null
SMILES CC[C@@](C)(Nc1ccnc(n1)-c1c[nH]c2ncccc12)C(=O)NCC(F)(F)F
InChI Key InChIKey=ASUGUQWIHMTFJL-QGZVFWFLSA-N
PDB links: 1 PDB ID matches this monomer.
Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB
Found 38 hits for monomerid = 50021655
In DepthDetails
Affinity DataKi: 2.5nMAssay Description:Inhibition of JAK3 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails
In DepthDetails
3D Structure (crystal)Affinity DataKi: 13nMAssay Description:Inhibition of JAK2 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 11nMAssay Description:Inhibition of JAK1 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 619nMAssay Description:Inhibition of JAK2 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 932nMAssay Description:Inhibition of JAK1/JAK3 in human whole blood assessed as inhibition of IL-15-induced STAT-5 phosphorylation preincubated for 45 mins followed by IL-1...More data for this Ligand-Target Pair
TargetNon-receptor tyrosine-protein kinase TYK2/Tyrosine-protein kinase JAK1(Homo sapiens (Human))
Pfizer Inc.
Curated by ChEMBL
Pfizer Inc.
Curated by ChEMBL
Affinity DataIC50: 1.29E+3nMAssay Description:Inhibition of JAK1/TYK2 in human whole blood assessed as inhibition of IFN-alpha-induced STAT-3 phosphorylation preincubated for 45 mins followed by ...More data for this Ligand-Target Pair
TargetNon-receptor tyrosine-protein kinase TYK2/Tyrosine-protein kinase JAK1/Tyrosine-protein kinase JAK2(Homo sapiens (Human))
Pfizer Inc.
Curated by ChEMBL
Pfizer Inc.
Curated by ChEMBL
Affinity DataIC50: 1.87E+3nMAssay Description:Inhibition of JAK1/JAK2/TYK2 in human whole blood assessed as inhibition of IL-6-induced STAT-1 phosphorylation preincubated for 45 mins followed by ...More data for this Ligand-Target Pair
TargetNon-receptor tyrosine-protein kinase TYK2/Tyrosine-protein kinase JAK2(Homo sapiens (Human))
Pfizer Inc.
Curated by ChEMBL
Pfizer Inc.
Curated by ChEMBL
Affinity DataIC50: 1.12E+4nMAssay Description:Inhibition of JAK2/TYK2 in human whole blood assessed as inhibition of IL-23-induced STAT-3 phosphorylation preincubated for 45 mins followed by IL-2...More data for this Ligand-Target Pair
TargetNon-receptor tyrosine-protein kinase TYK2/Tyrosine-protein kinase JAK2(Homo sapiens (Human))
Pfizer Inc.
Curated by ChEMBL
Pfizer Inc.
Curated by ChEMBL
Affinity DataIC50: 1.64E+4nMAssay Description:Inhibition of JAK2/TYK2 in human whole blood assessed as inhibition of IL-12-induced STAT-4 phosphorylation preincubated for 45 mins followed by IL-1...More data for this Ligand-Target Pair
Affinity DataIC50: 1.00E+4nMAssay Description:Inhibition of TYK2 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 1.00E+4nMAssay Description:Inhibition of JAK2 homodimer in human CD34+ cells spiked into human whole blood assessed as inhibition of EPO-induced STAT-5 phosphorylation preincub...More data for this Ligand-Target Pair
Affinity DataIC50: 11nMAssay Description:Inhibition of Tyk2 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 2.5nMAssay Description:Inhibition of JAK3 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 13nMAssay Description:Inhibition of JAK2 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 11nMAssay Description:Inhibition of JAK1 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 20nMpH: 7.5Assay Description:A kinase selectivity panel which measures substrate peptide phosphorylation was set-up for recombinant human Jak1 (aa 866-1154), Jak2 (aa808-1132), J...More data for this Ligand-Target Pair
Affinity DataIC50: 130nMpH: 7.5Assay Description:A kinase selectivity panel which measures substrate peptide phosphorylation was set-up for recombinant human Jak1 (aa 866-1154), Jak2 (aa808-1132), J...More data for this Ligand-Target Pair
