Affinity DataKi: 0.123nMAssay Description:Displacement of 2-((1E,3E,5E)-5-(1-Ethyl-3,3-dimethyl-5-sulfoindolin-2-ylidene)-penta-1,3-dien-1-yl)-1-(6-((6-((6S,7R,7aR,12bS)-9-hydroxy-7-methoxy-3...More data for this Ligand-Target Pair
Affinity DataKi: 0.200nMAssay Description:Displacement of [3H]DAMGO from human MOR expressed in HEK293 cells preincubated for 1 hr followed by radioligand addition measured after 1 hr by liqu...More data for this Ligand-Target Pair
Affinity DataKi: 0.200nMAssay Description:Displacement of [3H]DAMGO from human MOR expressed in HEK293 cells preincubated for 1 hr followed by radioligand addition measured after 1 hr by liqu...More data for this Ligand-Target Pair
Affinity DataKi: 0.275nMAssay Description:Displacement of 2-((1E,3E,5E)-5-(1-Ethyl-3,3-dimethyl-5-sulfoindolin-2-ylidene)-penta-1,3-dien-1-yl)-1-(6-((6-((6S,7R,7aR,12bS)-9-hydroxy-7-methoxy-3...More data for this Ligand-Target Pair
Affinity DataKi: 1.10nMAssay Description:Displacement of 2-((1E,3E,5E)-5-(1-Ethyl-3,3-dimethyl-5-sulfoindolin-2-ylidene)-penta-1,3-dien-1-yl)-1-(6-((6-((6S,7R,7aR,12bS)-9-hydroxy-7-methoxy-3...More data for this Ligand-Target Pair
Affinity DataKi: 1.30nMAssay Description:Displacement of [3H]DAMGO from human MOR expressed in HEK293 cells preincubated for 1 hr followed by radioligand addition measured after 1 hr by liqu...More data for this Ligand-Target Pair
Affinity DataKi: 1.30nMAssay Description:Displacement of [3H]DAMGO from human MOR expressed in HEK293 cells preincubated for 1 hr followed by radioligand addition measured after 1 hr by liqu...More data for this Ligand-Target Pair
Affinity DataKi: 1.40nMAssay Description:Displacement of 2-((1E,3E,5E)-5-(1-Ethyl-3,3-dimethyl-5-sulfoindolin-2-ylidene)-penta-1,3-dien-1-yl)-1-(6-((6-((6S,7R,7aR,12bS)-9-hydroxy-7-methoxy-3...More data for this Ligand-Target Pair
Affinity DataKi: 1.60nMAssay Description:Displacement of [3H]DAMGO from human MOR expressed in HEK293 cells preincubated for 1 hr followed by radioligand addition measured after 1 hr by liqu...More data for this Ligand-Target Pair
Affinity DataKi: 1.60nMAssay Description:Displacement of [3H]diprenorphine from human MOR expressed in CHO-FlpIn cell membranes after 1 hr by liquid scintillation counting analysisMore data for this Ligand-Target Pair
Affinity DataKi: 2.20nMAssay Description:Displacement of [3H]diprenorphine from human MOR expressed in CHO-FlpIn cell membranes after 1 hr by liquid scintillation counting analysisMore data for this Ligand-Target Pair
Affinity DataKi: 3.20nMAssay Description:Displacement of [3H]DAMGO from human MOR expressed in HEK293 cells preincubated for 1 hr followed by radioligand addition measured after 1 hr by liqu...More data for this Ligand-Target Pair
Affinity DataKi: 7.40nMAssay Description:Displacement of [3H]diprenorphine from human MOR expressed in CHO-FlpIn cell membranes after 1 hr by liquid scintillation counting analysisMore data for this Ligand-Target Pair
Affinity DataKi: 19nMAssay Description:Displacement of 2-((1E,3E,5E)-5-(1-Ethyl-3,3-dimethyl-5-sulfoindolin-2-ylidene)-penta-1,3-dien-1-yl)-1-(6-((6-((6S,7R,7aR,12bS)-9-hydroxy-7-methoxy-3...More data for this Ligand-Target Pair
Affinity DataKi: 87nMAssay Description:Displacement of 2-((1E,3E,5E)-5-(1-Ethyl-3,3-dimethyl-5-sulfoindolin-2-ylidene)-penta-1,3-dien-1-yl)-1-(6-((6-((6S,7R,7aR,12bS)-9-hydroxy-7-methoxy-3...More data for this Ligand-Target Pair
