Affinity DataKi: 0.00000600nM ΔG°: -82.5kJ/molepH: 5.5 T: 2°CAssay Description:The method was a competitive displacement assay used to determine binding affinities of other inhibitors relative to that of GW0385. The inhibitor of...More data for this Ligand-Target Pair
Affinity DataKi: 0.0000130nM ΔG°: -80.6kJ/molepH: 5.5 T: 2°CAssay Description:The method was a competitive displacement assay used to determine binding affinities of other inhibitors relative to that of GW0385. The inhibitor of...More data for this Ligand-Target Pair
Affinity DataKi: 0.0000150nM ΔG°: -80.2kJ/molepH: 5.5 T: 2°CAssay Description:The assay method employed kinetic determinations of values for k1 and k-1, from which value of inhibition constant (Ki ) was determined (k-1/k1). The...More data for this Ligand-Target Pair
Affinity DataKi: 0.000165nM ΔG°: -74.2kJ/molepH: 5.5 T: 2°CAssay Description:The method was a competitive displacement assay used to determine binding affinities of other inhibitors relative to that of GW0385. The inhibitor of...More data for this Ligand-Target Pair
TargetDimer of Gag-Pol polyprotein [489-587,M535I,L552P,A560V,V571F,I573V](Human immunodeficiency virus type 1)
Glaxosmithkline
Glaxosmithkline
Affinity DataKi: 0.000220nM ΔG°: -73.5kJ/molepH: 5.5 T: 2°CAssay Description:Enzymatic activity was determined with fluorogenic substrate in the presence and absence of inhibitor. The fluorescence increase due to hydrolysis of...More data for this Ligand-Target Pair
Affinity DataKi: 0.000240nM ΔG°: -73.2kJ/molepH: 5.5 T: 2°CAssay Description:The method was a competitive displacement assay used to determine binding affinities of other inhibitors relative to that of GW0385. The inhibitor of...More data for this Ligand-Target Pair
TargetDimer of Gag-Pol polyprotein [489-587,M535I,L552P,A560V,V571F,I573V](Human immunodeficiency virus type 1)
Glaxosmithkline
Glaxosmithkline
Affinity DataKi: 0.000420nM ΔG°: -71.8kJ/molepH: 5.5 T: 2°CAssay Description:Enzymatic activity was determined with fluorogenic substrate in the presence and absence of inhibitor. The fluorescence increase due to hydrolysis of...More data for this Ligand-Target Pair
TargetDimer of Gag-Pol polyprotein [489-587,M535I,L552P,A560V,V571F,I573V](Human immunodeficiency virus type 1)
Glaxosmithkline
Glaxosmithkline
Affinity DataKi: 0.000750nM ΔG°: -70.4kJ/molepH: 5.5 T: 2°CAssay Description:The assay method employed kinetic determinations of values for k1 and k-1, from which value of inhibition constant (Ki ) was determined (k-1/k1). The...More data for this Ligand-Target Pair
TargetDimer of Gag-Pol polyprotein [489-587,L499I,L508Q,K509R,E524D,M525I,S526N,M535I,I539V,I543V,I551V,L552P,A560V,V571A,L579M](Human immunodeficiency virus type 1)
Glaxosmithkline
Glaxosmithkline
Affinity DataKi: 0.00120nM ΔG°: -69.2kJ/molepH: 5.5 T: 2°CAssay Description:Enzymatic activity was determined with fluorogenic substrate in the presence and absence of inhibitor. The fluorescence increase due to hydrolysis of...More data for this Ligand-Target Pair
TargetDimer of Gag-Pol polyprotein [489-587,L499I,L508Q,K509R,E524D,M525I,S526N,M535I,I539V,I543V,I551V,L552P,A560V,V571A,L579M](Human immunodeficiency virus type 1)
Glaxosmithkline
Glaxosmithkline
