Compile Data Set for Download or QSAR
Found 69 Enz. Inhib. hit(s) with all data for entry = 1903
TargetAngiopoietin-1 receptor(Homo sapiens (Human))
Amgen Inc

LigandPNGBDBM14948(4-Methyl-3-(3-(2-(methylamino)pyrimidin-4-yl)pyrid...)
Show SMILES CNc1nccc(n1)-c1cccnc1Oc1cc(ccc1C)C(=O)Nc1cccc(c1)C(F)(F)F
Show InChI InChI=1S/C25H20F3N5O2/c1-15-8-9-16(22(34)32-18-6-3-5-17(14-18)25(26,27)28)13-21(15)35-23-19(7-4-11-30-23)20-10-12-31-24(29-2)33-20/h3-14H,1-2H3,(H,32,34)(H,29,31,33)
Affinity DataIC50: 1nMpH: 7.5 T: 2°CAssay Description:The assay uses purified enzyme interacting with biotinylated peptide substrate. HTRF is based on the proximity of europium cryptate (donor fluorophor...More data for this Ligand-Target Pair
TargetTyrosine-protein kinase Lck [245-498](Homo sapiens (Human))
Amgen Inc

LigandPNGBDBM14969(4-Methyl-3-(2-(quinolin-3-yl)ethynyl)-N-(3-(triflu...)
Show SMILES Cc1ccc(cc1C#Cc1cnc2ccccc2c1)C(=O)Nc1cccc(c1)C(F)(F)F
Show InChI InChI=1S/C26H17F3N2O/c1-17-9-11-21(25(32)31-23-7-4-6-22(15-23)26(27,28)29)14-19(17)12-10-18-13-20-5-2-3-8-24(20)30-16-18/h2-9,11,13-16H,1H3,(H,31,32)
Affinity DataIC50: 1nMAssay Description:The assay uses purified enzyme interacting with biotinylated peptide substrate. HTRF is based on the proximity of europium cryptate (donor fluorophor...More data for this Ligand-Target Pair
TargetAngiopoietin-1 receptor(Homo sapiens (Human))
Amgen Inc

LigandPNGBDBM14949(2-aminoquinazoline 5 | 3-(2-aminoquinazolin-6-yl)-...)
Show SMILES Cc1ccc(cc1-c1ccc2nc(N)ncc2c1)C(=O)Nc1cccc(c1)C(F)(F)F
Show InChI InChI=1S/C23H17F3N4O/c1-13-5-6-15(21(31)29-18-4-2-3-17(11-18)23(24,25)26)10-19(13)14-7-8-20-16(9-14)12-28-22(27)30-20/h2-12H,1H3,(H,29,31)(H2,27,28,30)
Affinity DataIC50: 1nMpH: 7.5 T: 2°CAssay Description:The assay uses purified enzyme interacting with biotinylated peptide substrate. HTRF is based on the proximity of europium cryptate (donor fluorophor...More data for this Ligand-Target Pair
TargetTyrosine-protein kinase Lck [245-498](Homo sapiens (Human))
Amgen Inc

LigandPNGBDBM14967(3-(2-(3H-Imidazo[4,5-b]pyridin-6-yl)ethynyl)-4-met...)
Show SMILES Cc1ccc(cc1C#Cc1cnc2nc[nH]c2c1)C(=O)Nc1cccc(c1)C(F)(F)F
Show InChI InChI=1S/C23H15F3N4O/c1-14-5-7-17(22(31)30-19-4-2-3-18(11-19)23(24,25)26)10-16(14)8-6-15-9-20-21(27-12-15)29-13-28-20/h2-5,7,9-13H,1H3,(H,30,31)(H,27,28,29)
Affinity DataIC50: 1nMAssay Description:The assay uses purified enzyme interacting with biotinylated peptide substrate. HTRF is based on the proximity of europium cryptate (donor fluorophor...More data for this Ligand-Target Pair
TargetTyrosine-protein kinase Lck [245-498](Homo sapiens (Human))
Amgen Inc

LigandPNGBDBM14966(3-(2-(6-Aminopyridin-3-yl)ethynyl)-4-methyl-N-(3-(...)
Show SMILES Cc1ccc(cc1C#Cc1ccc(N)nc1)C(=O)Nc1cccc(c1)C(F)(F)F
Show InChI InChI=1S/C22H16F3N3O/c1-14-5-8-17(11-16(14)9-6-15-7-10-20(26)27-13-15)21(29)28-19-4-2-3-18(12-19)22(23,24)25/h2-5,7-8,10-13H,1H3,(H2,26,27)(H,28,29)
Affinity DataIC50: 1nMAssay Description:The assay uses purified enzyme interacting with biotinylated peptide substrate. HTRF is based on the proximity of europium cryptate (donor fluorophor...More data for this Ligand-Target Pair
TargetTyrosine-protein kinase Lck [245-498](Homo sapiens (Human))
Amgen Inc

LigandPNGBDBM14950(3-(2-(2-Aminopyrimidin-5-yl)ethynyl)-4-methyl-N-(3...)
Show SMILES Cc1ccc(cc1C#Cc1cnc(N)nc1)C(=O)Nc1cccc(c1)C(F)(F)F
Show InChI InChI=1S/C21H15F3N4O/c1-13-5-7-16(9-15(13)8-6-14-11-26-20(25)27-12-14)19(29)28-18-4-2-3-17(10-18)21(22,23)24/h2-5,7,9-12H,1H3,(H,28,29)(H2,25,26,27)
Affinity DataIC50: 1nMAssay Description:The assay uses purified enzyme interacting with biotinylated peptide substrate. HTRF is based on the proximity of europium cryptate (donor fluorophor...More data for this Ligand-Target Pair
TargetTyrosine-protein kinase Lck [245-498](Homo sapiens (Human))
Amgen Inc

