BDBM249396 US10537571, Compound 108::US10562888, Compound 108::US10654836, The compound of example 108 of WO2015057938::US10912774, Compound 108::US11001572, Example 108 of WO2015057938::US9434697, 108::US9730931, Compound 108
SMILES CCN1CCN(CC1)c1ccc(Nc2cc(ncn2)N(C)C(=O)Nc2c(Cl)c(OC)cc(OC)c2Cl)c(NC(=O)C=C)c1
InChI Key InChIKey=MBWRLLRCTIYXDW-UHFFFAOYSA-N
Data 52 IC50
Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB
Found 52 hits for monomerid = 249396
TargetFibroblast growth factor receptor 4(Homo sapiens (Human))
Eisai R&D Management Co., Ltd
US Patent
Eisai R&D Management Co., Ltd
US Patent
Affinity DataIC50: 1nMpH: 7.5 T: 2°CAssay Description:Compounds were profiled for FGFR inhibition activity at Reaction Biology Corporation (Malvern, Pa.) with their Kinase HotSpot assay. See, Anastassiad...More data for this Ligand-Target Pair
Affinity DataIC50: 320nMAssay Description:Inhibition of FGFR1 (unknown origin) using poly-GT as substrate preincubated for 1 hr followed by substrate addition and measured after 1 hr by FRET ...More data for this Ligand-Target Pair
TargetFibroblast growth factor receptor 2(Homo sapiens (Human))
Eisai R&D Management Co., Ltd
US Patent
Eisai R&D Management Co., Ltd
US Patent
Affinity DataIC50: 1.98E+3nMpH: 7.5 T: 2°CAssay Description:Compounds were profiled for FGFR inhibition activity at Reaction Biology Corporation (Malvern, Pa.) with their Kinase HotSpot assay. See, Anastassiad...More data for this Ligand-Target Pair
TargetFibroblast growth factor receptor 3(Homo sapiens (Human))
Eisai R&D Management Co., Ltd
US Patent
Eisai R&D Management Co., Ltd
US Patent
Affinity DataIC50: 2.00E+3nMpH: 7.5 T: 2°CAssay Description:Compounds were profiled for FGFR inhibition activity at Reaction Biology Corporation (Malvern, Pa.) with their Kinase HotSpot assay. See, Anastassiad...More data for this Ligand-Target Pair
Affinity DataIC50: 173nMpH: 7.5 T: 2°CAssay Description:Compounds were profiled for FGFR inhibition activity at Reaction Biology Corporation (Malvern, Pa.) with their Kinase HotSpot assay. See, Anastassiad...More data for this Ligand-Target Pair
TargetFibroblast growth factor receptor 4(Homo sapiens (Human))
Eisai R&D Management Co., Ltd
US Patent
Eisai R&D Management Co., Ltd
US Patent
Affinity DataIC50: 1nMpH: 7.5 T: 2°CAssay Description:Compounds were profiled for FGFR inhibition activity at Reaction Biology Corporation (Malvern, Pa.) with their Kinase HotSpot assay. See, Anastassiad...More data for this Ligand-Target Pair
TargetFibroblast growth factor receptor 4(Homo sapiens (Human))
Eisai R&D Management Co., Ltd
US Patent
Eisai R&D Management Co., Ltd
US Patent
Affinity DataIC50: 0.200nMpH: 7.5 T: 2°CAssay Description:Recombinant FGFR1 (2.5 nM), or FGFR4 (12 nM) was prepared as a mixture with substrate KKKSPGEYVNIEFG (SEQ ID NO:1) (20 μM, FGFR1 substrate); Pol...More data for this Ligand-Target Pair
Affinity DataIC50: 513nMpH: 7.5 T: 2°CAssay Description:Recombinant FGFR1 (2.5 nM), or FGFR4 (12 nM) was prepared as a mixture with substrate KKKSPGEYVNIEFG (SEQ ID NO:1) (20 μM, FGFR1 substrate); Pol...More data for this Ligand-Target Pair
TargetFibroblast growth factor receptor 4(Homo sapiens (Human))
Eisai R&D Management Co., Ltd
US Patent
Eisai R&D Management Co., Ltd
US Patent
