BDBM21130 N-methyl-2-phenyl-N-[(5R,7S,8S)-7-(pyrrolidin-1-yl)-1-oxaspiro[4.5]decan-8-yl]acetamide::N-methyl-N-(7-(1-pyrrolidinyl)-1-oxaspiro(4,5)dec-8-yl)benzeneacetamide::U-69593::U69,593::[3H]U69593

SMILES CN([C@H]1CC[C@@]2(CCCO2)C[C@@H]1N1CCCC1)C(=O)Cc1ccccc1

InChI Key InChIKey=PGZRDDYTKFZSFR-UHFFFAOYSA-N

Data  66 KI  8 IC50  10 Kd  41 EC50

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
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Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 125 hits for monomerid = 21130   Sort by

TargetKappa-type opioid receptor(Human)
University of North Carolina

LigandPNGBDBM21130(U69,593 | N-methyl-N-(7-(1-pyrrolidinyl)-1-oxaspir...)
Affinity DataEC50:  3.20nMpH: 7.4Assay Description:HEK293T cells were co-transfected with plasmids encoding the cAMP biosensor GloSensor-22F (Promega) and the different human KOR variants as described...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetKappa-type opioid receptor [Y66A](Human)
University of North Carolina

LigandPNGBDBM21130(U69,593 | N-methyl-N-(7-(1-pyrrolidinyl)-1-oxaspir...)
Affinity DataEC50:  18nMpH: 7.4Assay Description:HEK293T cells were co-transfected with plasmids encoding the cAMP biosensor GloSensor-22F (Promega) and the different human KOR variants as described...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetKappa-type opioid receptor [Q115A](Human)
University of North Carolina

LigandPNGBDBM21130(U69,593 | N-methyl-N-(7-(1-pyrrolidinyl)-1-oxaspir...)
Affinity DataEC50:  3nMpH: 7.4Assay Description:HEK293T cells were co-transfected with plasmids encoding the cAMP biosensor GloSensor-22F (Promega) and the different human KOR variants as described...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetKappa-type opioid receptor [Y119A](Human)
University of North Carolina

LigandPNGBDBM21130(U69,593 | N-methyl-N-(7-(1-pyrrolidinyl)-1-oxaspir...)
Affinity DataEC50:  9.10nMpH: 7.4Assay Description:HEK293T cells were co-transfected with plasmids encoding the cAMP biosensor GloSensor-22F (Promega) and the different human KOR variants as described...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetKappa-type opioid receptor [Y119F](Human)
University of North Carolina

LigandPNGBDBM21130(U69,593 | N-methyl-N-(7-(1-pyrrolidinyl)-1-oxaspir...)
Affinity DataEC50:  8.10nMpH: 7.4Assay Description:HEK293T cells were co-transfected with plasmids encoding the cAMP biosensor GloSensor-22F (Promega) and the different human KOR variants as described...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetKappa-type opioid receptor [I135A](Human)
University of North Carolina

LigandPNGBDBM21130(U69,593 | N-methyl-N-(7-(1-pyrrolidinyl)-1-oxaspir...)
Affinity DataEC50:  72nMpH: 7.4Assay Description:HEK293T cells were co-transfected with plasmids encoding the cAMP biosensor GloSensor-22F (Promega) and the different human KOR variants as described...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetKappa-type opioid receptor [D138N](Human)
University of North Carolina

LigandPNGBDBM21130(U69,593 | N-methyl-N-(7-(1-pyrrolidinyl)-1-oxaspir...)
Affinity DataEC50:  6.90E+3nMpH: 7.4Assay Description:HEK293T cells were co-transfected with plasmids encoding the cAMP biosensor GloSensor-22F (Promega) and the different human KOR variants as described...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetKappa-type opioid receptor [Y139A](Human)
University of North Carolina

LigandPNGBDBM21130(U69,593 | N-methyl-N-(7-(1-pyrrolidinyl)-1-oxaspir...)
Affinity DataEC50:  28nMpH: 7.4Assay Description:HEK293T cells were co-transfected with plasmids encoding the cAMP biosensor GloSensor-22F (Promega) and the different human KOR variants as described...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetKappa-type opioid receptor [Y139F](Human)
University of North Carolina

