BDBM246868 US10053465, 7::US10065963, Compound 7::US10125150, Example 7::US10336759, # 7::US10479803, Example 7::US10519163, Example 7::US10675284, Example 7::US10875847, Compound INCB39110::US11084822, Example 7::US11130767, # 7::US11136326, Example 7::US11285140, Example 364::US11304949, Compound 1::US11324749, Comp. No. 1::US11406640, Comp. No. 1::US11596632, Comp. No. 1::US11918581, Compound 1::US11957661, Compound 4::US11992490, Compound 1::US20240058343, Compound 1::US20240307353, Compound 4::US9732097, Example 7::US9999619, Example 364::{1-{1-[3-Fluoro-2- (trifluoromethyl) isonicotinoyl] piperidin-4- yl}-3-[4-(7H- pyrrolo[2,3- d]pyrimidin-4-yl)- 1H-pyrazol-1- yl]azetidin-3- yl}acetonitrile
SMILES Fc1c(ccnc1C(F)(F)F)C(=O)N1CCC(CC1)N1CC(CC#N)(C1)n1cc(cn1)-c1ncnc2[nH]ccc12
InChI Key InChIKey=KTBSXLIQKWEBRB-UHFFFAOYSA-N
Data 68 IC50
Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB
Found 68 hits for monomerid = 246868
Affinity DataIC50: 500nMAssay 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: 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: 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: 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: 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: 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: 500nMAssay 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 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: 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: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: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: 75nMAssay 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 were tested for inhibitory activity of JAK targe...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
TargetNon-receptor tyrosine-protein kinase TYK2(Human)
China Pharmaceutical University
Curated by ChEMBL
China Pharmaceutical University
Curated by ChEMBL
Affinity DataIC50: 795nMAssay Description:Inhibition of TYK2 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 2nMAssay Description:Inhibition of JAK1 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 2.00E+3nMAssay Description:Inhibition of JAK3 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 63nMAssay Description:Inhibition of JAK2 (unknown origin)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: 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: 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 are tested for inhibitory activity of JAK target...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: 2nMAssay Description:Inhibition of JAK 1 (unknown origin)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 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 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: 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: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: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: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: 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: 500nMT: 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: 500nMT: 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: 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: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: 1.00E+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: 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: 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: 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