Affinity DataKi: 107nMAssay Description:Displacement of [3H]diprenorphine from human MOR expressed in CHO-FlpIn cell membranes after 1 hr by liquid scintillation counting analysisMore data for this Ligand-Target Pair
Affinity DataKi: 195nMAssay Description:Displacement of [3H]diprenorphine from human MOR expressed in CHO-FlpIn cell membranes after 1 hr by liquid scintillation counting analysisMore data for this Ligand-Target Pair
Affinity DataKi: 263nMAssay Description:Displacement of [3H]diprenorphine from human MOR expressed in CHO-FlpIn cell membranes after 1 hr by liquid scintillation counting analysisMore data for this Ligand-Target Pair
Affinity DataKi: 2.04E+3nMAssay Description:Displacement of [3H]diprenorphine from human MOR expressed in CHO-FlpIn cell membranes after 1 hr by liquid scintillation counting analysisMore data for this Ligand-Target Pair
Affinity DataKi: 2.19E+3nMAssay Description:Displacement of [3H]diprenorphine from human MOR expressed in CHO-FlpIn cell membranes after 1 hr by liquid scintillation counting analysisMore data for this Ligand-Target Pair
Affinity DataIC50: 0.5nMpH: 7.2 T: 2°CAssay Description:The purified PKB beta enzyme was assayed with a peptide substrate and test compound in the presence of 30 uM ATP/ [gamma-33P]ATP in 96-well plates. I...More data for this Ligand-Target Pair
TargetMitogen-activated protein kinase 1(Homo sapiens (Human))
Astex Pharmaceuticals
Curated by ChEMBL
Astex Pharmaceuticals
Curated by ChEMBL
Affinity DataIC50: 2.10nMAssay Description:Inhibition of full length human N-terminal MAHHHHHH-tagged ERK2 expressed in Escherichia coli BL21 (DE3) using ATF2-GFP as substrate after 30 mins by...More data for this Ligand-Target Pair
TargetMitogen-activated protein kinase 1/3(Homo sapiens (Human))
Astex Pharmaceuticals
Curated by ChEMBL
Astex Pharmaceuticals
Curated by ChEMBL
Affinity DataIC50: 2.30nMAssay Description:Inhibition of ERK1/2 phosphorylation in human A375 cells harboring BRAF V600E mutant after 4 hrs by ELISAMore data for this Ligand-Target Pair
TargetMitogen-activated protein kinase 1(Homo sapiens (Human))
Astex Pharmaceuticals
Curated by ChEMBL
Astex Pharmaceuticals
Curated by ChEMBL
Affinity DataIC50: 2.5nMAssay Description:Inhibition of full length human N-terminal MAHHHHHH-tagged ERK2 expressed in Escherichia coli BL21 (DE3) using ATF2-GFP as substrate after 30 mins by...More data for this Ligand-Target Pair
TargetMitogen-activated protein kinase 1(Homo sapiens (Human))
Astex Pharmaceuticals
Curated by ChEMBL
Astex Pharmaceuticals
Curated by ChEMBL
Affinity DataIC50: 3nMAssay Description:Inhibition of full length human N-terminal MAHHHHHH-tagged ERK2 expressed in Escherichia coli BL21 (DE3) using ATF2-GFP as substrate after 30 mins by...More data for this Ligand-Target Pair
Affinity DataIC50: 3.5nMpH: 8.0Assay Description:IC50s for HG-9-91-01 derivatives were measured by Caliper-based mobility shift assay (PerkinElmer). For these experiments, full length His6-MBP...More data for this Ligand-Target Pair
TargetMitogen-activated protein kinase 1/3(Homo sapiens (Human))
Astex Pharmaceuticals
Curated by ChEMBL
Astex Pharmaceuticals
Curated by ChEMBL
Affinity DataIC50: 3.5nMAssay Description:Inhibition of ERK1/2 in human A375 cells harboring BRAF V600E mutant assessed as suppression of RSK phosphorylation after 4 hrs by MSD assayMore data for this Ligand-Target Pair
TargetMitogen-activated protein kinase 1(Homo sapiens (Human))
Astex Pharmaceuticals
Curated by ChEMBL
Astex Pharmaceuticals
Curated by ChEMBL