LigandPNGBDBM14949(2-aminoquinazoline 5 | 3-(2-aminoquinazolin-6-yl)-...)
Show SMILES Cc1ccc(cc1-c1ccc2nc(N)ncc2c1)C(=O)Nc1cccc(c1)C(F)(F)F
Show InChI InChI=1S/C23H17F3N4O/c1-13-5-6-15(21(31)29-18-4-2-3-17(11-18)23(24,25)26)10-19(13)14-7-8-20-16(9-14)12-28-22(27)30-20/h2-12H,1H3,(H,29,31)(H2,27,28,30)
Affinity DataIC50: 1nMAssay Description:The assay uses purified enzyme interacting with biotinylated peptide substrate. HTRF is based on the proximity of europium cryptate (donor fluorophor...More data for this Ligand-Target Pair
TargetTyrosine-protein kinase Lck [245-498](Homo sapiens (Human))
Amgen Inc

LigandPNGBDBM14948(4-Methyl-3-(3-(2-(methylamino)pyrimidin-4-yl)pyrid...)
Show SMILES CNc1nccc(n1)-c1cccnc1Oc1cc(ccc1C)C(=O)Nc1cccc(c1)C(F)(F)F
Show InChI InChI=1S/C25H20F3N5O2/c1-15-8-9-16(22(34)32-18-6-3-5-17(14-18)25(26,27)28)13-21(15)35-23-19(7-4-11-30-23)20-10-12-31-24(29-2)33-20/h3-14H,1-2H3,(H,32,34)(H,29,31,33)
Affinity DataIC50: 1nMAssay Description:The assay uses purified enzyme interacting with biotinylated peptide substrate. HTRF is based on the proximity of europium cryptate (donor fluorophor...More data for this Ligand-Target Pair
TargetVascular endothelial growth factor receptor 2(Homo sapiens (Human))
Amgen Inc

LigandPNGBDBM14951(3-(2-(2-Aminopyrimidin-5-yl)ethynyl)-N-(3-(trifluo...)
Show SMILES Nc1ncc(cn1)C#Cc1cccc(c1)C(=O)Nc1cccc(c1)C(F)(F)F
Show InChI InChI=1S/C20H13F3N4O/c21-20(22,23)16-5-2-6-17(10-16)27-18(28)15-4-1-3-13(9-15)7-8-14-11-25-19(24)26-12-14/h1-6,9-12H,(H,27,28)(H2,24,25,26)
Affinity DataIC50: 1nMAssay Description:The assay uses purified enzyme interacting with biotinylated peptide substrate. HTRF is based on the proximity of europium cryptate (donor fluorophor...More data for this Ligand-Target Pair
TargetVascular endothelial growth factor receptor 2(Homo sapiens (Human))
Amgen Inc

LigandPNGBDBM14966(3-(2-(6-Aminopyridin-3-yl)ethynyl)-4-methyl-N-(3-(...)
Show SMILES Cc1ccc(cc1C#Cc1ccc(N)nc1)C(=O)Nc1cccc(c1)C(F)(F)F
Show InChI InChI=1S/C22H16F3N3O/c1-14-5-8-17(11-16(14)9-6-15-7-10-20(26)27-13-15)21(29)28-19-4-2-3-18(12-19)22(23,24)25/h2-5,7-8,10-13H,1H3,(H2,26,27)(H,28,29)
Affinity DataIC50: 1nMAssay Description:The assay uses purified enzyme interacting with biotinylated peptide substrate. HTRF is based on the proximity of europium cryptate (donor fluorophor...More data for this Ligand-Target Pair
TargetVascular endothelial growth factor receptor 2(Homo sapiens (Human))
Amgen Inc

LigandPNGBDBM14967(3-(2-(3H-Imidazo[4,5-b]pyridin-6-yl)ethynyl)-4-met...)
Show SMILES Cc1ccc(cc1C#Cc1cnc2nc[nH]c2c1)C(=O)Nc1cccc(c1)C(F)(F)F
Show InChI InChI=1S/C23H15F3N4O/c1-14-5-7-17(22(31)30-19-4-2-3-18(11-19)23(24,25)26)10-16(14)8-6-15-9-20-21(27-12-15)29-13-28-20/h2-5,7,9-13H,1H3,(H,30,31)(H,27,28,29)
Affinity DataIC50: 1nMAssay Description:The assay uses purified enzyme interacting with biotinylated peptide substrate. HTRF is based on the proximity of europium cryptate (donor fluorophor...More data for this Ligand-Target Pair
TargetVascular endothelial growth factor receptor 2(Homo sapiens (Human))
Amgen Inc

LigandPNGBDBM14969(4-Methyl-3-(2-(quinolin-3-yl)ethynyl)-N-(3-(triflu...)
Show SMILES Cc1ccc(cc1C#Cc1cnc2ccccc2c1)C(=O)Nc1cccc(c1)C(F)(F)F
Show InChI InChI=1S/C26H17F3N2O/c1-17-9-11-21(25(32)31-23-7-4-6-22(15-23)26(27,28)29)14-19(17)12-10-18-13-20-5-2-3-8-24(20)30-16-18/h2-9,11,13-16H,1H3,(H,31,32)
Affinity DataIC50: 1nMAssay Description:The assay uses purified enzyme interacting with biotinylated peptide substrate. HTRF is based on the proximity of europium cryptate (donor fluorophor...More data for this Ligand-Target Pair
TargetVascular endothelial growth factor receptor 2(Homo sapiens (Human))
Amgen Inc

LigandPNGBDBM14950(3-(2-(2-Aminopyrimidin-5-yl)ethynyl)-4-methyl-N-(3...)
Show SMILES Cc1ccc(cc1C#Cc1cnc(N)nc1)C(=O)Nc1cccc(c1)C(F)(F)F
Show InChI InChI=1S/C21H15F3N4O/c1-13-5-7-16(9-15(13)8-6-14-11-26-20(25)27-12-14)19(29)28-18-4-2-3-17(10-18)21(22,23)24/h2-5,7,9-12H,1H3,(H,28,29)(H2,25,26,27)
Affinity DataIC50: 2nMAssay Description:The assay uses purified enzyme interacting with biotinylated peptide substrate. HTRF is based on the proximity of europium cryptate (donor fluorophor...More data for this Ligand-Target Pair
TargetVascular endothelial growth factor receptor 2(Homo sapiens (Human))
Amgen Inc

