Compile Data Set for Download or QSAR
Report error Found 117 Enz. Inhib. hit(s) for PDB: 9UXU
TargetKappa-type opioid receptor(Human)
Universit£T M£Nster

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 50159165BDBM50159165(2S,4aR,6a(R,7R,9S,10aS,10bR)-9-(acetyloxy)-2-(fura...)
Affinity DataEC50:  0.0150nMAssay Description:Agonist activity at human KOR expressed in HEK293T cells assessed as inhibition of Galphai-mediated cAMP accumulation after 15 mins by microbeta coun...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/22/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetKappa-type opioid receptor(Human)
Universit£T M£Nster

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 50159165BDBM50159165(2S,4aR,6a(R,7R,9S,10aS,10bR)-9-(acetyloxy)-2-(fura...)
Affinity DataEC50:  0.0300nMAssay Description:Agonist activity at human KOR expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by lumi...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/23/2022
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetKappa-type opioid receptor [D138N](Human)
University of North Carolina

LigandChemical structure of BindingDB Monomer ID 50159165BDBM50159165(2S,4aR,6a(R,7R,9S,10aS,10bR)-9-(acetyloxy)-2-(fura...)
Affinity DataEC50:  0.0300nMpH: 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 Depth
Date in BDB:
3/1/2017
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetKappa-type opioid receptor(Human)
Universit£T M£Nster

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 50159165BDBM50159165(2S,4aR,6a(R,7R,9S,10aS,10bR)-9-(acetyloxy)-2-(fura...)
Affinity DataEC50:  0.0300nMAssay 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 Depth
Date in BDB:
3/13/2016
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetKappa-type opioid receptor [M226A](Human)
University of North Carolina

LigandChemical structure of BindingDB Monomer ID 50159165BDBM50159165(2S,4aR,6a(R,7R,9S,10aS,10bR)-9-(acetyloxy)-2-(fura...)
Affinity DataEC50:  0.0370nMpH: 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 Depth
Date in BDB:
3/1/2017
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetKappa-type opioid receptor(Human)
Universit£T M£Nster

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 50159165BDBM50159165(2S,4aR,6a(R,7R,9S,10aS,10bR)-9-(acetyloxy)-2-(fura...)
Affinity DataEC50:  0.0400nMAssay Description:Agonist activity at human kappa opiod receptor expressed in CHO-K1 cells assessed as increase in forskolin induced cAMP production measured after 30 ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/27/2022
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetKappa-type opioid receptor(Human)
Universit£T M£Nster

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 50159165BDBM50159165(2S,4aR,6a(R,7R,9S,10aS,10bR)-9-(acetyloxy)-2-(fura...)
Affinity DataEC50:  0.0420nMAssay Description:Agonist activity at human kappa-type opioid receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/16/2020
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetKappa-type opioid receptor [I294A](Human)
University of North Carolina

LigandChemical structure of BindingDB Monomer ID 50159165BDBM50159165(2S,4aR,6a(R,7R,9S,10aS,10bR)-9-(acetyloxy)-2-(fura...)
Affinity DataEC50:  0.0870nMpH: 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 Depth
Date in BDB:
3/1/2017
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetKappa-type opioid receptor [K200A](Human)
University of North Carolina

LigandChemical structure of BindingDB Monomer ID 50159165BDBM50159165(2S,4aR,6a(R,7R,9S,10aS,10bR)-9-(acetyloxy)-2-(fura...)
Affinity DataEC50:  0.0930nMpH: 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 Depth
Date in BDB:
3/1/2017
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetKappa-type opioid receptor [E297A](Human)
University of North Carolina

LigandChemical structure of BindingDB Monomer ID 50159165BDBM50159165(2S,4aR,6a(R,7R,9S,10aS,10bR)-9-(acetyloxy)-2-(fura...)
Affinity DataEC50:  0.120nMpH: 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 Depth
Date in BDB:
3/1/2017
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetKappa-type opioid receptor(Human)
Universit£T M£Nster