Affinity DataKi: 0.00170nM ΔG°: -68.3kJ/molepH: 5.5 T: 2°CAssay Description:Enzymatic activity was determined with fluorogenic substrate in the presence and absence of inhibitor. The fluorescence increase due to hydrolysis of...More data for this Ligand-Target Pair
TargetDimer of Gag-Pol polyprotein [489-587,I539V](Human immunodeficiency virus type 1)
Glaxosmithkline
Glaxosmithkline
Affinity DataKi: 0.00200nM ΔG°: -67.9kJ/molepH: 5.5 T: 2°CAssay Description:The assay method employed kinetic determinations of values for k1 and k-1, from which value of inhibition constant (Ki ) was determined (k-1/k1). The...More data for this Ligand-Target Pair
TargetDimer of Gag-Pol polyprotein [489-587,L499I,L508Q,K509R,E524D,M525I,S526N,M535I,I539V,I543V,I551V,L552P,A560V,V571A,L579M](Human immunodeficiency virus type 1)
Glaxosmithkline
Glaxosmithkline
Affinity DataKi: 0.00240nM ΔG°: -67.4kJ/molepH: 5.5 T: 2°CAssay Description:Enzymatic activity was determined with fluorogenic substrate in the presence and absence of inhibitor. The fluorescence increase due to hydrolysis of...More data for this Ligand-Target Pair
TargetDimer of Gag-Pol polyprotein [489-587,I539V](Human immunodeficiency virus type 1)
Glaxosmithkline
Glaxosmithkline
Affinity DataKi: 0.00260nM ΔG°: -67.2kJ/molepH: 5.5 T: 2°CAssay Description:The method was a competitive displacement assay used to determine binding affinities of other inhibitors relative to that of GW0385. The inhibitor of...More data for this Ligand-Target Pair
TargetDimer of Gag-Pol polyprotein [489-587,L499I,L508Q,K509R,E524D,M525I,S526N,M535I,I539V,I543V,I551V,L552P,A560V,V571A,L579M](Human immunodeficiency virus type 1)
Glaxosmithkline
Glaxosmithkline
Affinity DataKi: 0.00340nM ΔG°: -66.6kJ/molepH: 5.5 T: 2°CAssay Description:The assay method employed kinetic determinations of values for k1 and k-1, from which value of inhibition constant (Ki ) was determined (k-1/k1). The...More data for this Ligand-Target Pair
TargetDimer of Gag-Pol polyprotein [489-587,I539V](Human immunodeficiency virus type 1)
Glaxosmithkline
Glaxosmithkline
Affinity DataKi: 0.00390nM ΔG°: -66.2kJ/molepH: 5.5 T: 2°CAssay Description:The method was a competitive displacement assay used to determine binding affinities of other inhibitors relative to that of GW0385. The inhibitor of...More data for this Ligand-Target Pair
TargetDimer of Gag-Pol polyprotein [489-587,M535I,L552P,A560V,V571F,I573V](Human immunodeficiency virus type 1)
Glaxosmithkline
Glaxosmithkline
Affinity DataKi: 0.00430nM ΔG°: -66.0kJ/molepH: 5.5 T: 2°CAssay Description:Enzymatic activity was determined with fluorogenic substrate in the presence and absence of inhibitor. The fluorescence increase due to hydrolysis of...More data for this Ligand-Target Pair
TargetDimer of Gag-Pol polyprotein [489-587,I539V](Human immunodeficiency virus type 1)
Glaxosmithkline
Glaxosmithkline
Affinity DataKi: 0.00460nM ΔG°: -65.8kJ/molepH: 5.5 T: 2°CAssay Description:The method was a competitive displacement assay used to determine binding affinities of other inhibitors relative to that of GW0385. The inhibitor of...More data for this Ligand-Target Pair
TargetDimer of Gag-Pol polyprotein [489-587,M535I,L552P,A560V,V571F,I573V](Human immunodeficiency virus type 1)
Glaxosmithkline
Glaxosmithkline
