BDBM246864 3-(1- [1,3]oxazolo[5,4- b]pyridin-2- ylpyrrolidin-3-yl)-3- [4-(7H-pyrrolo[2,3- d]pyrimidin-4-yl)- 1H-pyrazol-1- yl]propanenitrile::US10053465, 4::US10065963, Compound 4::US10125150, Example 4::US10336759, # 4::US10479803, Example 4::US10519163, Example 4::US10675284, Example 4::US11084822, Example 4::US11130767, # 4::US11136326, Example 4::US11304949, Compound 7::US11324749, Comp. No. 7::US11406640, Comp. No. 7::US11596632, Comp. No. 7::US11918581, Compound 7::US11957661, Compound 7::US11992490, Compound 7::US20240058343, Compound 7::US20240307353, Compound 7::US9732097, Example 4
SMILES N#CCC(C1CCN(C1)c1nc2cccnc2o1)n1cc(cn1)-c1ncnc2[nH]ccc12
InChI Key InChIKey=HTGGWBJDPLPEPS-UHFFFAOYSA-N
Data 38 IC50
Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB
Found 38 hits for monomerid = 246864
Affinity DataIC50: 10nMAssay Description:Selective JAK1 inhibitors that can be used in combination with an immunomodulatory agent and steroid for the treatment of hematological diseases or d...More data for this Ligand-Target Pair
Affinity DataIC50: 10nMAssay Description:JAK1 pathway inhibitors that can be used for the treatment of cytokine-related diseases or disorders are tested for inhibitory activity of JAK target...More data for this Ligand-Target Pair
Affinity DataIC50: 10nMAssay Description:Assays are carried out at room temperature in 50 mM HEPES, pH 7.4, 5 mM MgCl2, 50 mM NaCl, 5 mM DTT and CHAPS 0.04%. Reactions are initiated by the a...More data for this Ligand-Target Pair
Affinity DataIC50: 10nMAssay Description:The compounds in Table 1 were tested for inhibitory activity of JAK targets according to the following in vitro assay described in Park et al., Analy...More data for this Ligand-Target Pair
Affinity DataIC50: 10nMAssay Description:The IC50s obtained by the method of Assay A at 1 mM ATP as described in the US Patent Publications.More data for this Ligand-Target Pair
Affinity DataIC50: 750nMAssay Description:The kinase assay buffer contained 50 mM HEPES, pH7.5, 10 mM MgCl2, 1 mM EGTA, 0.01% NP-40 and 2 mM DTT. 0.1 ul test compounds dissolved in DMSO were ...More data for this Ligand-Target Pair
Affinity DataIC50: 750nMAssay Description:The kinase assay buffer contained 50 mM HEPES, pH7.5, 10 mM MgCl2, 1 mM EGTA, 0.01% NP-40 and 2 mM DTT. 0.1 ul test compounds dissolved in DMSO were ...More data for this Ligand-Target Pair
Affinity DataIC50: 3.00E+3nMAssay Description:The kinase assay buffer contained 50 mM HEPES, pH7.5, 10 mM MgCl2, 1 mM EGTA, 0.01% NP-40 and 2 mM DTT. 0.1 ul test compounds dissolved in DMSO were ...More data for this Ligand-Target Pair
Affinity DataIC50: 10nMAssay Description:JAK1 inhibitors that can be used for the treatment of cytokine-related diseases or disorders are tested for inhibitory activity of JAK targets accord...More data for this Ligand-Target Pair
Affinity DataIC50: 10nMAssay Description:JAK1 pathway inhibitors that can be used for the treatment of cytokine-related diseases or disorders are tested for inhibitory activity of JAK target...More data for this Ligand-Target Pair
Affinity DataIC50: 50nMAssay Description:Compounds herein were tested for inhibitory activity of JAK targets according to the following in vitro assay described in Park et al., Analytical Bi...More data for this Ligand-Target Pair
Affinity DataIC50: 10nMAssay Description:JAK1 inhibitors that can be used for the treatment of cytokine-related diseases or disorders are tested for inhibitory activity of JAK targets accord...More data for this Ligand-Target Pair
Affinity DataIC50: 10nMAssay Description:JAK1 pathway inhibitors that can be used for the treatment of cytokine-related diseases or disorders are tested for inhibitory activity of JAK target...More data for this Ligand-Target Pair
Affinity DataIC50: 10nMAssay Description:JAK1 pathway inhibitors that can be used for the treatment of cytokine-related diseases or disorders were tested for inhibitory activity of JAK targe...More data for this Ligand-Target Pair
Affinity DataIC50: 10nMAssay Description:JAK1 pathway inhibitors that can be used for the treatment of cytokine-related diseases or disorders were tested for inhibitory activity of JAK targe...More data for this Ligand-Target Pair
Affinity DataIC50: 10nMAssay Description:Selective JAK1 inhibitors that can be used in combination with a ROCK inhibitor as described herein are tested for inhibitory activity of JAK targets...More data for this Ligand-Target Pair
Affinity DataIC50: 10nMAssay Description:JAK1 inhibitors that can be used for the treatment of cytokine-related diseases or disorders are tested for inhibitory activity of JAK targets accord...More data for this Ligand-Target Pair
