPNGBDBM18627(Mifeprex | (10S,11S,14S,15S,17R)-17-[4-(dimethylam...)
Affinity DataIC50: 1.33E+5nMAssay Description:Inhibition of human MRP3 overexpressed in Sf9 insect cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/3/2019
Entry Details Article
PubMed
LigandPNGBDBM18627(Mifeprex | (10S,11S,14S,15S,17R)-17-[4-(dimethylam...)
Affinity DataIC50: 1.33E+5nMAssay Description:Inhibition of human MRP4 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/3/2019
Entry Details Article
PubMed
TargetBile salt export pump(Human)
Amgen

Curated by ChEMBL
LigandPNGBDBM18627(Mifeprex | (10S,11S,14S,15S,17R)-17-[4-(dimethylam...)
Affinity DataIC50: 2.02E+3nMAssay Description:Inhibition of human BSEP overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-taurocholate in presence of ATP measured after 15 to ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/3/2019
Entry Details Article
PubMed
TargetProgesterone receptor(Human)
Abbott Laboratories

LigandPNGBDBM18627(Mifeprex | (10S,11S,14S,15S,17R)-17-[4-(dimethylam...)
Affinity DataIC50: 5.20nMAssay Description:Displacement of [1,2,6,7-3H]progesterone from recombinant human GST-tagged PGR LBD (678 to 933 residues) expressed in baculovirus-infected insect cel...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/14/2020
Entry Details Article
PubMed
TargetGlucocorticoid receptor(Human)
Ligand Pharmaceuticals

LigandPNGBDBM18627(Mifeprex | (10S,11S,14S,15S,17R)-17-[4-(dimethylam...)
Affinity DataIC50: 0.800nMAssay Description:Antagonist activity at human GR assessed as reduction in dexamethasone-induced transactivationMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/14/2020
Entry Details Article
PubMed
TargetProgesterone receptor(Human)
Abbott Laboratories

LigandPNGBDBM18627(Mifeprex | (10S,11S,14S,15S,17R)-17-[4-(dimethylam...)
Affinity DataIC50: 0.300nMAssay Description:Antagonist activity at human PRB expressed in African green monkey CV1 cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/14/2020
Entry Details Article
PubMed
TargetAndrogen receptor(Human)
Abbott Laboratories

LigandPNGBDBM18627(Mifeprex | (10S,11S,14S,15S,17R)-17-[4-(dimethylam...)
Affinity DataIC50: 5nMAssay Description:Antagonist activity at human AR assessed as reduction in DHT-induced transactivationMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/14/2020
Entry Details Article
PubMed
TargetProgesterone receptor(Human)
Abbott Laboratories

LigandPNGBDBM18627(Mifeprex | (10S,11S,14S,15S,17R)-17-[4-(dimethylam...)
Affinity DataIC50: 0.0730nMAssay Description:Antagonist activity at PR in human T47D cells assessed as inhibition of progesterone-induced alkaline phosphatase activity measured after 24 hrsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/14/2020
Entry Details Article
PubMed
TargetCytochrome P450 3A4(Human)
Oric Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM18627(Mifeprex | (10S,11S,14S,15S,17R)-17-[4-(dimethylam...)
Affinity DataIC50: 9.50E+3nMAssay Description:Inhibition of CYP3A4 (unknown origin) using midazolam as substrateMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/14/2020
Entry Details Article
PubMed
TargetGlucocorticoid receptor(Pig)
Oric Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM18627(Mifeprex | (10S,11S,14S,15S,17R)-17-[4-(dimethylam...)
Affinity DataIC50: 11nMAssay Description:Antagonist activity at GR in mini pig PBMC assessed as reduction in dexamethasone-induced GILZ gene expression incubated for 24 hrs by RT-qPCR methodMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/14/2020
Entry Details Article
PubMed
TargetGlucocorticoid receptor(Human)
Ligand Pharmaceuticals

LigandPNGBDBM18627(Mifeprex | (10S,11S,14S,15S,17R)-17-[4-(dimethylam...)
Affinity DataEC50: >2.50E+3nMAssay Description:Agonist activity at human GR expressed in CHO-K1 cells incubated for 20 hrs by luciferase reporter gene assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/14/2020
Entry Details Article
PubMed
TargetGlucocorticoid receptor(Human)
Ligand Pharmaceuticals

