BDBM209866 PF-06651600::US11111242, Example 5::US20230348487, Example PF-06651600::US9617258, Example 5
SMILES C[C@H]1CC[C@H](CN1C(=O)C=C)Nc1ncnc2[nH]ccc12
InChI Key InChIKey=CBRJPFGIXUFMTM-UHFFFAOYSA-N
Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB
Found 97 hits for monomerid = 209866
Affinity DataKi: 0.0269nMpH: 7.5Assay Description:Assay buffer was 20 mM HEPES, pH 7.5, 10 mM MgCl2, 0.01% BSA, 1 mM DTT, 0.0005% Tween 20, and 2% DMSO. Inactivation kinetic reactions were performed ...More data for this Ligand-Target Pair
Affinity DataKi: 0.131nMpH: 7.5Assay Description:Assay buffer was 20 mM HEPES, pH 7.5, 10 mM MgCl2, 0.01% BSA, 1 mM DTT, 0.0005% Tween 20, and 2% DMSO. Inactivation kinetic reactions were performed ...More data for this Ligand-Target Pair
Affinity DataIC50: 0.300nMAssay Description:Test article was solubilized in dimethyl sulfoxide (DMSO) to a stock concentration of 30 mM. An 11-point half log dilution series was created in DMSO...More data for this Ligand-Target Pair
Affinity DataIC50: 0.300nMAssay Description:Inhibition of recombinant human GST-tagged JAK3 JH1 domain using KAIETDKEYYTVKD-NH2 as substrate in presence of ATP at Km concentration by coupled PK...More data for this Ligand-Target Pair
Affinity DataIC50: 0.300nMAssay Description:Inhibition of recombinant human GST-tagged cytoplasmic JAK3 catalytic domain (781 to 1124 residues) expressed in baculovirus expression system using ...More data for this Ligand-Target Pair
Affinity DataIC50: 0.300nMAssay Description:Test article was solubilized in dimethyl sulfoxide (DMSO) to a stock concentration of 30 mM. An 11-point half log dilution series was created in DMSO...More data for this Ligand-Target Pair
Affinity DataIC50: 0.300nMAssay Description:JAK Caliper Enzyme Assay at 4 μM: Test article was solubilized in dimethyl sulfoxide (DMSO) to a stock concentration of 30 mM. An 11-point half ...More data for this Ligand-Target Pair
Affinity DataIC50: 0.300nMAssay Description:Inhibition of human recombinant GST tagged JAK3 kinase domain (781 to 1124 amino acids) expressed in insect cells in presence of ATPMore data for this Ligand-Target Pair
Affinity DataIC50: 0.346nMpH: 7.4 T: 2°CAssay Description:Test compounds were solubilized in dimethyl sulfoxide (DMSO) to a stock concentration of 30 mM. Compounds were diluted in DMSO to create an 11-point ...More data for this Ligand-Target Pair
Affinity DataIC50: 0.350nMAssay Description:Inhibition of JAK3 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 0.400nMAssay Description:Inhibition of human N-terminal His-tagged JAK3 (795 to 1124 residues) expressed in baculovirus expression system in presence of 6 uM ATP by HTRF assa...More data for this Ligand-Target Pair
Affinity DataKi: 0.545nMpH: 7.5Assay Description:Assay buffer was 20 mM HEPES, pH 7.5, 10 mM MgCl2, 0.01% BSA, 1 mM DTT, 0.0005% Tween 20, and 2% DMSO. Inactivation kinetic reactions were performed ...More data for this Ligand-Target Pair
Affinity DataKi: 0.679nMpH: 7.5Assay Description:Assay buffer was 20 mM HEPES, pH 7.5, 10 mM MgCl2, 0.01% BSA, 1 mM DTT, 0.0005% Tween 20, and 2% DMSO. Inactivation kinetic reactions were performed ...More data for this Ligand-Target Pair
Affinity DataIC50: 2.30nMAssay Description:Inhibition of GST tagged recombinant human JAK3 expressed in baculovirus infection system by FRET assayMore data for this Ligand-Target Pair
Affinity DataIC50: 2.32nMAssay Description:Test method: Firstly, test compounds were prepared into 10 mM stock solution with DMSO, and continuously diluted into 10 concentrations at a 3-fold g...More data for this Ligand-Target Pair