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 50159165BDBM50159165(2S,4aR,6a(R,7R,9S,10aS,10bR)-9-(acetyloxy)-2-(fura...)
Affinity DataEC50:  0.130nMpH: 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 Depth
Date in BDB:
3/1/2017
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetKappa-type opioid receptor [Y139F](Human)
University of North Carolina

LigandChemical structure of BindingDB Monomer ID 50159165BDBM50159165(2S,4aR,6a(R,7R,9S,10aS,10bR)-9-(acetyloxy)-2-(fura...)
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 Depth
Date in BDB:
3/1/2017
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetKappa-type opioid receptor(Human)
Universit£T M£Nster

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 50159165BDBM50159165(2S,4aR,6a(R,7R,9S,10aS,10bR)-9-(acetyloxy)-2-(fura...)
Affinity DataEC50:  0.200nMAssay Description:Displacement of [3H]U69593 from kappa opioid receptor expressed in HEK293 cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/22/2011
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetKappa-type opioid receptor(Human)
Universit£T M£Nster

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 50159165BDBM50159165(2S,4aR,6a(R,7R,9S,10aS,10bR)-9-(acetyloxy)-2-(fura...)
Affinity DataEC50:  0.210nMAssay Description:Agonist activity at human kappa-type opioid receptor expressed in CHO-K1 cells assessed as forskolin-induced cAMP accumulation after 30 mins in prese...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/13/2020
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetKappa-type opioid receptor [Y313F](Human)
University of North Carolina

LigandChemical structure of BindingDB Monomer ID 50159165BDBM50159165(2S,4aR,6a(R,7R,9S,10aS,10bR)-9-(acetyloxy)-2-(fura...)
Affinity DataEC50:  0.280nMpH: 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 Depth
Date in BDB:
3/1/2017
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetKappa-type opioid receptor [Y312F](Human)
University of North Carolina

LigandChemical structure of BindingDB Monomer ID 50159165BDBM50159165(2S,4aR,6a(R,7R,9S,10aS,10bR)-9-(acetyloxy)-2-(fura...)
Affinity DataEC50:  0.280nMpH: 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 Depth
Date in BDB:
3/1/2017
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetKappa-type opioid receptor [D138A](Human)
University of North Carolina

LigandChemical structure of BindingDB Monomer ID 50159165BDBM50159165(2S,4aR,6a(R,7R,9S,10aS,10bR)-9-(acetyloxy)-2-(fura...)
Affinity DataEC50:  0.300nMpH: 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 Depth
Date in BDB:
3/1/2017
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetKappa-type opioid receptor(Human)
Universit£T M£Nster

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 50159165BDBM50159165(2S,4aR,6a(R,7R,9S,10aS,10bR)-9-(acetyloxy)-2-(fura...)
Affinity DataEC50:  0.360nMAssay Description:Inhibition of human kappa opioid receptor expressed in HEK293T cells assessed as inhibition of cAMP production after 30 minsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/7/2016
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetKappa-type opioid receptor [K227A](Human)
University of North Carolina

LigandChemical structure of BindingDB Monomer ID 50159165BDBM50159165(2S,4aR,6a(R,7R,9S,10aS,10bR)-9-(acetyloxy)-2-(fura...)
Affinity DataEC50:  0.510nMpH: 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 Depth
Date in BDB:
3/1/2017
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetKappa-type opioid receptor [Y119F](Human)
University of North Carolina

LigandChemical structure of BindingDB Monomer ID 50159165BDBM50159165(2S,4aR,6a(R,7R,9S,10aS,10bR)-9-(acetyloxy)-2-(fura...)
Affinity DataEC50:  0.520nMpH: 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 Depth
Date in BDB:
3/1/2017
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetKappa-type opioid receptor [D138N](Human)
University of North Carolina