LigandPNGBDBM18627(Mifeprex | (10S,11S,14S,15S,17R)-17-[4-(dimethylam...)
Affinity DataIC50: 3.30nMAssay Description:Antagonist activity at human GR expressed in CHO-K1 cells assessed as reduction in dexamethasone-induced response incubated for 20 hrs by luciferase ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/14/2020
Entry Details Article
PubMed
TargetAndrogen receptor(Human)
Abbott Laboratories

LigandPNGBDBM18627(Mifeprex | (10S,11S,14S,15S,17R)-17-[4-(dimethylam...)
Affinity DataEC50:  12nMAssay Description:Agonist activity at AR (unknown origin) expressed in human LNCaP cells incubated for 20 hrs by luciferase reporter gene assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/14/2020
Entry Details Article
PubMed
TargetCytochrome P450 2C8(Human)
Oric Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM18627(Mifeprex | (10S,11S,14S,15S,17R)-17-[4-(dimethylam...)
Affinity DataIC50: 1.50E+3nMAssay Description:Inhibition of CYP2C8 (unknown origin) using midazolam as substrateMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/14/2020
Entry Details Article
PubMed
TargetProgesterone receptor(Human)
Abbott Laboratories

LigandPNGBDBM18627(Mifeprex | (10S,11S,14S,15S,17R)-17-[4-(dimethylam...)
Affinity DataIC50: 0.400nMAssay Description:Antagonist activity at human PR expressed in CHO-K1 cells assessed as reduction in progesterone-induced response incubated for 20 hrs by luciferase r...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/14/2020
Entry Details Article
PubMed
TargetGlucocorticoid receptor(Human)
Ligand Pharmaceuticals

LigandPNGBDBM18627(Mifeprex | (10S,11S,14S,15S,17R)-17-[4-(dimethylam...)
Affinity DataIC50: 18nMAssay Description:Antagonist activity at GR in human PBMC assessed as reduction in dexamethasone-induced GILZ gene expression incubated for 6 hrs by RT-qPCR methodMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/14/2020
Entry Details Article
PubMed
TargetGlucocorticoid receptor(Human)
Ligand Pharmaceuticals

LigandPNGBDBM18627(Mifeprex | (10S,11S,14S,15S,17R)-17-[4-(dimethylam...)
Affinity DataIC50: 15nMAssay Description:Antagonist activity at GR in human PBMC assessed as reduction in dexamethasone-induced FKBP5 gene expression incubated for 6 hrs by RT-qPCR methodMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/14/2020
Entry Details Article
PubMed
TargetGlucocorticoid receptor(Dog)
Oric Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM18627(Mifeprex | (10S,11S,14S,15S,17R)-17-[4-(dimethylam...)
Affinity DataIC50: 33nMAssay Description:Antagonist activity at GR in dog PBMC assessed as reduction in dexamethasone-induced GILZ gene expression incubated for 6 hrs by RT-qPCR methodMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/14/2020
Entry Details Article
PubMed
TargetGlucocorticoid receptor(Pig)
Oric Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM18627(Mifeprex | (10S,11S,14S,15S,17R)-17-[4-(dimethylam...)
Affinity DataIC50: 20nMAssay Description:Antagonist activity at GR in mini pig PBMC assessed as reduction in dexamethasone-induced FKBP5 gene expression incubated for 24 hrs by RT-qPCR metho...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/14/2020
Entry Details Article
PubMed
TargetGlucocorticoid receptor(Human)
Ligand Pharmaceuticals