LigandPNGBDBM14949(2-aminoquinazoline 5 | 3-(2-aminoquinazolin-6-yl)-...)
Show SMILES Cc1ccc(cc1-c1ccc2nc(N)ncc2c1)C(=O)Nc1cccc(c1)C(F)(F)F
Show InChI InChI=1S/C23H17F3N4O/c1-13-5-6-15(21(31)29-18-4-2-3-17(11-18)23(24,25)26)10-19(13)14-7-8-20-16(9-14)12-28-22(27)30-20/h2-12H,1H3,(H,29,31)(H2,27,28,30)
Affinity DataIC50: 2nMAssay Description:The assay uses purified enzyme interacting with biotinylated peptide substrate. HTRF is based on the proximity of europium cryptate (donor fluorophor...More data for this Ligand-Target Pair
TargetAngiopoietin-1 receptor(Homo sapiens (Human))
Amgen Inc

LigandPNGBDBM14967(3-(2-(3H-Imidazo[4,5-b]pyridin-6-yl)ethynyl)-4-met...)
Show SMILES Cc1ccc(cc1C#Cc1cnc2nc[nH]c2c1)C(=O)Nc1cccc(c1)C(F)(F)F
Show InChI InChI=1S/C23H15F3N4O/c1-14-5-7-17(22(31)30-19-4-2-3-18(11-19)23(24,25)26)10-16(14)8-6-15-9-20-21(27-12-15)29-13-28-20/h2-5,7,9-13H,1H3,(H,30,31)(H,27,28,29)
Affinity DataIC50: 2nMpH: 7.5 T: 2°CAssay Description:The assay uses purified enzyme interacting with biotinylated peptide substrate. HTRF is based on the proximity of europium cryptate (donor fluorophor...More data for this Ligand-Target Pair
TargetVascular endothelial growth factor receptor 2(Homo sapiens (Human))
Amgen Inc

LigandPNGBDBM14948(4-Methyl-3-(3-(2-(methylamino)pyrimidin-4-yl)pyrid...)
Show SMILES CNc1nccc(n1)-c1cccnc1Oc1cc(ccc1C)C(=O)Nc1cccc(c1)C(F)(F)F
Show InChI InChI=1S/C25H20F3N5O2/c1-15-8-9-16(22(34)32-18-6-3-5-17(14-18)25(26,27)28)13-21(15)35-23-19(7-4-11-30-23)20-10-12-31-24(29-2)33-20/h3-14H,1-2H3,(H,32,34)(H,29,31,33)
Affinity DataIC50: 3nMAssay Description:The assay uses purified enzyme interacting with biotinylated peptide substrate. HTRF is based on the proximity of europium cryptate (donor fluorophor...More data for this Ligand-Target Pair
TargetAngiopoietin-1 receptor(Homo sapiens (Human))
Amgen Inc

LigandPNGBDBM14966(3-(2-(6-Aminopyridin-3-yl)ethynyl)-4-methyl-N-(3-(...)
Show SMILES Cc1ccc(cc1C#Cc1ccc(N)nc1)C(=O)Nc1cccc(c1)C(F)(F)F
Show InChI InChI=1S/C22H16F3N3O/c1-14-5-8-17(11-16(14)9-6-15-7-10-20(26)27-13-15)21(29)28-19-4-2-3-18(12-19)22(23,24)25/h2-5,7-8,10-13H,1H3,(H2,26,27)(H,28,29)
Affinity DataIC50: 3nMpH: 7.5 T: 2°CAssay Description:The assay uses purified enzyme interacting with biotinylated peptide substrate. HTRF is based on the proximity of europium cryptate (donor fluorophor...More data for this Ligand-Target Pair
TargetAngiopoietin-1 receptor(Homo sapiens (Human))
Amgen Inc

LigandPNGBDBM14950(3-(2-(2-Aminopyrimidin-5-yl)ethynyl)-4-methyl-N-(3...)
Show SMILES Cc1ccc(cc1C#Cc1cnc(N)nc1)C(=O)Nc1cccc(c1)C(F)(F)F
Show InChI InChI=1S/C21H15F3N4O/c1-13-5-7-16(9-15(13)8-6-14-11-26-20(25)27-12-14)19(29)28-18-4-2-3-17(10-18)21(22,23)24/h2-5,7,9-12H,1H3,(H,28,29)(H2,25,26,27)
Affinity DataIC50: 3nMpH: 7.5 T: 2°CAssay Description:The assay uses purified enzyme interacting with biotinylated peptide substrate. HTRF is based on the proximity of europium cryptate (donor fluorophor...More data for this Ligand-Target Pair
TargetVascular endothelial growth factor receptor 2(Homo sapiens (Human))
Amgen Inc

LigandPNGBDBM14970(4-Methyl-3-(2-(quinoxalin-2-yl)ethynyl)-N-(3-(trif...)
Show SMILES Cc1ccc(cc1C#Cc1cnc2ccccc2n1)C(=O)Nc1cccc(c1)C(F)(F)F
Show InChI InChI=1S/C25H16F3N3O/c1-16-9-10-18(24(32)31-20-6-4-5-19(14-20)25(26,27)28)13-17(16)11-12-21-15-29-22-7-2-3-8-23(22)30-21/h2-10,13-15H,1H3,(H,31,32)
Affinity DataIC50: 4nMAssay Description:The assay uses purified enzyme interacting with biotinylated peptide substrate. HTRF is based on the proximity of europium cryptate (donor fluorophor...More data for this Ligand-Target Pair
TargetTyrosine-protein kinase Lck [245-498](Homo sapiens (Human))
Amgen Inc