Affinity DataIC50: 1nMAssay Description:Purified, recombinant FGFR4 was pre-incubated with 10 μM compound overnight at 4° C., or for 1 hour at room temperature. Following pre-incubatio...More data for this Ligand-Target Pair
Affinity DataIC50: 173nMAssay Description:Recombinant FGFR1 (2.5 nM), FGFR2 (1 nM), FGFR3 (5 nM), or FGFR4 (12 nM) (Invitrogen™) was prepared as a mixture with substrate KKKSPGEYVNIEFG (...More data for this Ligand-Target Pair
TargetFibroblast growth factor receptor 2(Homo sapiens (Human))
Eisai R&D Management Co., Ltd
US Patent
Eisai R&D Management Co., Ltd
US Patent
Affinity DataIC50: 1.98E+3nMAssay Description:Recombinant FGFR1 (2.5 nM), FGFR2 (1 nM), FGFR3 (5 nM), or FGFR4 (12 nM) (Invitrogen™) was prepared as a mixture with substrate KKKSPGEYVNIEFG (...More data for this Ligand-Target Pair
TargetFibroblast growth factor receptor 3(Homo sapiens (Human))
Eisai R&D Management Co., Ltd
US Patent
Eisai R&D Management Co., Ltd
US Patent
Affinity DataIC50: 2.00E+3nMAssay Description:Recombinant FGFR1 (2.5 nM), FGFR2 (1 nM), FGFR3 (5 nM), or FGFR4 (12 nM) (Invitrogen™) was prepared as a mixture with substrate KKKSPGEYVNIEFG (...More data for this Ligand-Target Pair
Affinity DataIC50: 173nMAssay Description:Recombinant FGFR1 (2.5 nM), FGFR2 (1 nM), FGFR3 (5 nM), or FGFR4 (12 nM) (Invitrogen™) was prepared as a mixture with substrate KKKSPGEYVNIEFG (...More data for this Ligand-Target Pair
TargetFibroblast growth factor receptor 4(Homo sapiens (Human))
Eisai R&D Management Co., Ltd
US Patent
Eisai R&D Management Co., Ltd
US Patent
Affinity DataIC50: 1nMAssay Description:Purified, recombinant FGFR4 was pre-incubated with 10 μM compound overnight at 4° C., or for 1 hour at room temperature. Following pre-incubatio...More data for this Ligand-Target Pair
TargetFibroblast growth factor receptor 4(Homo sapiens (Human))
Eisai R&D Management Co., Ltd
US Patent
Eisai R&D Management Co., Ltd
US Patent
Affinity DataIC50: 0.200nMAssay Description:Recombinant FGFR1 (2.5 nM), or FGFR4 (12 nM) was prepared as a mixture with substrate KKKSPGEYVNIEFG (SEQ ID NO:1) (20 μM, FGFR1 substrate); Pol...More data for this Ligand-Target Pair
Affinity DataIC50: 513nMAssay Description:Recombinant FGFR1 (2.5 nM), or FGFR4 (12 nM) was prepared as a mixture with substrate KKKSPGEYVNIEFG (SEQ ID NO:1) (20 μM, FGFR1 substrate); Pol...More data for this Ligand-Target Pair
Affinity DataIC50: 1nMAssay Description:Recombinant FGFR1 (2.5 nM), FGFR2 (1 nM), FGFR3 (5 nM), or FGFR4 (12 nM) was prepared as a mixture with substrate KKKSPGEYVNIEFG (SEQ ID NO:1) (20 &#...More data for this Ligand-Target Pair
Affinity DataIC50: 173nMAssay Description:Recombinant FGFR1 (2.5 nM), FGFR2 (1 nM), FGFR3 (5 nM), or FGFR4 (12 nM) was prepared as a mixture with substrate KKKSPGEYVNIEFG (SEQ ID NO:1) (20 &#...More data for this Ligand-Target Pair
TargetFibroblast growth factor receptor 2(Homo sapiens (Human))
Eisai R&D Management Co., Ltd
US Patent
Eisai R&D Management Co., Ltd
US Patent
Affinity DataIC50: 1.98E+3nMAssay Description:Recombinant FGFR1 (2.5 nM), FGFR2 (1 nM), FGFR3 (5 nM), or FGFR4 (12 nM) was prepared as a mixture with substrate KKKSPGEYVNIEFG (SEQ ID NO:1) (20 &#...More data for this Ligand-Target Pair
TargetFibroblast growth factor receptor 3(Homo sapiens (Human))