Affinity DataKi: 0.0250nM ΔG°: -61.5kJ/molepH: 5.5 T: 2°CAssay Description:Enzymatic activity was determined with fluorogenic substrate in the presence and absence of inhibitor. The fluorescence increase due to hydrolysis of...More data for this Ligand-Target Pair
TargetDimer of Gag-Pol polyprotein [489-587,I539V](Human immunodeficiency virus type 1)
Glaxosmithkline
Glaxosmithkline
Affinity DataKi: 0.0270nM ΔG°: -61.3kJ/molepH: 5.5 T: 2°CAssay Description:The method was a competitive displacement assay used to determine binding affinities of other inhibitors relative to that of GW0385. The inhibitor of...More data for this Ligand-Target Pair
TargetDimer of Gag-Pol polyprotein [489-587,L499I,L508Q,K509R,E524D,M525I,S526N,M535I,I539V,I543V,I551V,L552P,A560V,V571A,L579M](Human immunodeficiency virus type 1)
Glaxosmithkline
Glaxosmithkline
Affinity DataKi: 0.0544nM ΔG°: -59.6kJ/molepH: 5.5 T: 2°CAssay Description:Enzymatic activity was determined with fluorogenic substrate in the presence and absence of inhibitor. The fluorescence increase due to hydrolysis of...More data for this Ligand-Target Pair
Affinity DataKi: 0.0570nM ΔG°: -59.5kJ/molepH: 5.5 T: 2°CAssay Description:Enzymatic activity was determined with fluorogenic substrate in the presence and absence of inhibitor. The fluorescence increase due to hydrolysis of...More data for this Ligand-Target Pair
TargetGag-Pol polyprotein [489-587](Human immunodeficiency virus type 1)
Vertex Pharmaceuticals
Curated by ChEMBL
Vertex Pharmaceuticals
Curated by ChEMBL
Affinity DataKi: 0.5nMAssay Description:Compound was assayed for inhibition against HIV protease activityMore data for this Ligand-Target Pair
TargetGag-Pol polyprotein [489-587](Human immunodeficiency virus type 1)
Vertex Pharmaceuticals
Curated by ChEMBL
Vertex Pharmaceuticals
Curated by ChEMBL
Affinity DataKi: 0.600nMAssay Description:Compound was assayed for inhibition against HIV protease activityMore data for this Ligand-Target Pair
TargetDimer of Gag-Pol polyprotein [489-587,M535I,L552P,A560V,V571F,I573V](Human immunodeficiency virus type 1)
Glaxosmithkline
Glaxosmithkline
Affinity DataKi: 2.30nM ΔG°: -50.1kJ/molepH: 5.5 T: 2°CAssay Description:Enzymatic activity was determined with fluorogenic substrate in the presence and absence of inhibitor. The fluorescence increase due to hydrolysis of...More data for this Ligand-Target Pair
TargetDimer of Gag-Pol polyprotein [489-587,I539V](Human immunodeficiency virus type 1)
Glaxosmithkline
Glaxosmithkline
Affinity DataKi: 4.90nM ΔG°: -48.2kJ/molepH: 5.5 T: 2°CAssay Description:Enzymatic activity was determined with fluorogenic substrate in the presence and absence of inhibitor. The fluorescence increase due to hydrolysis of...More data for this Ligand-Target Pair
TargetGag-Pol polyprotein [489-587](Human immunodeficiency virus type 1)
Vertex Pharmaceuticals
Curated by ChEMBL
Vertex Pharmaceuticals
Curated by ChEMBL
Affinity DataKi: 15nMAssay Description:Compound was assayed for inhibition against HIV protease activityMore data for this Ligand-Target Pair
TargetGag-Pol polyprotein [489-587](Human immunodeficiency virus type 1)
Vertex Pharmaceuticals
Curated by ChEMBL
Vertex Pharmaceuticals
Curated by ChEMBL
Affinity DataKi: 17nMAssay Description:Compound was assayed for inhibition against HIV protease activityMore data for this Ligand-Target Pair
TargetGag-Pol polyprotein [489-587](Human immunodeficiency virus type 1)