Affinity DataIC50: 4nMAssay Description:Inhibition of full length human N-terminal MAHHHHHH-tagged ERK2 expressed in Escherichia coli BL21 (DE3) using ATF2-GFP as substrate after 30 mins by...More data for this Ligand-Target Pair
TargetMitogen-activated protein kinase 1(Homo sapiens (Human))
Astex Pharmaceuticals
Curated by ChEMBL
Astex Pharmaceuticals
Curated by ChEMBL
Affinity DataIC50: 4.10nMAssay Description:Inhibition of full length human N-terminal MAHHHHHH-tagged ERK2 expressed in Escherichia coli BL21 (DE3) using ATF2-GFP as substrate after 30 mins by...More data for this Ligand-Target Pair
TargetMitogen-activated protein kinase 1(Homo sapiens (Human))
Astex Pharmaceuticals
Curated by ChEMBL
Astex Pharmaceuticals
Curated by ChEMBL
Affinity DataIC50: 4.20nMAssay Description:Inhibition of full length human N-terminal MAHHHHHH-tagged ERK2 expressed in Escherichia coli BL21 (DE3) using ATF2-GFP as substrate after 30 mins by...More data for this Ligand-Target Pair
TargetMitogen-activated protein kinase 1(Homo sapiens (Human))
Astex Pharmaceuticals
Curated by ChEMBL
Astex Pharmaceuticals
Curated by ChEMBL
Affinity DataIC50: 4.30nMAssay Description:Inhibition of full length human N-terminal MAHHHHHH-tagged ERK2 expressed in Escherichia coli BL21 (DE3) using ATF2-GFP as substrate after 30 mins by...More data for this Ligand-Target Pair
Affinity DataIC50: 6nMpH: 8.0Assay Description:IC50s for HG-9-91-01 derivatives were measured by Caliper-based mobility shift assay (PerkinElmer). For these experiments, full length His6-MBP...More data for this Ligand-Target Pair
TargetMitogen-activated protein kinase 1(Homo sapiens (Human))
Astex Pharmaceuticals
Curated by ChEMBL
Astex Pharmaceuticals
Curated by ChEMBL
Affinity DataIC50: 7.90nMAssay Description:Inhibition of full length human N-terminal MAHHHHHH-tagged ERK2 expressed in Escherichia coli BL21 (DE3) using ATF2-GFP as substrate after 30 mins by...More data for this Ligand-Target Pair
TargetMitogen-activated protein kinase 1(Homo sapiens (Human))
Astex Pharmaceuticals
Curated by ChEMBL
Astex Pharmaceuticals
Curated by ChEMBL
Affinity DataIC50: 11nMAssay Description:Inhibition of full length human N-terminal MAHHHHHH-tagged ERK2 expressed in Escherichia coli BL21 (DE3) using ATF2-GFP as substrate after 30 mins by...More data for this Ligand-Target Pair
Affinity DataIC50: 19.5nMpH: 8.0Assay Description:IC50s for HG-9-91-01 derivatives were measured by Caliper-based mobility shift assay (PerkinElmer). For these experiments, full length His6-MBP...More data for this Ligand-Target Pair
TargetMitogen-activated protein kinase 1(Homo sapiens (Human))
Astex Pharmaceuticals
Curated by ChEMBL
Astex Pharmaceuticals
Curated by ChEMBL
Affinity DataIC50: 21nMAssay Description:Inhibition of full length human N-terminal MAHHHHHH-tagged ERK2 expressed in Escherichia coli BL21 (DE3) using ATF2-GFP as substrate after 30 mins by...More data for this Ligand-Target Pair
TargetMitogen-activated protein kinase 1(Homo sapiens (Human))
Astex Pharmaceuticals
Curated by ChEMBL
Astex Pharmaceuticals
Curated by ChEMBL
Affinity DataIC50: 24nMAssay Description:Inhibition of full length human N-terminal MAHHHHHH-tagged ERK2 expressed in Escherichia coli BL21 (DE3) using ATF2-GFP as substrate after 30 mins by...More data for this Ligand-Target Pair
TargetMitogen-activated protein kinase 1(Homo sapiens (Human))
Astex Pharmaceuticals
Curated by ChEMBL
Astex Pharmaceuticals
Curated by ChEMBL
Affinity DataIC50: 26nMAssay Description:Inhibition of full length human N-terminal MAHHHHHH-tagged ERK2 expressed in Escherichia coli BL21 (DE3) using ATF2-GFP as substrate after 30 mins by...More data for this Ligand-Target Pair