LigandPNGBDBM14970(4-Methyl-3-(2-(quinoxalin-2-yl)ethynyl)-N-(3-(trif...)
Show SMILES Cc1ccc(cc1C#Cc1cnc2ccccc2n1)C(=O)Nc1cccc(c1)C(F)(F)F
Show InChI InChI=1S/C25H16F3N3O/c1-16-9-10-18(24(32)31-20-6-4-5-19(14-20)25(26,27)28)13-17(16)11-12-21-15-29-22-7-2-3-8-23(22)30-21/h2-10,13-15H,1H3,(H,31,32)
Affinity DataIC50: 4nMAssay Description:The assay uses purified enzyme interacting with biotinylated peptide substrate. HTRF is based on the proximity of europium cryptate (donor fluorophor...More data for this Ligand-Target Pair
TargetAngiopoietin-1 receptor(Homo sapiens (Human))
Amgen Inc

LigandPNGBDBM14961((S)-5-(2-(2-Aminopyrimidin-5-yl)ethynyl)-N-(2-(3-(...)
Show SMILES CN(C)[C@H]1CCCN(C1)c1ccc(cc1NC(=O)c1cc(ccc1F)C#Cc1cnc(N)nc1)C(F)(F)F
Show InChI InChI=1S/C27H26F4N6O/c1-36(2)20-4-3-11-37(16-20)24-10-8-19(27(29,30)31)13-23(24)35-25(38)21-12-17(7-9-22(21)28)5-6-18-14-33-26(32)34-15-18/h7-10,12-15,20H,3-4,11,16H2,1-2H3,(H,35,38)(H2,32,33,34)/t20-/m0/s1
Affinity DataIC50: 5nMpH: 7.5 T: 2°CAssay Description:The assay uses purified enzyme interacting with biotinylated peptide substrate. HTRF is based on the proximity of europium cryptate (donor fluorophor...More data for this Ligand-Target Pair
TargetVascular endothelial growth factor receptor 2(Homo sapiens (Human))
Amgen Inc

LigandPNGBDBM14952(5-(2-(2-Aminopyrimidin-5-yl)ethynyl)-2-fluoro-N-(3...)
Show SMILES Nc1ncc(cn1)C#Cc1ccc(F)c(c1)C(=O)Nc1cccc(c1)C(F)(F)F
Show InChI InChI=1S/C20H12F4N4O/c21-17-7-6-12(4-5-13-10-26-19(25)27-11-13)8-16(17)18(29)28-15-3-1-2-14(9-15)20(22,23)24/h1-3,6-11H,(H,28,29)(H2,25,26,27)
Affinity DataIC50: 6nMAssay Description:The assay uses purified enzyme interacting with biotinylated peptide substrate. HTRF is based on the proximity of europium cryptate (donor fluorophor...More data for this Ligand-Target Pair
TargetAngiopoietin-1 receptor(Homo sapiens (Human))
Amgen Inc

LigandPNGBDBM14957(5-(2-(2-Aminopyrimidin-5-yl)ethynyl)-N-(2-((3-(dim...)
Show SMILES CN(C)CCCN(C)c1ccc(cc1NC(=O)c1cc(ccc1F)C#Cc1cnc(N)nc1)C(F)(F)F
Show InChI InChI=1S/C26H26F4N6O/c1-35(2)11-4-12-36(3)23-10-8-19(26(28,29)30)14-22(23)34-24(37)20-13-17(7-9-21(20)27)5-6-18-15-32-25(31)33-16-18/h7-10,13-16H,4,11-12H2,1-3H3,(H,34,37)(H2,31,32,33)
Affinity DataIC50: 8nMpH: 7.5 T: 2°CAssay Description:The assay uses purified enzyme interacting with biotinylated peptide substrate. HTRF is based on the proximity of europium cryptate (donor fluorophor...More data for this Ligand-Target Pair
TargetAngiopoietin-1 receptor(Homo sapiens (Human))
Amgen Inc

LigandPNGBDBM14969(4-Methyl-3-(2-(quinolin-3-yl)ethynyl)-N-(3-(triflu...)
Show SMILES Cc1ccc(cc1C#Cc1cnc2ccccc2c1)C(=O)Nc1cccc(c1)C(F)(F)F
Show InChI InChI=1S/C26H17F3N2O/c1-17-9-11-21(25(32)31-23-7-4-6-22(15-23)26(27,28)29)14-19(17)12-10-18-13-20-5-2-3-8-24(20)30-16-18/h2-9,11,13-16H,1H3,(H,31,32)
Affinity DataIC50: 10nMpH: 7.5 T: 2°CAssay Description:The assay uses purified enzyme interacting with biotinylated peptide substrate. HTRF is based on the proximity of europium cryptate (donor fluorophor...More data for this Ligand-Target Pair
TargetVascular endothelial growth factor receptor 2(Homo sapiens (Human))
Amgen Inc

LigandPNGBDBM14957(5-(2-(2-Aminopyrimidin-5-yl)ethynyl)-N-(2-((3-(dim...)
Show SMILES CN(C)CCCN(C)c1ccc(cc1NC(=O)c1cc(ccc1F)C#Cc1cnc(N)nc1)C(F)(F)F
Show InChI InChI=1S/C26H26F4N6O/c1-35(2)11-4-12-36(3)23-10-8-19(26(28,29)30)14-22(23)34-24(37)20-13-17(7-9-21(20)27)5-6-18-15-32-25(31)33-16-18/h7-10,13-16H,4,11-12H2,1-3H3,(H,34,37)(H2,31,32,33)
Affinity DataIC50: 11nMAssay Description:The assay uses purified enzyme interacting with biotinylated peptide substrate. HTRF is based on the proximity of europium cryptate (donor fluorophor...More data for this Ligand-Target Pair
TargetAngiopoietin-1 receptor(Homo sapiens (Human))
Amgen Inc

LigandPNGBDBM14951(3-(2-(2-Aminopyrimidin-5-yl)ethynyl)-N-(3-(trifluo...)
Show SMILES Nc1ncc(cn1)C#Cc1cccc(c1)C(=O)Nc1cccc(c1)C(F)(F)F
Show InChI InChI=1S/C20H13F3N4O/c21-20(22,23)16-5-2-6-17(10-16)27-18(28)15-4-1-3-13(9-15)7-8-14-11-25-19(24)26-12-14/h1-6,9-12H,(H,27,28)(H2,24,25,26)
Affinity DataIC50: 11nMpH: 7.5 T: 2°CAssay Description:The assay uses purified enzyme interacting with biotinylated peptide substrate. HTRF is based on the proximity of europium cryptate (donor fluorophor...More data for this Ligand-Target Pair
TargetAngiopoietin-1 receptor(Homo sapiens (Human))
Amgen Inc