LigandPNGBDBM21130(U69,593 | N-methyl-N-(7-(1-pyrrolidinyl)-1-oxaspir...)
Affinity DataEC50:  3.30nMpH: 7.4Assay Description:HEK293T cells were co-transfected with plasmids encoding the cAMP biosensor GloSensor-22F (Promega) and the different human KOR variants as described...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetKappa-type opioid receptor [M142A](Human)
University of North Carolina

LigandPNGBDBM21130(U69,593 | N-methyl-N-(7-(1-pyrrolidinyl)-1-oxaspir...)
Affinity DataEC50:  19nMpH: 7.4Assay Description:HEK293T cells were co-transfected with plasmids encoding the cAMP biosensor GloSensor-22F (Promega) and the different human KOR variants as described...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetKappa-type opioid receptor [K200A](Human)
University of North Carolina

LigandPNGBDBM21130(U69,593 | N-methyl-N-(7-(1-pyrrolidinyl)-1-oxaspir...)
Affinity DataEC50:  1nMpH: 7.4Assay Description:HEK293T cells were co-transfected with plasmids encoding the cAMP biosensor GloSensor-22F (Promega) and the different human KOR variants as described...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetKappa-type opioid receptor [K212A](Human)
University of North Carolina

LigandPNGBDBM21130(U69,593 | N-methyl-N-(7-(1-pyrrolidinyl)-1-oxaspir...)
Affinity DataEC50:  17nMpH: 7.4Assay Description:HEK293T cells were co-transfected with plasmids encoding the cAMP biosensor GloSensor-22F (Promega) and the different human KOR variants as described...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetKappa-type opioid receptor [M226A](Human)
University of North Carolina

LigandPNGBDBM21130(U69,593 | N-methyl-N-(7-(1-pyrrolidinyl)-1-oxaspir...)
Affinity DataEC50:  0.190nMpH: 7.4Assay Description:HEK293T cells were co-transfected with plasmids encoding the cAMP biosensor GloSensor-22F (Promega) and the different human KOR variants as described...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetKappa-type opioid receptor [K227A](Human)
University of North Carolina

LigandPNGBDBM21130(U69,593 | N-methyl-N-(7-(1-pyrrolidinyl)-1-oxaspir...)
Affinity DataEC50:  4.20nMpH: 7.4Assay Description:HEK293T cells were co-transfected with plasmids encoding the cAMP biosensor GloSensor-22F (Promega) and the different human KOR variants as described...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetKappa-type opioid receptor [H291A](Human)
University of North Carolina

LigandPNGBDBM21130(U69,593 | N-methyl-N-(7-(1-pyrrolidinyl)-1-oxaspir...)
Affinity DataEC50:  130nMpH: 7.4Assay Description:HEK293T cells were co-transfected with plasmids encoding the cAMP biosensor GloSensor-22F (Promega) and the different human KOR variants as described...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetKappa-type opioid receptor [H291F](Human)
University of North Carolina

LigandPNGBDBM21130(U69,593 | N-methyl-N-(7-(1-pyrrolidinyl)-1-oxaspir...)
Affinity DataEC50:  4.30nMpH: 7.4Assay Description:HEK293T cells were co-transfected with plasmids encoding the cAMP biosensor GloSensor-22F (Promega) and the different human KOR variants as described...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetKappa-type opioid receptor [I294A](Human)
University of North Carolina

LigandPNGBDBM21130(U69,593 | N-methyl-N-(7-(1-pyrrolidinyl)-1-oxaspir...)
Affinity DataEC50:  4.70nMpH: 7.4Assay Description:HEK293T cells were co-transfected with plasmids encoding the cAMP biosensor GloSensor-22F (Promega) and the different human KOR variants as described...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetKappa-type opioid receptor [E297A](Human)
University of North Carolina

LigandPNGBDBM21130(U69,593 | N-methyl-N-(7-(1-pyrrolidinyl)-1-oxaspir...)
Affinity DataEC50:  1.20nMpH: 7.4Assay Description:HEK293T cells were co-transfected with plasmids encoding the cAMP biosensor GloSensor-22F (Promega) and the different human KOR variants as described...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetKappa-type opioid receptor [Y312A](Human)
University of North Carolina