Affinity DataIC50: 750nMT: 2°CAssay Description:The kinase assay buffer contained 50 mM HEPES, pH7.5, 10 mM MgCl2, 1 mM EGTA, 0.01% NP-40 and 2 mM DTT. 0.1 ul test compounds dissolved in DMSO were ...More data for this Ligand-Target Pair
Affinity DataIC50: 10nMAssay Description:As used herein, a selective JAK1 inhibitor is an inhibitor of JAK1 which is selective for JAK1 over JAK2, JAK3 and TYK2. In some embodiments, the com...More data for this Ligand-Target Pair
Affinity DataIC50: 100nMT: 2°CAssay Description:The kinase assay buffer contained 50 mM HEPES, pH7.5, 10 mM MgCl2, 1 mM EGTA, 0.01% NP-40 and 2 mM DTT. 0.1 ul test compounds dissolved in DMSO were ...More data for this Ligand-Target Pair
Affinity DataIC50: 750nMT: 2°CAssay Description:The kinase assay buffer contained 50 mM HEPES, pH7.5, 10 mM MgCl2, 1 mM EGTA, 0.01% NP-40 and 2 mM DTT. 0.1 ul test compounds dissolved in DMSO were ...More data for this Ligand-Target Pair
Affinity DataIC50: 300nMT: 2°CAssay Description:The kinase assay buffer contained 50 mM HEPES, pH7.5, 10 mM MgCl2, 1 mM EGTA, 0.01% NP-40 and 2 mM DTT. 0.1 ul test compounds dissolved in DMSO were ...More data for this Ligand-Target Pair
Affinity DataIC50: 10nMAssay Description:In some embodiments, the additional pharmaceutical agent is a JAK1 and/or JAK2 inhibitor. In some embodiments, the present application provides a met...More data for this Ligand-Target Pair
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform(Human)
Incyte
US Patent
Incyte
US Patent
Affinity DataIC50: 100nMpH: 6.7 T: 2°CAssay Description:[γ-33P]ATP (10 mCi/mL) was purchased from PerkinElmer (Waltham, Mass.). Lipid kinase substrate, D-myo-Phosphatidylinositol 4,5-bisphosphate (Ptd...More data for this Ligand-Target Pair
Affinity DataIC50: 100nMpH: 7.8 T: 2°CAssay Description:Compounds herein were tested for inhibitory activity of JAK targets according to the following in vitro assay described in Park et al., Analytical Bi...More data for this Ligand-Target Pair
Affinity DataIC50: 10nMAssay Description:As used herein, a selective JAK1 inhibitor is an inhibitor of JAK1 which is selective for JAK1 over JAK2, JAK3 and TYK2. In some embodiments, the com...More data for this Ligand-Target Pair
Affinity DataIC50: 750nMT: 2°CAssay Description:The kinase assay buffer contained 50 mM HEPES, pH7.5, 10 mM MgCl2, 1 mM EGTA, 0.01% NP-40 and 2 mM DTT. 0.1 ul test compounds dissolved in DMSO were ...More data for this Ligand-Target Pair
Affinity DataIC50: 10nMAssay Description:The compounds in Table A were tested for inhibitory activity of JAK targets according to the following in vitro assay described in Park et al., Analy...More data for this Ligand-Target Pair
Affinity DataIC50: 3.00E+3nMT: 2°CAssay Description:The kinase assay buffer contained 50 mM HEPES, pH7.5, 10 mM MgCl2, 1 mM EGTA, 0.01% NP-40 and 2 mM DTT. 0.1 ul test compounds dissolved in DMSO were ...More data for this Ligand-Target Pair
Affinity DataIC50: 10nMAssay Description:The kinase reaction was conducted in clear-bottom 96-well plate from Thermo Fisher Scientific in a final volume of 24 μL. Inhibitors were first ...More data for this Ligand-Target Pair
Affinity DataIC50: 10nMAssay Description:PI3-Kinase luminescent assay kit including lipid kinase substrate, D-myo-phosphatidylinositol 4,5-bisphosphate (PtdIns(4,5)P2)D (+)-sn-1,2-di-O-octan...More data for this Ligand-Target Pair
Affinity DataIC50: 750nMAssay Description:The kinase assay buffer contained 50 mM HEPES, pH7.5, 10 mM MgCl2, 1 mM EGTA, 0.01% NP-40 and 2 mM DTT. 0.1 ul test compounds dissolved in DMSO were ...More data for this Ligand-Target Pair
Affinity DataIC50: 750nMAssay Description:The kinase assay buffer contained 50 mM HEPES, pH7.5, 10 mM MgCl2, 1 mM EGTA, 0.01% NP-40 and 2 mM DTT. 0.1 ul test compounds dissolved in DMSO were ...More data for this Ligand-Target Pair
Affinity DataIC50: 3.00E+3nMAssay Description:The kinase assay buffer contained 50 mM HEPES, pH7.5, 10 mM MgCl2, 1 mM EGTA, 0.01% NP-40 and 2 mM DTT. 0.1 ul test compounds dissolved in DMSO were ...More data for this Ligand-Target Pair
Affinity DataIC50: 10nMAssay Description:PI3K: The kinase reactions are conducted in clear-bottom 96-well plate from Thermo Fisher Scientific in a final volume of 24 μL. Inhibitors are ...More data for this Ligand-Target Pair
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform(Human)
Incyte
US Patent
Incyte
US Patent
Affinity DataIC50: 10nMAssay Description:PI3Kδ:The kinase reaction was conducted in polystyrene 384-well matrix white plate from Thermo Fisher Scientific in a final volume of 25 μL...More data for this Ligand-Target Pair