LigandPNGBDBM18627(Mifeprex | (10S,11S,14S,15S,17R)-17-[4-(dimethylam...)
Affinity DataIC50: 13nMAssay Description:Antagonist activity at GR in human OVCAR5 assessed as reduction in dexamethasone-induced FKBP5 gene expression incubated for 24 hrs by RT-qPCR methodMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/14/2020
Entry Details Article
PubMed
TargetCytochrome P450 2C9(Human)
Oric Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM18627(Mifeprex | (10S,11S,14S,15S,17R)-17-[4-(dimethylam...)
Affinity DataIC50: 4.90E+3nMAssay Description:Inhibition of CYP2C9 (unknown origin) using midazolam as substrateMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/14/2020
Entry Details Article
PubMed
TargetGlucocorticoid receptor(Dog)
Oric Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM18627(Mifeprex | (10S,11S,14S,15S,17R)-17-[4-(dimethylam...)
Affinity DataIC50: 20nMAssay Description:Antagonist activity at GR in dog PBMC assessed as reduction in dexamethasone-induced FKBP5 gene expression incubated for 6 hrs by RT-qPCR methodMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/14/2020
Entry Details Article
PubMed
TargetGlucocorticoid receptor(Human)
Ligand Pharmaceuticals

LigandPNGBDBM18627(Mifeprex | (10S,11S,14S,15S,17R)-17-[4-(dimethylam...)
Affinity DataIC50: 8.70nMAssay Description:Displacement of fluormone RED from human full length glucocorticoid receptor after 4 hrs by fluorescence polarization assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/16/2020
Entry Details Article
PubMed
TargetGlucocorticoid receptor(Human)
Ligand Pharmaceuticals

LigandPNGBDBM18627(Mifeprex | (10S,11S,14S,15S,17R)-17-[4-(dimethylam...)
Affinity DataIC50: 15nMAssay Description:Antagonist activity at glucocorticoid receptor (unknown origin) expressed in human ChaGoK1 cells assessed as inhibition of dexamethasone induced tran...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/16/2020
Entry Details Article
PubMed
TargetProgesterone receptor(Rat)
Forschungszentrum Dresden-Rossendorf

Curated by ChEMBL
LigandPNGBDBM18627(Mifeprex | (10S,11S,14S,15S,17R)-17-[4-(dimethylam...)
Affinity DataEC50:  16nMAssay Description:Binding affinity to progesterone receptorMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/24/2020
Entry Details Article
PubMed
TargetGlucocorticoid receptor(Rat)
Abbott Laboratories

LigandPNGBDBM18627(Mifeprex | (10S,11S,14S,15S,17R)-17-[4-(dimethylam...)
Affinity DataEC50:  2.5nMAssay Description:Binding affinity to rat glucocorticoid receptorMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/24/2020
Entry Details Article
PubMed
TargetGlucocorticoid receptor(Human)
Ligand Pharmaceuticals

LigandPNGBDBM18627(Mifeprex | (10S,11S,14S,15S,17R)-17-[4-(dimethylam...)
Affinity DataKd:  15nMAssay Description:Binding affinity to GR (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/20/2021
Entry Details Article
PubMed
TargetAndrogen receptor(Human)
Abbott Laboratories

LigandPNGBDBM18627(Mifeprex | (10S,11S,14S,15S,17R)-17-[4-(dimethylam...)
Affinity DataEC50:  12nMAssay Description:Agonist activity at human androgen receptor in human LNCAP cells harboring firefly luciferase gene after 20 hrs by One-Glo luciferase reporter gene a...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/25/2021
Entry Details Article
PubMed
TargetProgesterone receptor(Human)
Abbott Laboratories

LigandPNGBDBM18627(Mifeprex | (10S,11S,14S,15S,17R)-17-[4-(dimethylam...)
Affinity DataIC50: 0.400nMAssay Description:Antagonist activity at human progesterone receptor expressed in CHO-K1 cells harboring firefly luciferase gene after 20 hrs by One-Glo luciferase rep...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/25/2021
Entry Details Article
PubMed
TargetCytochrome P450 3A4(Human)
Oric Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM18627(Mifeprex | (10S,11S,14S,15S,17R)-17-[4-(dimethylam...)
Affinity DataIC50: 9.50E+3nMAssay Description:Inhibition of CYP3A4 (unknown origin) using midazolam as substrateMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/25/2021
Entry Details Article
PubMed
TargetCytochrome P450 2C8(Human)
Oric Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM18627(Mifeprex | (10S,11S,14S,15S,17R)-17-[4-(dimethylam...)
Affinity DataIC50: 1.50E+3nMAssay Description:Inhibition of CYP2C8 (unknown origin) using paclitaxel as substrateMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/25/2021
Entry Details Article
PubMed
TargetGlucocorticoid receptor(Human)
Ligand Pharmaceuticals