LigandPNGBDBM14963((S)-N-(2-(3-Aminopiperidin-1-yl)-5-(trifluoromethy...)
Show SMILES N[C@H]1CCCN(C1)c1ccc(cc1NC(=O)c1cc(ccc1F)C#Cc1cnc(N)nc1)C(F)(F)F
Show InChI InChI=1S/C25H22F4N6O/c26-20-7-5-15(3-4-16-12-32-24(31)33-13-16)10-19(20)23(36)34-21-11-17(25(27,28)29)6-8-22(21)35-9-1-2-18(30)14-35/h5-8,10-13,18H,1-2,9,14,30H2,(H,34,36)(H2,31,32,33)/t18-/m0/s1
Affinity DataIC50: 13nMpH: 7.5 T: 2°CAssay Description:The assay uses purified enzyme interacting with biotinylated peptide substrate. HTRF is based on the proximity of europium cryptate (donor fluorophor...More data for this Ligand-Target Pair
TargetAngiopoietin-1 receptor(Homo sapiens (Human))
Amgen Inc

LigandPNGBDBM14958(5-[(2-aminopyrimidin-5-yl)ethynyl]-2-fluoro-N-[2-(...)
Show SMILES CN1CCN(CC1)c1ccc(cc1NC(=O)c1cc(ccc1F)C#Cc1cnc(N)nc1)C(F)(F)F
Show InChI InChI=1S/C25H22F4N6O/c1-34-8-10-35(11-9-34)22-7-5-18(25(27,28)29)13-21(22)33-23(36)19-12-16(4-6-20(19)26)2-3-17-14-31-24(30)32-15-17/h4-7,12-15H,8-11H2,1H3,(H,33,36)(H2,30,31,32)
Affinity DataIC50: 13nMpH: 7.5 T: 2°CAssay Description:The assay uses purified enzyme interacting with biotinylated peptide substrate. HTRF is based on the proximity of europium cryptate (donor fluorophor...More data for this Ligand-Target Pair
TargetAngiopoietin-1 receptor(Homo sapiens (Human))
Amgen Inc

LigandPNGBDBM14962((S)-5-(2-(2-Aminopyrimidin-5-yl)ethynyl)-2-fluoro-...)
Show SMILES CN[C@H]1CCCN(C1)c1ccc(cc1NC(=O)c1cc(ccc1F)C#Cc1cnc(N)nc1)C(F)(F)F
Show InChI InChI=1S/C26H24F4N6O/c1-32-19-3-2-10-36(15-19)23-9-7-18(26(28,29)30)12-22(23)35-24(37)20-11-16(6-8-21(20)27)4-5-17-13-33-25(31)34-14-17/h6-9,11-14,19,32H,2-3,10,15H2,1H3,(H,35,37)(H2,31,33,34)/t19-/m0/s1
Affinity DataIC50: 14nMpH: 7.5 T: 2°CAssay Description:The assay uses purified enzyme interacting with biotinylated peptide substrate. HTRF is based on the proximity of europium cryptate (donor fluorophor...More data for this Ligand-Target Pair
TargetAngiopoietin-1 receptor(Homo sapiens (Human))
Amgen Inc

LigandPNGBDBM14955(5-(2-(2-Aminopyrimidin-5-yl)ethynyl)-2-fluoro-N-(2...)
Show SMILES Nc1ncc(cn1)C#Cc1ccc(F)c(c1)C(=O)Nc1cc(ccc1N1CCCCC1)C(F)(F)F
Show InChI InChI=1S/C25H21F4N5O/c26-20-8-6-16(4-5-17-14-31-24(30)32-15-17)12-19(20)23(35)33-21-13-18(25(27,28)29)7-9-22(21)34-10-2-1-3-11-34/h6-9,12-15H,1-3,10-11H2,(H,33,35)(H2,30,31,32)
Affinity DataIC50: 17nMpH: 7.5 T: 2°CAssay Description:The assay uses purified enzyme interacting with biotinylated peptide substrate. HTRF is based on the proximity of europium cryptate (donor fluorophor...More data for this Ligand-Target Pair
TargetTyrosine-protein kinase Lck [245-498](Homo sapiens (Human))
Amgen Inc

LigandPNGBDBM14951(3-(2-(2-Aminopyrimidin-5-yl)ethynyl)-N-(3-(trifluo...)
Show SMILES Nc1ncc(cn1)C#Cc1cccc(c1)C(=O)Nc1cccc(c1)C(F)(F)F
Show InChI InChI=1S/C20H13F3N4O/c21-20(22,23)16-5-2-6-17(10-16)27-18(28)15-4-1-3-13(9-15)7-8-14-11-25-19(24)26-12-14/h1-6,9-12H,(H,27,28)(H2,24,25,26)
Affinity DataIC50: 19nMAssay Description:The assay uses purified enzyme interacting with biotinylated peptide substrate. HTRF is based on the proximity of europium cryptate (donor fluorophor...More data for this Ligand-Target Pair
TargetTyrosine-protein kinase Lck [245-498](Homo sapiens (Human))
Amgen Inc

LigandPNGBDBM14957(5-(2-(2-Aminopyrimidin-5-yl)ethynyl)-N-(2-((3-(dim...)
Show SMILES CN(C)CCCN(C)c1ccc(cc1NC(=O)c1cc(ccc1F)C#Cc1cnc(N)nc1)C(F)(F)F
Show InChI InChI=1S/C26H26F4N6O/c1-35(2)11-4-12-36(3)23-10-8-19(26(28,29)30)14-22(23)34-24(37)20-13-17(7-9-21(20)27)5-6-18-15-32-25(31)33-16-18/h7-10,13-16H,4,11-12H2,1-3H3,(H,34,37)(H2,31,32,33)
Affinity DataIC50: 21nMAssay Description:The assay uses purified enzyme interacting with biotinylated peptide substrate. HTRF is based on the proximity of europium cryptate (donor fluorophor...More data for this Ligand-Target Pair
TargetAngiopoietin-1 receptor(Homo sapiens (Human))
Amgen Inc