Eisai R&D Management Co., Ltd
US Patent
Eisai R&D Management Co., Ltd
US Patent
Affinity DataIC50: 2.00E+3nMAssay Description:Recombinant FGFR1 (2.5 nM), FGFR2 (1 nM), FGFR3 (5 nM), or FGFR4 (12 nM) was prepared as a mixture with substrate KKKSPGEYVNIEFG (SEQ ID NO:1) (20 &#...More data for this Ligand-Target Pair
Affinity DataIC50: 173nMAssay Description:Recombinant FGFR1 (2.5 nM), FGFR2 (1 nM), FGFR3 (5 nM), or FGFR4 (12 nM) was prepared as a mixture with substrate KKKSPGEYVNIEFG (SEQ ID NO:1) (20 &#...More data for this Ligand-Target Pair
Affinity DataIC50: 1nMAssay Description:Recombinant FGFR1 (2.5 nM), FGFR2 (1 nM), FGFR3 (5 nM), or FGFR4 (12 nM) was prepared as a mixture with substrate KKKSPGEYVNIEFG (SEQ ID NO:1) (20 &#...More data for this Ligand-Target Pair
TargetFibroblast growth factor receptor 4(Homo sapiens (Human))
Eisai R&D Management Co., Ltd
US Patent
Eisai R&D Management Co., Ltd
US Patent
Affinity DataIC50: 1nMAssay Description:Recombinant FGFR1 (2.5 nM), FGFR2 (1 nM), FGFR3 (5 nM), or FGFR4 (12 nM) was prepared as a mixture with substrate KKKSPGEYVNIEFG (SEQ ID NO:1) (20 ÎĽ...More data for this Ligand-Target Pair
Affinity DataIC50: 173nMAssay Description:Recombinant FGFR1 (2.5 nM), FGFR2 (1 nM), FGFR3 (5 nM), or FGFR4 (12 nM) was prepared as a mixture with substrate KKKSPGEYVNIEFG (SEQ ID NO:1) (20 ÎĽ...More data for this Ligand-Target Pair
TargetFibroblast growth factor receptor 2(Homo sapiens (Human))
Eisai R&D Management Co., Ltd
US Patent
Eisai R&D Management Co., Ltd
US Patent
Affinity DataIC50: 1.98E+3nMAssay Description:Recombinant FGFR1 (2.5 nM), FGFR2 (1 nM), FGFR3 (5 nM), or FGFR4 (12 nM) was prepared as a mixture with substrate KKKSPGEYVNIEFG (SEQ ID NO:1) (20 ÎĽ...More data for this Ligand-Target Pair
TargetFibroblast growth factor receptor 3(Homo sapiens (Human))
Eisai R&D Management Co., Ltd
US Patent
Eisai R&D Management Co., Ltd
US Patent
Affinity DataIC50: 2.00E+3nMAssay Description:Recombinant FGFR1 (2.5 nM), FGFR2 (1 nM), FGFR3 (5 nM), or FGFR4 (12 nM) was prepared as a mixture with substrate KKKSPGEYVNIEFG (SEQ ID NO:1) (20 ÎĽ...More data for this Ligand-Target Pair
Affinity DataIC50: 173nMAssay Description:Recombinant FGFR1 (2.5 nM), FGFR2 (1 nM), FGFR3 (5 nM), or FGFR4 (12 nM) was prepared as a mixture with substrate KKKSPGEYVNIEFG (SEQ ID NO:1) (20 ÎĽ...More data for this Ligand-Target Pair
TargetFibroblast growth factor receptor 4(Homo sapiens (Human))
Eisai R&D Management Co., Ltd
US Patent
Eisai R&D Management Co., Ltd
US Patent
Affinity DataIC50: 1nMAssay Description:Recombinant FGFR1 (2.5 nM), FGFR2 (1 nM), FGFR3 (5 nM), or FGFR4 (12 nM) was prepared as a mixture with substrate KKKSPGEYVNIEFG (SEQ ID NO:1) (20 ÎĽ...More data for this Ligand-Target Pair
Affinity DataIC50: 210nMAssay Description:The experimental procedure is briefly described as follows: the test compound was first dissolved in DMSO to prepare a stock solution, and then gradi...More data for this Ligand-Target Pair
TargetFibroblast growth factor receptor 2(Homo sapiens (Human))
Eisai R&D Management Co., Ltd
US Patent
Eisai R&D Management Co., Ltd
US Patent
Affinity DataIC50: 579nMAssay Description:The experimental procedure is briefly described as follows: the test compound was first dissolved in DMSO to prepare a stock solution, and then gradi...More data for this Ligand-Target Pair