LigandChemical structure of BindingDB Monomer ID 50159165BDBM50159165(2S,4aR,6a(R,7R,9S,10aS,10bR)-9-(acetyloxy)-2-(fura...)
Affinity DataKi:  0.590nM ΔG°:  -52.7kJ/molepH: 7.4 T: 2°CAssay Description:Radioligand binding assays were performed as previously detailed [Yan et al., Biochemistry, 48:6898-6908]. In brief, crude cell membranes were prepar...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/1/2017
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetKappa-type opioid receptor(Human)
Universit£T M£Nster

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 50159165BDBM50159165(2S,4aR,6a(R,7R,9S,10aS,10bR)-9-(acetyloxy)-2-(fura...)
Affinity DataKi:  0.75nMAssay Description:Displacement of [3H]U69593 from kappa opioid receptor expressed in HEK293 cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/22/2011
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetKappa-type opioid receptor(Rat)
University of Mississippi

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 50159165BDBM50159165(2S,4aR,6a(R,7R,9S,10aS,10bR)-9-(acetyloxy)-2-(fura...)
Affinity DataKi:  0.75nMAssay Description:Displacement of [3H]U-69593 from rat cloned KORMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetKappa-type opioid receptor(Human)
Universit£T M£Nster

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 50159165BDBM50159165(2S,4aR,6a(R,7R,9S,10aS,10bR)-9-(acetyloxy)-2-(fura...)
Affinity DataKi:  0.800nMAssay Description:Displacement of [3H]U69593 from kappa opioid receptor expressed in HEK293 cells by visible spectrophotometryMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/27/2012
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetKappa-type opioid receptor(Human)
Universit£T M£Nster

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 50159165BDBM50159165(2S,4aR,6a(R,7R,9S,10aS,10bR)-9-(acetyloxy)-2-(fura...)
Affinity DataEC50:  0.810nMAssay Description:Agonist activity at human kappa opioid receptor-Galpha-16 fusion protein expressed in CHO cells by calcium flux assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
1/11/2010
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetKappa-type opioid receptor [Y66A](Human)
University of North Carolina

LigandChemical structure of BindingDB Monomer ID 50159165BDBM50159165(2S,4aR,6a(R,7R,9S,10aS,10bR)-9-(acetyloxy)-2-(fura...)
Affinity DataEC50:  0.980nMpH: 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 Depth
Date in BDB:
3/1/2017
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetKappa-type opioid receptor(Human)
Universit£T M£Nster

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 50159165BDBM50159165(2S,4aR,6a(R,7R,9S,10aS,10bR)-9-(acetyloxy)-2-(fura...)
Affinity DataEC50:  1.24nMAssay Description:Agonist activity at human kappa opioid receptor assessed as inhibition of Galpha-16-induced calcium fluxMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetKappa-type opioid receptor(Human)
Universit£T M£Nster

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 50159165BDBM50159165(2S,4aR,6a(R,7R,9S,10aS,10bR)-9-(acetyloxy)-2-(fura...)
Affinity DataKi:  1.30nMAssay Description:Displacement of [3H]diprenorphine from human kappa opioid receptor expressed in CHO cell membranesMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/9/2016
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetKappa-type opioid receptor(Human)
Universit£T M£Nster

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 50159165BDBM50159165(2S,4aR,6a(R,7R,9S,10aS,10bR)-9-(acetyloxy)-2-(fura...)
Affinity DataKi:  1.30nMAssay Description:Displacement of [3H]diprenorphine binding from human kappa opioid receptor expressed in CHO cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetKappa-type opioid receptor(Human)
Universit£T M£Nster

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 50159165BDBM50159165(2S,4aR,6a(R,7R,9S,10aS,10bR)-9-(acetyloxy)-2-(fura...)
Affinity DataKi:  1.30nMAssay Description:Inhibition of [3H]diprenorphine binding to human KOR expressed in CHO cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetKappa-type opioid receptor(Human)
Universit£T M£Nster