LigandPNGBDBM14956(5-(2-(2-Aminopyrimidin-5-yl)ethynyl)-2-methoxy-N-(...)
Show SMILES COc1ccc(cc1C(=O)Nc1cc(ccc1N1CCCCC1)C(F)(F)F)C#Cc1cnc(N)nc1
Show InChI InChI=1S/C26H24F3N5O2/c1-36-23-10-7-17(5-6-18-15-31-25(30)32-16-18)13-20(23)24(35)33-21-14-19(26(27,28)29)8-9-22(21)34-11-3-2-4-12-34/h7-10,13-16H,2-4,11-12H2,1H3,(H,33,35)(H2,30,31,32)
Affinity DataIC50: 21nMpH: 7.5 T: 2°CAssay Description:The assay uses purified enzyme interacting with biotinylated peptide substrate. HTRF is based on the proximity of europium cryptate (donor fluorophor...More data for this Ligand-Target Pair
TargetAngiopoietin-1 receptor(Homo sapiens (Human))
Amgen Inc

LigandPNGBDBM14953(3-(2-(2-Aminopyrimidin-5-yl)ethynyl)-4-methyl-N-(2...)
Show SMILES Cc1ccc(cc1C#Cc1cnc(N)nc1)C(=O)Nc1cc(ccc1N1CCCCC1)C(F)(F)F
Show InChI InChI=1S/C26H24F3N5O/c1-17-5-7-20(13-19(17)8-6-18-15-31-25(30)32-16-18)24(35)33-22-14-21(26(27,28)29)9-10-23(22)34-11-3-2-4-12-34/h5,7,9-10,13-16H,2-4,11-12H2,1H3,(H,33,35)(H2,30,31,32)
Affinity DataIC50: 30nMpH: 7.5 T: 2°CAssay Description:The assay uses purified enzyme interacting with biotinylated peptide substrate. HTRF is based on the proximity of europium cryptate (donor fluorophor...More data for this Ligand-Target Pair
TargetTyrosine-protein kinase Lck [245-498](Homo sapiens (Human))
Amgen Inc

LigandPNGBDBM14953(3-(2-(2-Aminopyrimidin-5-yl)ethynyl)-4-methyl-N-(2...)
Show SMILES Cc1ccc(cc1C#Cc1cnc(N)nc1)C(=O)Nc1cc(ccc1N1CCCCC1)C(F)(F)F
Show InChI InChI=1S/C26H24F3N5O/c1-17-5-7-20(13-19(17)8-6-18-15-31-25(30)32-16-18)24(35)33-22-14-21(26(27,28)29)9-10-23(22)34-11-3-2-4-12-34/h5,7,9-10,13-16H,2-4,11-12H2,1H3,(H,33,35)(H2,30,31,32)
Affinity DataIC50: 42nMAssay Description:The assay uses purified enzyme interacting with biotinylated peptide substrate. HTRF is based on the proximity of europium cryptate (donor fluorophor...More data for this Ligand-Target Pair
TargetAngiopoietin-1 receptor(Homo sapiens (Human))
Amgen Inc

LigandPNGBDBM14960((R)-5-(2-(2-Aminopyrimidin-5-yl)ethynyl)-N-(2-(3-(...)
Show SMILES CN(C)[C@@H]1CCCN(C1)c1ccc(cc1NC(=O)c1cc(ccc1F)C#Cc1cnc(N)nc1)C(F)(F)F
Show InChI InChI=1S/C27H26F4N6O/c1-36(2)20-4-3-11-37(16-20)24-10-8-19(27(29,30)31)13-23(24)35-25(38)21-12-17(7-9-22(21)28)5-6-18-14-33-26(32)34-15-18/h7-10,12-15,20H,3-4,11,16H2,1-2H3,(H,35,38)(H2,32,33,34)/t20-/m1/s1
Affinity DataIC50: 44nMpH: 7.5 T: 2°CAssay Description:The assay uses purified enzyme interacting with biotinylated peptide substrate. HTRF is based on the proximity of europium cryptate (donor fluorophor...More data for this Ligand-Target Pair
TargetAngiopoietin-1 receptor(Homo sapiens (Human))
Amgen Inc

LigandPNGBDBM14952(5-(2-(2-Aminopyrimidin-5-yl)ethynyl)-2-fluoro-N-(3...)
Show SMILES Nc1ncc(cn1)C#Cc1ccc(F)c(c1)C(=O)Nc1cccc(c1)C(F)(F)F
Show InChI InChI=1S/C20H12F4N4O/c21-17-7-6-12(4-5-13-10-26-19(25)27-11-13)8-16(17)18(29)28-15-3-1-2-14(9-15)20(22,23)24/h1-3,6-11H,(H,28,29)(H2,25,26,27)
Affinity DataIC50: 47nMpH: 7.5 T: 2°CAssay Description:The assay uses purified enzyme interacting with biotinylated peptide substrate. HTRF is based on the proximity of europium cryptate (donor fluorophor...More data for this Ligand-Target Pair
TargetAngiopoietin-1 receptor(Homo sapiens (Human))
Amgen Inc

LigandPNGBDBM14954(3-(2-(2-Aminopyrimidin-5-yl)ethynyl)-N-(2-(piperid...)
Show SMILES Nc1ncc(cn1)C#Cc1cccc(c1)C(=O)Nc1cc(ccc1N1CCCCC1)C(F)(F)F
Show InChI InChI=1S/C25H22F3N5O/c26-25(27,28)20-9-10-22(33-11-2-1-3-12-33)21(14-20)32-23(34)19-6-4-5-17(13-19)7-8-18-15-30-24(29)31-16-18/h4-6,9-10,13-16H,1-3,11-12H2,(H,32,34)(H2,29,30,31)
Affinity DataIC50: 63nMpH: 7.5 T: 2°CAssay Description:The assay uses purified enzyme interacting with biotinylated peptide substrate. HTRF is based on the proximity of europium cryptate (donor fluorophor...More data for this Ligand-Target Pair
TargetTyrosine-protein kinase Lck [245-498](Homo sapiens (Human))
Amgen Inc