TargetFibroblast growth factor receptor 3(Homo sapiens (Human))
Eisai R&D Management Co., Ltd
US Patent
Eisai R&D Management Co., Ltd
US Patent
Affinity DataIC50: 575nMAssay Description:The experimental procedure is briefly described as follows: the test compound was first dissolved in DMSO to prepare a stock solution, and then gradi...More data for this Ligand-Target Pair
TargetFibroblast growth factor receptor 4(Homo sapiens (Human))
Eisai R&D Management Co., Ltd
US Patent
Eisai R&D Management Co., Ltd
US Patent
Affinity DataIC50: 14nMAssay Description:The experimental procedure is briefly described as follows: the test compound was first dissolved in DMSO to prepare a stock solution, and then gradi...More data for this Ligand-Target Pair
TargetFibroblast growth factor receptor 2(Homo sapiens (Human))
Eisai R&D Management Co., Ltd
US Patent
Eisai R&D Management Co., Ltd
US Patent
Affinity DataIC50: 1.29E+3nMAssay Description:Inhibition of human FGFR2 using Poly [E,Y] 4:1 substrate pre-incubated for 15 to 60 mins followed by ATP and [gamma33P]-ATP additionMore data for this Ligand-Target Pair
TargetFibroblast growth factor receptor 3(Homo sapiens (Human))
Eisai R&D Management Co., Ltd
US Patent
Eisai R&D Management Co., Ltd
US Patent
Affinity DataIC50: 1.06E+3nMAssay Description:Inhibition of human FGFR3 using Poly [E,Y] 4:1 substrate pre-incubated for 15 to 60 mins followed by ATP and [gamma33P]-ATP additionMore data for this Ligand-Target Pair
Affinity DataIC50: 320nMAssay Description:Inhibition of human FGFR1 using KKKSPGEYVNIEFG substrate pre-incubated for 15 to 60 mins followed by ATP and [gamma33P]-ATP additionMore data for this Ligand-Target Pair
TargetFibroblast growth factor receptor 4(Homo sapiens (Human))
Eisai R&D Management Co., Ltd
US Patent
Eisai R&D Management Co., Ltd
US Patent
Affinity DataIC50: 1.20nMAssay Description:Inhibition of human FGFR4 using Poly [E,Y] 4:1 substrate pre-incubated for 15 to 60 mins followed by ATP and [gamma33P]-ATP additionMore data for this Ligand-Target Pair
TargetFibroblast growth factor receptor 4(Homo sapiens (Human))
Eisai R&D Management Co., Ltd
US Patent
Eisai R&D Management Co., Ltd
US Patent
Affinity DataIC50: 1nMAssay Description:Recombinant FGFR1 (2.5 nM), FGFR2 (1 nM), FGFR3 (5 nM), or FGFR4 (12 nM) (Invitrogen™) was prepared as a mixture with substrate KKKSPGEYVNIEFG (SEQ I...More data for this Ligand-Target Pair
Affinity DataIC50: 173nMAssay Description:Recombinant FGFR1 (2.5 nM), FGFR2 (1 nM), FGFR3 (5 nM), or FGFR4 (12 nM) (Invitrogen™) was prepared as a mixture with substrate KKKSPGEYVNIEFG (SEQ I...More data for this Ligand-Target Pair
TargetFibroblast growth factor receptor 2(Homo sapiens (Human))
Eisai R&D Management Co., Ltd
US Patent
Eisai R&D Management Co., Ltd
US Patent
Affinity DataIC50: 1.98E+3nMAssay Description:Recombinant FGFR1 (2.5 nM), FGFR2 (1 nM), FGFR3 (5 nM), or FGFR4 (12 nM) (Invitrogen™) was prepared as a mixture with substrate KKKSPGEYVNIEFG (SEQ I...More data for this Ligand-Target Pair
TargetFibroblast growth factor receptor 3(Homo sapiens (Human))
Eisai R&D Management Co., Ltd
US Patent
Eisai R&D Management Co., Ltd
US Patent