LigandPNGBDBM21130(U69,593 | N-methyl-N-(7-(1-pyrrolidinyl)-1-oxaspir...)
Affinity DataEC50:  65nMpH: 7.4Assay Description:HEK293T cells were co-transfected with plasmids encoding the cAMP biosensor GloSensor-22F (Promega) and the different human KOR variants as described...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetKappa-type opioid receptor [Y312F](Human)
University of North Carolina

LigandPNGBDBM21130(U69,593 | N-methyl-N-(7-(1-pyrrolidinyl)-1-oxaspir...)
Affinity DataEC50:  5.60nMpH: 7.4Assay Description:HEK293T cells were co-transfected with plasmids encoding the cAMP biosensor GloSensor-22F (Promega) and the different human KOR variants as described...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetKappa-type opioid receptor [Y313A](Human)
University of North Carolina

LigandPNGBDBM21130(U69,593 | N-methyl-N-(7-(1-pyrrolidinyl)-1-oxaspir...)
Affinity DataEC50:  4.20nMpH: 7.4Assay Description:HEK293T cells were co-transfected with plasmids encoding the cAMP biosensor GloSensor-22F (Promega) and the different human KOR variants as described...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetKappa-type opioid receptor [Y313F](Human)
University of North Carolina

LigandPNGBDBM21130(U69,593 | N-methyl-N-(7-(1-pyrrolidinyl)-1-oxaspir...)
Affinity DataEC50:  4.80nMpH: 7.4Assay Description:HEK293T cells were co-transfected with plasmids encoding the cAMP biosensor GloSensor-22F (Promega) and the different human KOR variants as described...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetKappa-type opioid receptor [I316A](Human)
University of North Carolina

LigandPNGBDBM21130(U69,593 | N-methyl-N-(7-(1-pyrrolidinyl)-1-oxaspir...)
Affinity DataEC50:  19nMpH: 7.4Assay Description:HEK293T cells were co-transfected with plasmids encoding the cAMP biosensor GloSensor-22F (Promega) and the different human KOR variants as described...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetKappa-type opioid receptor [Y320A](Human)
University of North Carolina

LigandPNGBDBM21130(U69,593 | N-methyl-N-(7-(1-pyrrolidinyl)-1-oxaspir...)
Affinity DataEC50:  830nMpH: 7.4Assay Description:HEK293T cells were co-transfected with plasmids encoding the cAMP biosensor GloSensor-22F (Promega) and the different human KOR variants as described...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetKappa-type opioid receptor [Y320F](Human)
University of North Carolina

LigandPNGBDBM21130(U69,593 | N-methyl-N-(7-(1-pyrrolidinyl)-1-oxaspir...)
Affinity DataEC50:  150nMpH: 7.4Assay Description:HEK293T cells were co-transfected with plasmids encoding the cAMP biosensor GloSensor-22F (Promega) and the different human KOR variants as described...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetKappa-type opioid receptor(Human)
University of North Carolina

LigandPNGBDBM21130(U69,593 | N-methyl-N-(7-(1-pyrrolidinyl)-1-oxaspir...)
Affinity DataEC50:  0.800nMAssay Description:Agonist activity at human KOR expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by luminescence assa...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetKappa-type opioid receptor(Rat)
University of Kansas Specialized Chemistry Center

Curated by ChEMBL
LigandPNGBDBM21130(U69,593 | N-methyl-N-(7-(1-pyrrolidinyl)-1-oxaspir...)
Affinity DataKd:  1nMAssay Description:Binding affinity to rat kappa opioid receptor expressed in HEK293 cell membranesMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetKappa-type opioid receptor(Human)
University of North Carolina

LigandPNGBDBM21130(U69,593 | N-methyl-N-(7-(1-pyrrolidinyl)-1-oxaspir...)
Affinity DataEC50:  12nMAssay Description:Agonist activity at human kappa opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS bindingMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetKappa-type opioid receptor(Human)
University of North Carolina

LigandPNGBDBM21130(U69,593 | N-methyl-N-(7-(1-pyrrolidinyl)-1-oxaspir...)
Affinity DataEC50:  28nMAssay Description:Agonist activity at human kappa opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetKappa-type opioid receptor(Human)
University of North Carolina