LigandPNGBDBM14952(5-(2-(2-Aminopyrimidin-5-yl)ethynyl)-2-fluoro-N-(3...)
Show SMILES Nc1ncc(cn1)C#Cc1ccc(F)c(c1)C(=O)Nc1cccc(c1)C(F)(F)F
Show InChI InChI=1S/C20H12F4N4O/c21-17-7-6-12(4-5-13-10-26-19(25)27-11-13)8-16(17)18(29)28-15-3-1-2-14(9-15)20(22,23)24/h1-3,6-11H,(H,28,29)(H2,25,26,27)
Affinity DataIC50: 65nMAssay Description:The assay uses purified enzyme interacting with biotinylated peptide substrate. HTRF is based on the proximity of europium cryptate (donor fluorophor...More data for this Ligand-Target Pair
TargetAngiopoietin-1 receptor(Homo sapiens (Human))
Amgen Inc

LigandPNGBDBM14970(4-Methyl-3-(2-(quinoxalin-2-yl)ethynyl)-N-(3-(trif...)
Show SMILES Cc1ccc(cc1C#Cc1cnc2ccccc2n1)C(=O)Nc1cccc(c1)C(F)(F)F
Show InChI InChI=1S/C25H16F3N3O/c1-16-9-10-18(24(32)31-20-6-4-5-19(14-20)25(26,27)28)13-17(16)11-12-21-15-29-22-7-2-3-8-23(22)30-21/h2-10,13-15H,1H3,(H,31,32)
Affinity DataIC50: 85nMpH: 7.5 T: 2°CAssay Description:The assay uses purified enzyme interacting with biotinylated peptide substrate. HTRF is based on the proximity of europium cryptate (donor fluorophor...More data for this Ligand-Target Pair
TargetTyrosine-protein kinase Lck [245-498](Homo sapiens (Human))
Amgen Inc

LigandPNGBDBM14961((S)-5-(2-(2-Aminopyrimidin-5-yl)ethynyl)-N-(2-(3-(...)
Show SMILES CN(C)[C@H]1CCCN(C1)c1ccc(cc1NC(=O)c1cc(ccc1F)C#Cc1cnc(N)nc1)C(F)(F)F
Show InChI InChI=1S/C27H26F4N6O/c1-36(2)20-4-3-11-37(16-20)24-10-8-19(27(29,30)31)13-23(24)35-25(38)21-12-17(7-9-22(21)28)5-6-18-14-33-26(32)34-15-18/h7-10,12-15,20H,3-4,11,16H2,1-2H3,(H,35,38)(H2,32,33,34)/t20-/m0/s1
Affinity DataIC50: 130nMAssay Description:The assay uses purified enzyme interacting with biotinylated peptide substrate. HTRF is based on the proximity of europium cryptate (donor fluorophor...More data for this Ligand-Target Pair
TargetAngiopoietin-1 receptor(Homo sapiens (Human))
Amgen Inc

LigandPNGBDBM14965((S)-5-(2-(2-Aminopyrimidin-5-yl)ethynyl)-N-(2-(3-(...)
Show SMILES CN(C)[C@H]1CCN(C1)c1ccc(cc1NC(=O)c1cc(ccc1F)C#Cc1cnc(N)nc1)C(F)(F)F
Show InChI InChI=1S/C26H24F4N6O/c1-35(2)19-9-10-36(15-19)23-8-6-18(26(28,29)30)12-22(23)34-24(37)20-11-16(5-7-21(20)27)3-4-17-13-32-25(31)33-14-17/h5-8,11-14,19H,9-10,15H2,1-2H3,(H,34,37)(H2,31,32,33)/t19-/m0/s1
Affinity DataIC50: 140nMpH: 7.5 T: 2°CAssay Description:The assay uses purified enzyme interacting with biotinylated peptide substrate. HTRF is based on the proximity of europium cryptate (donor fluorophor...More data for this Ligand-Target Pair
TargetTyrosine-protein kinase Lck [245-498](Homo sapiens (Human))
Amgen Inc

LigandPNGBDBM14959(5-(2-(2-Aminopyrimidin-5-yl)ethynyl)-N-(2-(4-(dime...)
Show SMILES CN(C)C1CCN(CC1)c1ccc(cc1NC(=O)c1cc(ccc1F)C#Cc1cnc(N)nc1)C(F)(F)F
Show InChI InChI=1S/C27H26F4N6O/c1-36(2)20-9-11-37(12-10-20)24-8-6-19(27(29,30)31)14-23(24)35-25(38)21-13-17(5-7-22(21)28)3-4-18-15-33-26(32)34-16-18/h5-8,13-16,20H,9-12H2,1-2H3,(H,35,38)(H2,32,33,34)
Affinity DataIC50: 150nMAssay Description:The assay uses purified enzyme interacting with biotinylated peptide substrate. HTRF is based on the proximity of europium cryptate (donor fluorophor...More data for this Ligand-Target Pair
TargetTyrosine-protein kinase Lck [245-498](Homo sapiens (Human))
Amgen Inc

LigandPNGBDBM14968(N-Methyl-5-(2-(2-methyl-5-((3-(trifluoromethyl)phe...)
Show SMILES CNC(=O)c1ccc(cn1)C#Cc1cc(ccc1C)C(=O)Nc1cccc(c1)C(F)(F)F
Show InChI InChI=1S/C24H18F3N3O2/c1-15-6-9-18(22(31)30-20-5-3-4-19(13-20)24(25,26)27)12-17(15)10-7-16-8-11-21(29-14-16)23(32)28-2/h3-6,8-9,11-14H,1-2H3,(H,28,32)(H,30,31)
Affinity DataIC50: 154nMAssay Description:The assay uses purified enzyme interacting with biotinylated peptide substrate. HTRF is based on the proximity of europium cryptate (donor fluorophor...More data for this Ligand-Target Pair
TargetVascular endothelial growth factor receptor 2(Homo sapiens (Human))
Amgen Inc