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 50159165BDBM50159165(2S,4aR,6a(R,7R,9S,10aS,10bR)-9-(acetyloxy)-2-(fura...)
Affinity DataKi:  1.30nMAssay Description:Inhibition of [3H]diprenorphine binding to human KOR expressed in CHO cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetKappa-type opioid receptor [H291F](Human)
University of North Carolina

LigandChemical structure of BindingDB Monomer ID 50159165BDBM50159165(2S,4aR,6a(R,7R,9S,10aS,10bR)-9-(acetyloxy)-2-(fura...)
Affinity DataEC50:  1.60nMpH: 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 Depth
Date in BDB:
3/1/2017
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetKappa-type opioid receptor(Human)
Universit£T M£Nster

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 50159165BDBM50159165(2S,4aR,6a(R,7R,9S,10aS,10bR)-9-(acetyloxy)-2-(fura...)
Affinity DataEC50:  1.70nMAssay Description:Agonist activity at human kappa opioid receptor expressed CHO cells co-expressing Galphaq16 assessed as calcium mobilization by fluorescence assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/20/2016
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetKappa-type opioid receptor(Human)
Universit£T M£Nster

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 50159165BDBM50159165(2S,4aR,6a(R,7R,9S,10aS,10bR)-9-(acetyloxy)-2-(fura...)
Affinity DataEC50:  1.80nMAssay 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 Depth
Date in BDB:
12/15/2012
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetKappa-type opioid receptor(Human)
Universit£T M£Nster

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 50159165BDBM50159165(2S,4aR,6a(R,7R,9S,10aS,10bR)-9-(acetyloxy)-2-(fura...)
Affinity DataKi:  1.90nMAssay Description:Inhibition of [125I]- IOXY binding to human Opioid receptor kappa1More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetKappa-type opioid receptor(Human)
Universit£T M£Nster

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 50159165BDBM50159165(2S,4aR,6a(R,7R,9S,10aS,10bR)-9-(acetyloxy)-2-(fura...)
Affinity DataKi:  1.90nMAssay Description:Agonist activity at human recombinant kappa opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/15/2012
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetKappa-type opioid receptor(Human)
Universit£T M£Nster

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 50159165BDBM50159165(2S,4aR,6a(R,7R,9S,10aS,10bR)-9-(acetyloxy)-2-(fura...)
Affinity DataKi:  1.90nMAssay Description:Displacement of [125]OXY from kappa opioid receptorMore data for this Ligand-Target Pair
In Depth
Date in BDB:
1/11/2010
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetKappa-type opioid receptor(Human)
Universit£T M£Nster

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 50159165BDBM50159165(2S,4aR,6a(R,7R,9S,10aS,10bR)-9-(acetyloxy)-2-(fura...)
Affinity DataKi:  1.90nMAssay Description:Displacement of [3H]-U69593 human KOR receptor at 10 uM by cell-based radioligand binding assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/6/2026
Entry Details
PubMedPDB3D3D Structure (crystal)
TargetKappa-type opioid receptor(Human)
Universit£T M£Nster

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 50159165BDBM50159165(2S,4aR,6a(R,7R,9S,10aS,10bR)-9-(acetyloxy)-2-(fura...)
Affinity DataKi:  1.90nMAssay Description:Binding affinity to kappa opioid receptorMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/31/2012
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetKappa-type opioid receptor(Human)
Universit£T M£Nster

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 50159165BDBM50159165(2S,4aR,6a(R,7R,9S,10aS,10bR)-9-(acetyloxy)-2-(fura...)
Affinity DataKi:  1.90nMAssay Description:Displacement of [125I]IOXY from human recombinant kappa opioid receptor expressed in CHO cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/15/2012
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetKappa-type opioid receptor(Human)
Universit£T M£Nster

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 50159165BDBM50159165(2S,4aR,6a(R,7R,9S,10aS,10bR)-9-(acetyloxy)-2-(fura...)
Affinity DataEC50:  2.10nMAssay Description:Agonist activity at human KOPR expressed in CHO cells assessed as enhancement of [35S]GTPgammaS bindingMore data for this Ligand-Target Pair
In Depth
Date in BDB:
1/11/2010
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetKappa-type opioid receptor(Human)
Universit£T M£Nster