Vertex Pharmaceuticals
Curated by ChEMBL
Vertex Pharmaceuticals
Curated by ChEMBL
Affinity DataKi: 17nMAssay Description:Compound was assayed for inhibition against HIV protease activityMore data for this Ligand-Target Pair
TargetDimer of Gag-Pol polyprotein [489-587,L499I,L508Q,K509R,E524D,M525I,S526N,M535I,I539V,I543V,I551V,L552P,A560V,V571A,L579M](Human immunodeficiency virus type 1)
Glaxosmithkline
Glaxosmithkline
Affinity DataKi: 58nM ΔG°: -42.0kJ/molepH: 5.5 T: 2°CAssay Description:Enzymatic activity was determined with fluorogenic substrate in the presence and absence of inhibitor. The fluorescence increase due to hydrolysis of...More data for this Ligand-Target Pair
TargetGag-Pol polyprotein [489-587](Human immunodeficiency virus type 1)
Vertex Pharmaceuticals
Curated by ChEMBL
Vertex Pharmaceuticals
Curated by ChEMBL
Affinity DataKi: 1.00E+3nMAssay Description:Compound was assayed for inhibition against HIV protease activityMore data for this Ligand-Target Pair
Affinity DataKi: 1.10E+3nMAssay Description:Inhibition of alpha1A adrenergic receptor (unknown origin)More data for this Ligand-Target Pair
TargetGag-Pol polyprotein [489-587](Human immunodeficiency virus type 1)
Vertex Pharmaceuticals
Curated by ChEMBL
Vertex Pharmaceuticals
Curated by ChEMBL
Affinity DataKi: 1.50E+3nMAssay Description:Compound was assayed for inhibition against HIV protease activityMore data for this Ligand-Target Pair
TargetAlpha-1A/Alpha-1B/Alpha-1D adrenergic receptor(Homo sapiens (Human))
Marquette University
Curated by ChEMBL
Marquette University
Curated by ChEMBL
Affinity DataKi: 1.80E+3nMAssay Description:Inhibition of alpha1 adrenergic receptor (unknown origin)More data for this Ligand-Target Pair
TargetProtein arginine N-methyltransferase 5(Homo sapiens (Human))
The Broad Institute Of Mit And Harvard
Curated by ChEMBL
The Broad Institute Of Mit And Harvard
Curated by ChEMBL
Affinity DataKi: 2.00E+3nMAssay Description:Covalent inhibition of human PRMT5 assessed as initial binding constant by LC-MS analysisMore data for this Ligand-Target Pair
Affinity DataKi: 2.50E+3nMAssay Description:Inhibition of PBR receptor (unknown origin)More data for this Ligand-Target Pair
TargetGag-Pol polyprotein [489-587](Human immunodeficiency virus type 1)
Vertex Pharmaceuticals
Curated by ChEMBL
Vertex Pharmaceuticals
Curated by ChEMBL
Affinity DataKi: 3.00E+3nMAssay Description:Compound was assayed for inhibition against HIV protease activityMore data for this Ligand-Target Pair
TargetAlpha-1A/Alpha-1B/Alpha-1D adrenergic receptor(Homo sapiens (Human))
Marquette University
Curated by ChEMBL
Marquette University
Curated by ChEMBL
Affinity DataKi: 3.90E+3nMAssay Description:Inhibition of alpha1 adrenergic receptor (unknown origin)More data for this Ligand-Target Pair
TargetProtein arginine N-methyltransferase 5(Homo sapiens (Human))
The Broad Institute Of Mit And Harvard
Curated by ChEMBL
The Broad Institute Of Mit And Harvard
Curated by ChEMBL
Affinity DataKi: 8.00E+3nMAssay Description:Covalent inhibition of human PRMT5 assessed as initial binding constant by LC-MS analysisMore data for this Ligand-Target Pair
TargetAlpha-1A/Alpha-1B/Alpha-1D adrenergic receptor(Homo sapiens (Human))
Marquette University
Curated by ChEMBL
Marquette University
Curated by ChEMBL