LigandPNGBDBM21130(U69,593 | N-methyl-N-(7-(1-pyrrolidinyl)-1-oxaspir...)
Affinity DataEC50:  28nMAssay Description:Agonist activity at human KOR expressed in CHO cell membranes by [35S]GTPgammaS binding assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetDelta-type opioid receptor(Human)
Research Triangle Institute

Curated by ChEMBL
LigandPNGBDBM21130(U69,593 | N-methyl-N-(7-(1-pyrrolidinyl)-1-oxaspir...)
Affinity DataKd:  1.98E+3nMAssay Description:Binding affinity against Delta opioid receptor in using [35S]GTP-gamma-S, binding assay in guinea pig caudate membranes blocked with 20 nM NTIMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetMu-type opioid receptor(Guinea pig)
Research Triangle Institute

Curated by ChEMBL
LigandPNGBDBM21130(U69,593 | N-methyl-N-(7-(1-pyrrolidinyl)-1-oxaspir...)
Affinity DataKd:  684nMAssay Description:Binding affinity against Mu opioid receptor using [35S]GTP-gamma-S, binding assay in guinea pig caudate membranes in unblocked conditionMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetMu-type opioid receptor(Guinea pig)
Research Triangle Institute

Curated by ChEMBL
LigandPNGBDBM21130(U69,593 | N-methyl-N-(7-(1-pyrrolidinyl)-1-oxaspir...)
Affinity DataKd:  2.14E+3nMAssay Description:Binding affinity against Mu opioid receptor using [35S]GTP-gamma-S, binding assay in guinea pig caudate membranes blocked with 6000 nM CTAPMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetKappa-type opioid receptor(Guinea pig)
Research Triangle Institute

Curated by ChEMBL
LigandPNGBDBM21130(U69,593 | N-methyl-N-(7-(1-pyrrolidinyl)-1-oxaspir...)
Affinity DataKd:  4.89E+3nMAssay Description:Binding affinity against kappa opioid receptor using [35S]GTP-gamma-S, binding assay in guinea pig caudate membranes blocked with 6 nM nor-BNIMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetDelta-type opioid receptor(Human)
Research Triangle Institute

Curated by ChEMBL
LigandPNGBDBM21130(U69,593 | N-methyl-N-(7-(1-pyrrolidinyl)-1-oxaspir...)
Affinity DataIC50: 5.84E+3nMAssay Description:Binding affinity towards Opioid receptor delta 1 by the displacement of [125I]-DeltorphinMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetMu-type opioid receptor(Human)
Astrazeneca R&D MöLndal

Curated by ChEMBL
LigandPNGBDBM21130(U69,593 | N-methyl-N-(7-(1-pyrrolidinyl)-1-oxaspir...)
Affinity DataIC50: 248nMAssay Description:Binding affinity towards Opioid receptor mu 1 by the displacement of [125I]Enkephalin; Not determinedMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetKappa-type opioid receptor(Human)
University of North Carolina

LigandPNGBDBM21130(U69,593 | N-methyl-N-(7-(1-pyrrolidinyl)-1-oxaspir...)
Affinity DataIC50: 2nMAssay Description:Binding affinity towards Opioid receptor kappa 1 by the displacement of [125I]-(D-Pro10)-Dynorphin AMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetMu-type opioid receptor(Guinea pig)
Research Triangle Institute

Curated by ChEMBL
LigandPNGBDBM21130(U69,593 | N-methyl-N-(7-(1-pyrrolidinyl)-1-oxaspir...)
Affinity DataKd:  684nMAssay Description:Binding affinity against Mu opioid receptor using [35S]GTP-gamma-S, binding assay in guinea pig caudate membranes in unblocked conditionMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetKappa-type opioid receptor(Guinea pig)
Research Triangle Institute

Curated by ChEMBL
LigandPNGBDBM21130(U69,593 | N-methyl-N-(7-(1-pyrrolidinyl)-1-oxaspir...)
Affinity DataKd:  4.89E+3nMAssay Description:Binding affinity against kappa opioid receptor using [35S]GTP-gamma-S, binding assay in guinea pig caudate membranes blocked with 6 nM nor-BNIMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetDelta-type opioid receptor(Human)
Research Triangle Institute