Affinity DataIC50: 2.42nMAssay Description:Test method: Firstly, test compounds were prepared into 10 mM stock solution with DMSO, and continuously diluted into 10 concentrations at a 3-fold g...More data for this Ligand-Target Pair
Affinity DataKi: 6.31nMpH: 7.5Assay Description:Assay buffer was 20 mM HEPES, pH 7.5, 10 mM MgCl2, 0.01% BSA, 1 mM DTT, 0.0005% Tween 20, and 2% DMSO. Inactivation kinetic reactions were performed ...More data for this Ligand-Target Pair
Affinity DataKi: 27nMAssay Description:Inhibition of full length recombinant human GST-tagged cytoplasmic ITK expressed in baculovirus expression system by KT236 probe based TR-FRET assayMore data for this Ligand-Target Pair
Affinity DataKi: 32.4nMpH: 7.5Assay Description:Assay buffer was 20 mM HEPES, pH 7.5, 10 mM MgCl2, 0.01% BSA, 1 mM DTT, 0.0005% Tween 20, and 2% DMSO. Inactivation kinetic reactions were performed ...More data for this Ligand-Target Pair
Affinity DataIC50: 33nMAssay Description:Inhibition of recombinant human GST-tagged cytoplasmic JAK3 catalytic domain (781 to 1124 residues) expressed in baculovirus expression system using ...More data for this Ligand-Target Pair
Affinity DataIC50: 33nMAssay Description:Inhibition of JAK3 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 33nMAssay Description:Inhibition of JAK3 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 33nMAssay Description:Inhibition of JAK3 (unknown origin) in presence of ATPMore data for this Ligand-Target Pair
Affinity DataIC50: 33nMAssay Description:Inhibition of human recombinant His-tagged JAK3 expressed in baculovirus-infected Sf21 cells using FITC-KGGEEEEYFELVKK as substrate by fluorescence b...More data for this Ligand-Target Pair
Affinity DataIC50: 33nMAssay Description:Inhibition of recombinant human GST-tagged JAK3 JH1 domain using KAIETDKEYYTVKD-NH2 as substrate in presence of 1 mM ATP concentration by coupled PK/...More data for this Ligand-Target Pair
Affinity DataIC50: 33nMAssay Description:Inhibition of JAK 3 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 33nMAssay Description:Inhibition of recombinant human JAK3 assessed as phosphorylation level in presence of 1 mM ATPMore data for this Ligand-Target Pair
Affinity DataIC50: 33.1nMpH: 7.4 T: 2°CAssay Description:Test compounds were solubilized in dimethyl sulfoxide (DMSO) to a stock concentration of 30 mM. Compounds were diluted in DMSO to create an 11-point ...More data for this Ligand-Target Pair
Affinity DataIC50: 33.1nMAssay Description:Test article was solubilized in dimethyl sulfoxide (DMSO) to a stock concentration of 30 mM. An 11-point half log dilution series was created in DMSO...More data for this Ligand-Target Pair
Affinity DataIC50: 33.1nMAssay Description:Test article was solubilized in dimethyl sulfoxide (DMSO) to a stock concentration of 30 mM. An 11-point half log dilution series was created in DMSO...More data for this Ligand-Target Pair
Affinity DataIC50: 33.1nMAssay Description:JAK Caliper Enzyme Assay at 1 mM ATP: Test article was solubilized in dimethyl sulfoxide (DMSO) to a stock concentration of 30 mM. An 11-point half l...More data for this Ligand-Target Pair
Affinity DataIC50: 51nMAssay Description:Inhibition of JAK3 in human PBMC assessed as inhibition of IL-15 induced STAT5 phosphorylation preincubated for 75 mins followed by IL-15 addition an...More data for this Ligand-Target Pair
Affinity DataKi: 62.3nMpH: 7.5Assay Description:Assay buffer was 20 mM HEPES, pH 7.5, 10 mM MgCl2, 0.01% BSA, 1 mM DTT, 0.0005% Tween 20, and 2% DMSO. Inactivation kinetic reactions were performed ...More data for this Ligand-Target Pair