LigandPNGBDBM18627(Mifeprex | (10S,11S,14S,15S,17R)-17-[4-(dimethylam...)
Affinity DataIC50: 3.5nMAssay Description:Antagonist activity at human glucocorticoid receptor expressed in CHO-K1 cells assessed as inhibition of glucocorticoid receptor-dexamethasone coacti...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/25/2021
Entry Details Article
PubMed
TargetGlucocorticoid receptor(Human)
Ligand Pharmaceuticals

LigandPNGBDBM18627(Mifeprex | (10S,11S,14S,15S,17R)-17-[4-(dimethylam...)
Affinity DataIC50: 3.30nMAssay Description:Antagonist activity at human glucocorticoid receptor expressed in CHO-K1 cells harboring firefly luciferase gene after 20 hrs by One-Glo luciferase r...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/25/2021
Entry Details Article
PubMed
TargetGlucocorticoid receptor(Human)
Ligand Pharmaceuticals

LigandPNGBDBM18627(Mifeprex | (10S,11S,14S,15S,17R)-17-[4-(dimethylam...)
Affinity DataIC50: 2.30nMAssay Description:Displacement of fluormone tracer from full length human recombinant glucocorticoid receptor expressed in baculovirus expression system incubated for ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/25/2021
Entry Details Article
PubMed
TargetProgesterone receptor(Human)
Abbott Laboratories

LigandPNGBDBM18627(Mifeprex | (10S,11S,14S,15S,17R)-17-[4-(dimethylam...)
Affinity DataIC50: 0.100nMAssay Description:Inhibition of 3 nM [3H]R5020 binding to progesterone receptor of human T47D cell cytosolMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetGlucocorticoid receptor(Human)
Ligand Pharmaceuticals

LigandPNGBDBM18627(Mifeprex | (10S,11S,14S,15S,17R)-17-[4-(dimethylam...)
Affinity DataIC50: 0.640nMAssay 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
In Depth
Date in BDB:
3/7/2023
Entry Details Article
PubMed
TargetGlucocorticoid receptor(Human)
Ligand Pharmaceuticals

LigandPNGBDBM18627(Mifeprex | (10S,11S,14S,15S,17R)-17-[4-(dimethylam...)
In Depth
Date in BDB:
TBA
Entry Details
TargetGlucocorticoid receptor(Human)
Ligand Pharmaceuticals

LigandPNGBDBM18627(Mifeprex | (10S,11S,14S,15S,17R)-17-[4-(dimethylam...)
Affinity DataIC50: 18nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
TargetGlucocorticoid receptor(Human)
Ligand Pharmaceuticals

LigandPNGBDBM18627(Mifeprex | (10S,11S,14S,15S,17R)-17-[4-(dimethylam...)
In Depth
Date in BDB:
TBA
Entry Details
TargetProgesterone receptor(Human)
Abbott Laboratories

LigandPNGBDBM18627(Mifeprex | (10S,11S,14S,15S,17R)-17-[4-(dimethylam...)
Affinity DataIC50: 1.40nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
TargetAndrogen receptor(Human)
Abbott Laboratories

LigandPNGBDBM18627(Mifeprex | (10S,11S,14S,15S,17R)-17-[4-(dimethylam...)
Affinity DataIC50: 17nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
TargetProgesterone receptor(Human)
Abbott Laboratories

LigandPNGBDBM18627(Mifeprex | (10S,11S,14S,15S,17R)-17-[4-(dimethylam...)
Affinity DataIC50: 10nMAssay Description:Antagonist activity at progesterone receptorMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/22/2012
Entry Details Article
PubMed
TargetProgesterone receptor(Rat)
Forschungszentrum Dresden-Rossendorf

Curated by ChEMBL
LigandPNGBDBM18627(Mifeprex | (10S,11S,14S,15S,17R)-17-[4-(dimethylam...)
Affinity DataIC50: 3.5nMAssay Description:Inhibition of [3H]R5020 binding to cytosolic progesterone receptor (PRc) of rat uterusMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/25/2012
Entry Details Article

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