Affinity DataIC50: 27nMpH: 7.2 T: 2°CAssay Description:The recombinant alpha catalytic subunit of bovine PKA was assayed with a peptide substrate and test compound in the presence of 40 uM ATP/ [gamma-33P...More data for this Ligand-Target Pair
Affinity DataIC50: 34nMpH: 8.0Assay Description:IC50s for HG-9-91-01 derivatives were measured by Caliper-based mobility shift assay (PerkinElmer). For these experiments, full length His6-MBP...More data for this Ligand-Target Pair
TargetMitogen-activated protein kinase 1(Homo sapiens (Human))
Astex Pharmaceuticals
Curated by ChEMBL
Astex Pharmaceuticals
Curated by ChEMBL
Affinity DataIC50: 40nMAssay Description:Inhibition of full length human N-terminal MAHHHHHH-tagged ERK2 expressed in Escherichia coli BL21 (DE3) using ATF2-GFP as substrate after 30 mins by...More data for this Ligand-Target Pair
Affinity DataIC50: 40nMpH: 8.0Assay Description:IC50s for HG-9-91-01 derivatives were measured by Caliper-based mobility shift assay (PerkinElmer). For these experiments, full length His6-MBP...More data for this Ligand-Target Pair
TargetMitogen-activated protein kinase 1(Homo sapiens (Human))
Astex Pharmaceuticals
Curated by ChEMBL
Astex Pharmaceuticals
Curated by ChEMBL
Affinity DataIC50: 68nMAssay Description:Inhibition of full length human N-terminal MAHHHHHH-tagged ERK2 expressed in Escherichia coli BL21 (DE3) using ATF2-GFP as substrate after 30 mins by...More data for this Ligand-Target Pair
Affinity DataIC50: 100nM Kd: 62nMT: 2°CAssay Description:The protease activity of the full-length NS3-NS4a and the protease domain were measured using a FRET-based assay using a peptide substrate derived fr...More data for this Ligand-Target Pair
Affinity DataIC50: 150nMpH: 8.0Assay Description:IC50s for HG-9-91-01 derivatives were measured by Caliper-based mobility shift assay (PerkinElmer). For these experiments, full length His6-MBP...More data for this Ligand-Target Pair
Affinity DataIC50: 170nMpH: 7.2 T: 2°CAssay Description:The recombinant alpha catalytic subunit of bovine PKA was assayed with a peptide substrate and test compound in the presence of 40 uM ATP/ [gamma-33P...More data for this Ligand-Target Pair
Affinity DataIC50: 230nMpH: 7.2 T: 2°CAssay Description:The purified PKB beta enzyme was assayed with a peptide substrate and test compound in the presence of 30 uM ATP/ [gamma-33P]ATP in 96-well plates. I...More data for this Ligand-Target Pair
TargetMitogen-activated protein kinase 1(Homo sapiens (Human))
Astex Pharmaceuticals
Curated by ChEMBL
Astex Pharmaceuticals
Curated by ChEMBL
Affinity DataIC50: 420nMAssay Description:Inhibition of full length human N-terminal MAHHHHHH-tagged ERK2 expressed in Escherichia coli BL21 (DE3) using ATF2-GFP as substrate after 30 mins by...More data for this Ligand-Target Pair
TargetMitogen-activated protein kinase 1/3(Homo sapiens (Human))
Astex Pharmaceuticals
Curated by ChEMBL
Astex Pharmaceuticals
Curated by ChEMBL
Affinity DataIC50: 630nMAssay Description:Inhibition of ERK1/2 in human A375 cells harboring BRAF V600E mutant assessed as suppression of RSK phosphorylation after 4 hrs by MSD assayMore data for this Ligand-Target Pair
Affinity DataIC50: 1.30E+3nMT: 2°CAssay Description:The protease activity of the full-length NS3-NS4a and the protease domain were measured using a FRET-based assay using a peptide substrate derived fr...More data for this Ligand-Target Pair