Affinity DataKi: >1.00E+4nMAssay Description:Inhibition of alpha1 adrenergic receptor (unknown origin)More data for this Ligand-Target Pair
Affinity DataKi: >1.00E+4nMAssay Description:Inhibition of D3 receptor (unknown origin)More data for this Ligand-Target Pair
TargetProtein arginine N-methyltransferase 5(Homo sapiens (Human))
The Broad Institute Of Mit And Harvard
Curated by ChEMBL
The Broad Institute Of Mit And Harvard
Curated by ChEMBL
Affinity DataKi: 1.90E+4nMAssay Description:Covalent inhibition of human PRMT5 assessed as initial binding constant by LC-MS analysisMore data for this Ligand-Target Pair
TargetProtein arginine N-methyltransferase 5(Homo sapiens (Human))
The Broad Institute Of Mit And Harvard
Curated by ChEMBL
The Broad Institute Of Mit And Harvard
Curated by ChEMBL
Affinity DataKi: 3.60E+4nMAssay Description:Covalent inhibition of human PRMT5 assessed as initial binding constant by LC-MS analysisMore data for this Ligand-Target Pair
TargetProtein arginine N-methyltransferase 5(Homo sapiens (Human))
The Broad Institute Of Mit And Harvard
Curated by ChEMBL
The Broad Institute Of Mit And Harvard
Curated by ChEMBL
Affinity DataKi: 4.20E+4nMAssay Description:Covalent inhibition of human PRMT5 assessed as initial binding constant by LC-MS analysisMore data for this Ligand-Target Pair
TargetProtein arginine N-methyltransferase 5(Homo sapiens (Human))
The Broad Institute Of Mit And Harvard
Curated by ChEMBL
The Broad Institute Of Mit And Harvard
Curated by ChEMBL
Affinity DataKi: 4.90E+4nMAssay Description:Covalent inhibition of human PRMT5 assessed as initial binding constant by LC-MS analysisMore data for this Ligand-Target Pair
TargetProtein arginine N-methyltransferase 5(Homo sapiens (Human))
The Broad Institute Of Mit And Harvard
Curated by ChEMBL
The Broad Institute Of Mit And Harvard
Curated by ChEMBL
Affinity DataKi: 5.80E+4nMAssay Description:Covalent inhibition of human PRMT5 assessed as initial binding constant by LC-MS analysisMore data for this Ligand-Target Pair
TargetProtein arginine N-methyltransferase 5(Homo sapiens (Human))
The Broad Institute Of Mit And Harvard
Curated by ChEMBL
The Broad Institute Of Mit And Harvard
Curated by ChEMBL
Affinity DataKi: 7.80E+4nMAssay Description:Covalent inhibition of human PRMT5 assessed as initial binding constant by LC-MS analysisMore data for this Ligand-Target Pair
Affinity DataIC50: 0.900nMT: 2°CAssay Description:For the biochemical assay panel, 50 nl of the test compounds, reference compounds and buffer/DMSO control are transferred to the respective wells of ...More data for this Ligand-Target Pair
Affinity DataIC50: 0.900nMAssay Description:To determine the HECT E3 ligase selectivity of the compounds, a panel of biochemical HECT E3 ligase autoubiquitinylation assays was employed (Smurf-1...More data for this Ligand-Target Pair
Affinity DataIC50: 1.40nMAssay Description:To determine the HECT E3 ligase selectivity of the compounds, a panel of biochemical HECT E3 ligase autoubiquitinylation assays was employed (Smurf-1...More data for this Ligand-Target Pair
Affinity DataIC50: 1.40nMT: 2°CAssay Description:For the biochemical assay panel, 50 nl of the test compounds, reference compounds and buffer/DMSO control are transferred to the respective wells of ...More data for this Ligand-Target Pair