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 50159165BDBM50159165(2S,4aR,6a(R,7R,9S,10aS,10bR)-9-(acetyloxy)-2-(fura...)
Affinity DataEC50:  2.20nMAssay Description:Displacement of [35S]GTPgammaS binding from human KOR assessed as inhibition constantMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/18/2024
Entry Details
PubMedPDB3D3D Structure (crystal)
TargetKappa-type opioid receptor(Human)
Universit£T M£Nster

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 50159165BDBM50159165(2S,4aR,6a(R,7R,9S,10aS,10bR)-9-(acetyloxy)-2-(fura...)
Affinity DataKi:  2.40nMAssay Description:Displacement of [3H]diprenorphine from human kappa opioid receptor expressed in CHO cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/15/2012
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetKappa-type opioid receptor(Human)
Universit£T M£Nster

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 50159165BDBM50159165(2S,4aR,6a(R,7R,9S,10aS,10bR)-9-(acetyloxy)-2-(fura...)
Affinity DataKi:  2.5nMAssay Description:Displacement of [3H]diprenorphine from human KOPR expressed in CHO cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
1/11/2010
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetKappa-type opioid receptor [Q115A](Human)
University of North Carolina

LigandChemical structure of BindingDB Monomer ID 50159165BDBM50159165(2S,4aR,6a(R,7R,9S,10aS,10bR)-9-(acetyloxy)-2-(fura...)
Affinity DataEC50:  2.60nMpH: 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 Depth
Date in BDB:
3/1/2017
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetKappa-type opioid receptor(Human)
Universit£T M£Nster

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 50159165BDBM50159165(2S,4aR,6a(R,7R,9S,10aS,10bR)-9-(acetyloxy)-2-(fura...)
Affinity DataKi:  2.70nMAssay Description:Binding affinity to human Kappa-opioid receptor expressed in CHO cell membrane assessed as inhibition of [3H]-U69593 binding to KOR by measuring inhi...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/12/2025
Entry Details
PubMedPDB3D3D Structure (crystal)
TargetKappa-type opioid receptor(Human)
Universit£T M£Nster

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 50159165BDBM50159165(2S,4aR,6a(R,7R,9S,10aS,10bR)-9-(acetyloxy)-2-(fura...)
Affinity DataEC50:  2.82nMAssay Description:Activity at human kappa opioid receptor expressed in HEK293 cells as intracellular calcium mobilizationMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetKappa-type opioid receptor(Human)
Universit£T M£Nster

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 50159165BDBM50159165(2S,4aR,6a(R,7R,9S,10aS,10bR)-9-(acetyloxy)-2-(fura...)
Affinity DataKi:  2.90nMAssay Description:Displacement of [3H]U69593 from kappa opioid receptor (unknown origin) expressed in HEK293T cells after 1.5 hrs by radioligand binding assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/7/2016
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetKappa-type opioid receptor(Human)
Universit£T M£Nster

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 50159165BDBM50159165(2S,4aR,6a(R,7R,9S,10aS,10bR)-9-(acetyloxy)-2-(fura...)
Affinity DataKi:  3nMAssay Description:Displacement of [3H]diprenorphine from human KOPR expressed in CHO cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/22/2012
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetKappa-type opioid receptor [D138A](Human)
University of North Carolina

LigandChemical structure of BindingDB Monomer ID 50159165BDBM50159165(2S,4aR,6a(R,7R,9S,10aS,10bR)-9-(acetyloxy)-2-(fura...)
Affinity DataKi:  3.5nM ΔG°:  -48.3kJ/molepH: 7.4 T: 2°CAssay Description:Radioligand binding assays were performed as previously detailed [Yan et al., Biochemistry, 48:6898-6908]. In brief, crude cell membranes were prepar...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/1/2017
Entry Details Article
PubMedPDB3D3D Structure (crystal)
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