Affinity DataIC50: 2.00E+3nMAssay Description:Recombinant FGFR1 (2.5 nM), FGFR2 (1 nM), FGFR3 (5 nM), or FGFR4 (12 nM) (Invitrogen™) was prepared as a mixture with substrate KKKSPGEYVNIEFG (SEQ I...More data for this Ligand-Target Pair
Affinity DataIC50: 173nMAssay Description:Recombinant FGFR1 (2.5 nM), FGFR2 (1 nM), FGFR3 (5 nM), or FGFR4 (12 nM) (Invitrogen™) was prepared as a mixture with substrate KKKSPGEYVNIEFG (SEQ I...More data for this Ligand-Target Pair
TargetFibroblast growth factor receptor 4(Homo sapiens (Human))
Eisai R&D Management Co., Ltd
US Patent
Eisai R&D Management Co., Ltd
US Patent
Affinity DataIC50: 1nMAssay Description:Recombinant FGFR1 (2.5 nM), FGFR2 (1 nM), FGFR3 (5 nM), or FGFR4 (12 nM) (Invitrogen™) was prepared as a mixture with substrate KKKSPGEYVNIEFG (SEQ I...More data for this Ligand-Target Pair
TargetFibroblast growth factor receptor 4(Homo sapiens (Human))
Eisai R&D Management Co., Ltd
US Patent
Eisai R&D Management Co., Ltd
US Patent
Affinity DataIC50: 0.100nMAssay Description:Recombinant FGFR1 (2.5 nM), FGFR2 (1 nM), FGFR3 (5 nM), or FGFR4 (12 nM) (Invitrogen™) was prepared as a mixture with substrate KKKSPGEYVNIEFG (SEQ I...More data for this Ligand-Target Pair
Affinity DataIC50: 513nMAssay Description:Recombinant FGFR1 (2.5 nM), FGFR2 (1 nM), FGFR3 (5 nM), or FGFR4 (12 nM) (Invitrogen™) was prepared as a mixture with substrate KKKSPGEYVNIEFG (SEQ I...More data for this Ligand-Target Pair
Affinity DataIC50: 210nMAssay Description:The following method was used to determine the inhibition degree of the kinase activity of recombinant human FGFR protein by the compounds of the pre...More data for this Ligand-Target Pair
TargetFibroblast growth factor receptor 2(Homo sapiens (Human))
Eisai R&D Management Co., Ltd
US Patent
Eisai R&D Management Co., Ltd
US Patent
Affinity DataIC50: 579nMAssay Description:The following method was used to determine the inhibition degree of the kinase activity of recombinant human FGFR protein by the compounds of the pre...More data for this Ligand-Target Pair
TargetFibroblast growth factor receptor 3(Homo sapiens (Human))
Eisai R&D Management Co., Ltd
US Patent
Eisai R&D Management Co., Ltd
US Patent
Affinity DataIC50: 575nMAssay Description:The following method was used to determine the inhibition degree of the kinase activity of recombinant human FGFR protein by the compounds of the pre...More data for this Ligand-Target Pair
TargetFibroblast growth factor receptor 4(Homo sapiens (Human))
Eisai R&D Management Co., Ltd
US Patent
Eisai R&D Management Co., Ltd
US Patent
Affinity DataIC50: 14nMAssay Description:The following method was used to determine the inhibition degree of the kinase activity of recombinant human FGFR protein by the compounds of the pre...More data for this Ligand-Target Pair
TargetFibroblast growth factor receptor 2(Homo sapiens (Human))
Eisai R&D Management Co., Ltd
US Patent
Eisai R&D Management Co., Ltd
US Patent
Affinity DataIC50: 1.29E+3nMAssay Description:Inhibition of FGFR2 (unknown origin)More data for this Ligand-Target Pair
TargetFibroblast growth factor receptor 3(Homo sapiens (Human))
Eisai R&D Management Co., Ltd
US Patent
Eisai R&D Management Co., Ltd
US Patent
Affinity DataIC50: 1.06E+3nMAssay Description:Inhibition of FGFR3 (unknown origin)More data for this Ligand-Target Pair