Curated by ChEMBL
LigandPNGBDBM21130(U69,593 | N-methyl-N-(7-(1-pyrrolidinyl)-1-oxaspir...)
Affinity DataKd:  1.98E+3nMAssay Description:Binding affinity against Delta opioid receptor in using [35S]GTP-gamma-S, binding assay in guinea pig caudate membranes blocked with 20 nM NTIMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetMu-type opioid receptor(Guinea pig)
Research Triangle Institute

Curated by ChEMBL
LigandPNGBDBM21130(U69,593 | N-methyl-N-(7-(1-pyrrolidinyl)-1-oxaspir...)
Affinity DataKd:  2.14E+3nMAssay Description:Binding affinity against Mu opioid receptor using [35S]GTP-gamma-S, binding assay in guinea pig caudate membranes blocked with 6000 nM CTAPMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetMu-type opioid receptor(Human)
Astrazeneca R&D MöLndal

Curated by ChEMBL
LigandPNGBDBM21130(U69,593 | N-methyl-N-(7-(1-pyrrolidinyl)-1-oxaspir...)
Affinity DataIC50: 250nMAssay Description:Inhibition of [125I]Enkephalin binding to human mu opioid receptor from membranes of HEK293 cellsMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetDelta-type opioid receptor(Human)
Research Triangle Institute

Curated by ChEMBL
LigandPNGBDBM21130(U69,593 | N-methyl-N-(7-(1-pyrrolidinyl)-1-oxaspir...)
Affinity DataIC50: 5.80E+3nMAssay Description:Inhibition of [125I]deltorphin binding to human delta opioid receptor from membranes of HEK293 cellsMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetKappa-type opioid receptor(Human)
University of North Carolina

LigandPNGBDBM21130(U69,593 | N-methyl-N-(7-(1-pyrrolidinyl)-1-oxaspir...)
Affinity DataIC50: 2nMAssay Description:Inhibition of [125I]-(D-Pro10)-Dynorphin A binding to human kappa opioid receptor from membranes of HEK293 cellsMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetKappa-type opioid receptor(Rat)
University of Kansas Specialized Chemistry Center

Curated by ChEMBL
LigandPNGBDBM21130(U69,593 | N-methyl-N-(7-(1-pyrrolidinyl)-1-oxaspir...)
Affinity DataIC50: 0.630nMAssay Description:Binding affinity against rat kappa-opioid receptor expressed in CHO cells was determined by competitive inhibition of 2 nM [3H]-U 69593More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetKappa-type opioid receptor(Guinea pig)
Research Triangle Institute

Curated by ChEMBL
LigandPNGBDBM21130(U69,593 | N-methyl-N-(7-(1-pyrrolidinyl)-1-oxaspir...)
Affinity DataKd:  4.30nMAssay Description:Binding affinity at Opioid receptor kappa 1 in guinea pig brain membrane determined by using [3H]U-69593 as radioligandMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetKappa-type opioid receptor(Human)
University of North Carolina

LigandPNGBDBM21130(U69,593 | N-methyl-N-(7-(1-pyrrolidinyl)-1-oxaspir...)
Affinity DataEC50:  5.30nMAssay Description:Agonist activity at recombinant human kappa-type opioid receptor expressed in HEK293 cells after 30 mins by [35S]GTPgammaS binding assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetKappa-type opioid receptor(Human)
University of North Carolina

LigandPNGBDBM21130(U69,593 | N-methyl-N-(7-(1-pyrrolidinyl)-1-oxaspir...)
Affinity DataEC50:  52nMAssay Description:Agonist activity at human KOR expressed in CHO cells assessed as induction of beta-arrestin-2 recruitment by enzyme fragment complementation assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetKappa-type opioid receptor(Human)
University of North Carolina

LigandPNGBDBM21130(U69,593 | N-methyl-N-(7-(1-pyrrolidinyl)-1-oxaspir...)
Affinity DataEC50:  2.60nMAssay Description:Agonist activity at human KOR expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by HTRF assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetKappa-type opioid receptor(Human)
University of North Carolina

LigandPNGBDBM21130(U69,593 | N-methyl-N-(7-(1-pyrrolidinyl)-1-oxaspir...)
Affinity DataEC50:  205nMAssay Description:Agonist activity at human kappa opioid receptor expressed in human U2OS cells co-transfected with GFP and beta-arrestin-2 assessed as increase in bet...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
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