Affinity DataIC50: 90nMAssay Description:Inhibition of recombinant human GST-tagged cytoplasmic JAK3 catalytic domain (781 to 1124 residues) expressed in baculovirus expression system in pre...More data for this Ligand-Target Pair
Affinity DataIC50: 106nMAssay Description:Inhibition of JAK3 in human whole blood assessed as free drug concentration required for inhibition of IL-15 induced STAT5 phosphorylation preincubat...More data for this Ligand-Target Pair
Affinity DataKi: 131nMAssay Description:Inhibition of recombinant human N-terminal GST-tagged TXK using GEPLYWSFPAKKK as substrate measured every 60 secs for 1 hr by PK/LDH coupled spectrop...More data for this Ligand-Target Pair
Affinity DataIC50: 155nMAssay Description:Inhibition of TEC (unknown origin) in presence of ATPMore data for this Ligand-Target Pair
Affinity DataIC50: 193nMAssay Description:Inhibition of recombinant human N-terminal GST-tagged TXK using GEPLYWSFPAKKK as substrate in presence of 1 mM ATP measured every 60 secs for 1 hr by...More data for this Ligand-Target Pair
Affinity DataIC50: 194nMpH: 7.4 T: 2°CAssay Description:Test compounds were solubilized in dimethyl sulfoxide (DMSO) to a stock concentration of 30 mM. Compounds were diluted in DMSO to create an 11-point ...More data for this Ligand-Target Pair
Affinity DataIC50: 197nMAssay Description:Inhibition of JAK3 in human whole blood assessed as inhibition of IL-15 induced STAT5 phosphorylation preincubated for 45 mins followed by IL-15 addi...More data for this Ligand-Target Pair
Affinity DataIC50: 202nMAssay Description:Inhibition of human N-terminal His-tagged JAK3 (795 to 1124 residues) expressed in baculovirus expression system in presence of 1 mM ATP by HTRF assa...More data for this Ligand-Target Pair
Affinity DataKi: 545nMAssay Description:Inhibition of full length recombinant human His-tagged cytoplasmic BMX expressed in baculovirus expression system by KT236 probe based TR-FRET assayMore data for this Ligand-Target Pair
Affinity DataIC50: 592nMAssay Description:Inhibition of full length human His-tagged TEC in presence of 1 mM ATP by KT178 probe based TR-FRET assayMore data for this Ligand-Target Pair
Affinity DataIC50: 592nMpH: 7.4 T: 2°CAssay Description:Test compounds were solubilized in dimethyl sulfoxide (DMSO) to a stock concentration of 30 mM. Compounds were diluted in DMSO to create an 11-point ...More data for this Ligand-Target Pair
Affinity DataIC50: 606nMAssay Description:Inhibition of full length recombinant human His-tagged cytoplasmic BMX expressed in baculovirus expression system in presence of 1 mM ATP by KT236 pr...More data for this Ligand-Target Pair
Affinity DataIC50: 606nMpH: 7.4 T: 2°CAssay Description:Test compounds were solubilized in dimethyl sulfoxide (DMSO) to a stock concentration of 30 mM. Compounds were diluted in DMSO to create an 11-point ...More data for this Ligand-Target Pair
Affinity DataIC50: 607nMAssay Description:Inhibition of full length recombinant human His-tagged cytoplasmic BTK expressed in baculovirus expression system in presence of 1 mM ATP by KT236 pr...More data for this Ligand-Target Pair
Affinity DataIC50: 608nMpH: 7.4 T: 2°CAssay Description:Test compounds were solubilized in dimethyl sulfoxide (DMSO) to a stock concentration of 30 mM. Compounds were diluted in DMSO to create an 11-point ...More data for this Ligand-Target Pair
Affinity DataKi: 679nMAssay Description:Inhibition of full length human His-tagged TEC by KT178 probe based TR-FRET assayMore data for this Ligand-Target Pair
Affinity DataIC50: 1.51E+3nMpH: 7.4 T: 2°CAssay Description:Test compounds were solubilized in dimethyl sulfoxide (DMSO) to a stock concentration of 30 mM. Compounds were diluted in DMSO to create an 11-point ...More data for this Ligand-Target Pair