LigandPNGBDBM14968(N-Methyl-5-(2-(2-methyl-5-((3-(trifluoromethyl)phe...)
Show SMILES CNC(=O)c1ccc(cn1)C#Cc1cc(ccc1C)C(=O)Nc1cccc(c1)C(F)(F)F
Show InChI InChI=1S/C24H18F3N3O2/c1-15-6-9-18(22(31)30-20-5-3-4-19(13-20)24(25,26)27)12-17(15)10-7-16-8-11-21(29-14-16)23(32)28-2/h3-6,8-9,11-14H,1-2H3,(H,28,32)(H,30,31)
Affinity DataIC50: 169nMAssay Description:The assay uses purified enzyme interacting with biotinylated peptide substrate. HTRF is based on the proximity of europium cryptate (donor fluorophor...More data for this Ligand-Target Pair
TargetVascular endothelial growth factor receptor 2(Homo sapiens (Human))
Amgen Inc

LigandPNGBDBM14959(5-(2-(2-Aminopyrimidin-5-yl)ethynyl)-N-(2-(4-(dime...)
Show SMILES CN(C)C1CCN(CC1)c1ccc(cc1NC(=O)c1cc(ccc1F)C#Cc1cnc(N)nc1)C(F)(F)F
Show InChI InChI=1S/C27H26F4N6O/c1-36(2)20-9-11-37(12-10-20)24-8-6-19(27(29,30)31)14-23(24)35-25(38)21-13-17(5-7-22(21)28)3-4-18-15-33-26(32)34-16-18/h5-8,13-16,20H,9-12H2,1-2H3,(H,35,38)(H2,32,33,34)
Affinity DataIC50: 170nMAssay Description:The assay uses purified enzyme interacting with biotinylated peptide substrate. HTRF is based on the proximity of europium cryptate (donor fluorophor...More data for this Ligand-Target Pair
TargetTyrosine-protein kinase Lck [245-498](Homo sapiens (Human))
Amgen Inc

LigandPNGBDBM14958(5-[(2-aminopyrimidin-5-yl)ethynyl]-2-fluoro-N-[2-(...)
Show SMILES CN1CCN(CC1)c1ccc(cc1NC(=O)c1cc(ccc1F)C#Cc1cnc(N)nc1)C(F)(F)F
Show InChI InChI=1S/C25H22F4N6O/c1-34-8-10-35(11-9-34)22-7-5-18(25(27,28)29)13-21(22)33-23(36)19-12-16(4-6-20(19)26)2-3-17-14-31-24(30)32-15-17/h4-7,12-15H,8-11H2,1H3,(H,33,36)(H2,30,31,32)
Affinity DataIC50: 210nMAssay Description:The assay uses purified enzyme interacting with biotinylated peptide substrate. HTRF is based on the proximity of europium cryptate (donor fluorophor...More data for this Ligand-Target Pair
TargetAngiopoietin-1 receptor(Homo sapiens (Human))
Amgen Inc

LigandPNGBDBM14964((R)-5-(2-(2-Aminopyrimidin-5-yl)ethynyl)-N-(2-(3-(...)
Show SMILES CN(C)[C@@H]1CCN(C1)c1ccc(cc1NC(=O)c1cc(ccc1F)C#Cc1cnc(N)nc1)C(F)(F)F
Show InChI InChI=1S/C26H24F4N6O/c1-35(2)19-9-10-36(15-19)23-8-6-18(26(28,29)30)12-22(23)34-24(37)20-11-16(5-7-21(20)27)3-4-17-13-32-25(31)33-14-17/h5-8,11-14,19H,9-10,15H2,1-2H3,(H,34,37)(H2,31,32,33)/t19-/m1/s1
Affinity DataIC50: 220nMpH: 7.5 T: 2°CAssay Description:The assay uses purified enzyme interacting with biotinylated peptide substrate. HTRF is based on the proximity of europium cryptate (donor fluorophor...More data for this Ligand-Target Pair
TargetTyrosine-protein kinase Lck [245-498](Homo sapiens (Human))
Amgen Inc

LigandPNGBDBM14955(5-(2-(2-Aminopyrimidin-5-yl)ethynyl)-2-fluoro-N-(2...)
Show SMILES Nc1ncc(cn1)C#Cc1ccc(F)c(c1)C(=O)Nc1cc(ccc1N1CCCCC1)C(F)(F)F
Show InChI InChI=1S/C25H21F4N5O/c26-20-8-6-16(4-5-17-14-31-24(30)32-15-17)12-19(20)23(35)33-21-13-18(25(27,28)29)7-9-22(21)34-10-2-1-3-11-34/h6-9,12-15H,1-3,10-11H2,(H,33,35)(H2,30,31,32)
Affinity DataIC50: 370nMAssay Description:The assay uses purified enzyme interacting with biotinylated peptide substrate. HTRF is based on the proximity of europium cryptate (donor fluorophor...More data for this Ligand-Target Pair
TargetVascular endothelial growth factor receptor 2(Homo sapiens (Human))
Amgen Inc

LigandPNGBDBM14956(5-(2-(2-Aminopyrimidin-5-yl)ethynyl)-2-methoxy-N-(...)
Show SMILES COc1ccc(cc1C(=O)Nc1cc(ccc1N1CCCCC1)C(F)(F)F)C#Cc1cnc(N)nc1
Show InChI InChI=1S/C26H24F3N5O2/c1-36-23-10-7-17(5-6-18-15-31-25(30)32-16-18)13-20(23)24(35)33-21-14-19(26(27,28)29)8-9-22(21)34-11-3-2-4-12-34/h7-10,13-16H,2-4,11-12H2,1H3,(H,33,35)(H2,30,31,32)
Affinity DataIC50: 390nMAssay Description:The assay uses purified enzyme interacting with biotinylated peptide substrate. HTRF is based on the proximity of europium cryptate (donor fluorophor...More data for this Ligand-Target Pair
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