Compile Data Set for Download or QSAR
Report error Found 9 Enz. Inhib. hit(s) with Target = 'Kappa-type opioid receptor [D138N]'
TargetKappa-type opioid receptor [D138N](Human)
University of North Carolina

LigandPNGBDBM50001714(2-[3-cyclopropylmethyl-11-hydroxy-15-methoxy-13-ox...)
Affinity DataKd:  2nMpH: 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
PubMed
TargetKappa-type opioid receptor [D138N](Human)
University of North Carolina

LigandPNGBDBM50159165(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
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 Depth
Date in BDB:
3/1/2017
Entry Details Article
PubMed
TargetKappa-type opioid receptor [D138N](Human)
University of North Carolina

LigandPNGBDBM214798(YGGFLRRIRPKLK | Dynorphin A (1-17))
Affinity DataEC50:  1.90E+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 Depth
Date in BDB:
3/1/2017
Entry Details Article
PubMed
TargetKappa-type opioid receptor [D138N](Human)
University of North Carolina

LigandPNGBDBM214799(1xx)
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 Depth
Date in BDB:
3/1/2017
Entry Details Article
PubMed
TargetKappa-type opioid receptor [D138N](Human)
University of North Carolina

LigandPNGBDBM50159165(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
PubMed
TargetKappa-type opioid receptor [D138N](Human)
University of North Carolina

LigandPNGBDBM214799(1xx)
Affinity DataKi:  4nM ΔG°:  -47.9kJ/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
PubMed
TargetKappa-type opioid receptor [D138N](Human)
University of North Carolina

LigandPNGBDBM214798(YGGFLRRIRPKLK | Dynorphin A (1-17))
Affinity DataKi:  1.60E+3nM ΔG°:  -33.1kJ/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
PubMed
TargetKappa-type opioid receptor [D138N](Human)
University of North Carolina

LigandPNGBDBM21130(U69,593 | N-methyl-N-(7-(1-pyrrolidinyl)-1-oxaspir...)
Affinity DataKi:  4.40E+3nM ΔG°:  -30.6kJ/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
PubMed