Affinity DataIC50: 10nMpH: 7.5Assay Description:A kinase selectivity panel which measures substrate peptide phosphorylation was set-up for recombinant human Jak1 (aa 866-1154), Jak2 (aa808-1132), J...More data for this Ligand-Target Pair
TargetNon-receptor tyrosine-protein kinase TYK2 [888-1187](Homo sapiens (Human))
NOVARTIS AG
US Patent
NOVARTIS AG
US Patent
Affinity DataIC50: 1.50E+3nMpH: 7.5Assay Description:A kinase selectivity panel which measures substrate peptide phosphorylation was set-up for recombinant human Jak1 (aa 866-1154), Jak2 (aa808-1132), J...More data for this Ligand-Target Pair
Affinity DataIC50: 20nMAssay Description:The assays were performed in 384-well, low volume microtiter assay plates in a final reaction volume of 9 ul. Dose-response curves were generated by ...More data for this Ligand-Target Pair
Affinity DataIC50: 130nMAssay Description:The assays were performed in 384-well, low volume microtiter assay plates in a final reaction volume of 9 ul. Dose-response curves were generated by ...More data for this Ligand-Target Pair
Affinity DataIC50: 10nMAssay Description:The assays were performed in 384-well, low volume microtiter assay plates in a final reaction volume of 9 ul. Dose-response curves were generated by ...More data for this Ligand-Target Pair
Affinity DataIC50: 1.50E+3nMAssay Description:The assays were performed in 384-well, low volume microtiter assay plates in a final reaction volume of 9 ul. Dose-response curves were generated by ...More data for this Ligand-Target Pair
Affinity DataIC50: 20nMAssay Description:The assays were performed in 384-well, low volume microtiter assay plates in a final reaction volume of 9 ul. Dose-response curves were generated by ...More data for this Ligand-Target Pair
Affinity DataIC50: 130nMAssay Description:The assays were performed in 384-well, low volume microtiter assay plates in a final reaction volume of 9 ul. Dose-response curves were generated by ...More data for this Ligand-Target Pair
Affinity DataIC50: 10nMAssay Description:The assays were performed in 384-well, low volume microtiter assay plates in a final reaction volume of 9 ul. Dose-response curves were generated by ...More data for this Ligand-Target Pair
TargetNon-receptor tyrosine-protein kinase TYK2 [888-1187](Homo sapiens (Human))
NOVARTIS AG
US Patent
NOVARTIS AG
US Patent
Affinity DataIC50: 1.50E+3nMAssay Description:The assays were performed in 384-well, low volume microtiter assay plates in a final reaction volume of 9 ul. Dose-response curves were generated by ...More data for this Ligand-Target Pair
Affinity DataIC50: 74nMAssay Description:Inhibition of JAK3 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 1.20nMAssay Description:Inhibition of JAK3 (unknown origin) using poly(Glu)4Tyr as substrate assessed as 33P incorporation after 20 mins by scintillation counting analysis i...More data for this Ligand-Target Pair
Affinity DataIC50: 24nMAssay Description:Inhibition of JAK2 (unknown origin) using poly(Glu)4Tyr as substrate assessed as 33P incorporation after 20 mins by scintillation counting analysis i...More data for this Ligand-Target Pair
Affinity DataIC50: 11nMAssay Description:Inhibition of JAK1 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 50nMAssay Description:Inhibition of JAK3 in mouse HT-2 clone A5E cells assessed as inhibition of interleukin-2-induced STAT-5 phosphorylation at Y694 preincubated for 1 hr...More data for this Ligand-Target Pair
Affinity DataIC50: 50nMAssay Description:Inhibition of JAK1 (unknown origin) by cell-based assayMore data for this Ligand-Target Pair
Affinity DataIC50: 13nMAssay Description:Inhibition of JAK1 (unknown origin) using poly(Glu)4Tyr as substrate assessed as 33P incorporation after 20 mins by scintillation counting analysis i...More data for this Ligand-Target Pair