BDBM246870 US10053465, 9::US10065963, Compound 9::US10125150, Example 9::US10336759, # 9::US10479803, Example 9::US10675284, Example 9::US11084822, Example 9::US11130767, # 9::US11136326, Example 9::US11285140, Example 85::US11304949, Compound 3::US11324749, Comp. No. 3::US11406640, Comp. No. 3::US11596632, Comp. No. 3::US20240058343, Compound 3::US9732097, Example 9::US9999619, Example 86::[3-[4-(7H- pyrrolo[2,3- d]pyrimidin-4-yl)- 1H-pyrazol-1-yl]-1- (1-{[2- (trifluoromethyl) pyrimidin-4- yl]carbonyl} piperidin-4-yl) azetidin-3- yl]acetonitrile
SMILES FC(F)(F)c1nccc(n1)C(=O)N1CCC(CC1)N1CC(CC#N)(C1)n1cc(cn1)-c1ncnc2[nH]ccc12
InChI Key InChIKey=QFPGZAJRDFHPCE-UHFFFAOYSA-N
Data 26 IC50
Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB
Found 26 hits for monomerid = 246870
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: <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: <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: 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
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: <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: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: 25nMAssay 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: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: <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
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: 12.5nMAssay Description:The catalytic domains of human JAK1 (a.a. 837-1142), Jak2 (a.a. 828-1132) and Jak3 (a.a. 781-1124) with an N-terminal His tag were expressed using ba...More data for this Ligand-Target Pair
Affinity DataIC50: >100nMAssay Description:The catalytic domains of human JAK1 (a.a. 837-1142), Jak2 (a.a. 828-1132) and Jak3 (a.a. 781-1124) with an N-terminal His tag were expressed using ba...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: 12.5nMAssay 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: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 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: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