Compile Data Set for Download or QSAR
Report error Found 123 Enz. Inhib. hit(s) with all data for entry = 50008465
TargetCytochrome P450 3A4(Human)
TBA

Curated by ChEMBL
LigandPNGBDBM50507816(Bms-986165 | Deucravacitinib | US12351572, Example...)
Affinity DataEC50: >4.00E+4nMAssay Description:Induction of CYP3A4 (unknown origin) by PXR-transactivation assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/23/2021
Entry Details Article
PubMed
LigandPNGBDBM50507816(Bms-986165 | Deucravacitinib | US12351572, Example...)
Affinity DataIC50: 0.200nMAssay Description:Allosteric inhibition of fluorescein labeled probe binding to His-tagged recombinant human TYK2 pseudokinase JH2 domain (575-869 residues) incubated ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/23/2021
Entry Details Article
PubMed
TargetTyrosine-protein kinase JAK3(Human)
TBA

Curated by ChEMBL
LigandPNGBDBM50463838(CHEMBL4238926)
Affinity DataIC50: 0.700nMAssay Description:Inhibition of JAK3 (unknown origin) in presence of Km ATPMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/23/2021
Entry Details Article
PubMed
TargetTyrosine-protein kinase JAK1(Human)
TBA

Curated by ChEMBL
LigandPNGBDBM50507816(Bms-986165 | Deucravacitinib | US12351572, Example...)
Affinity DataIC50: 1nMAssay Description:Inhibition of fluorescein labeled probe binding to human recombinant JAK1 JH2 incubated for 1 hr by HTRF assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/23/2021
Entry Details Article
PubMed
LigandPNGBDBM50507816(Bms-986165 | Deucravacitinib | US12351572, Example...)
Affinity DataIC50: 2nMAssay Description:Inhibition of TYK2 in human PBMC assessed as decrease in IFNalpha-induced STAT5 phosphorylation in CD3+ T cells preincubated for 1 hr followed by sti...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/23/2021
Entry Details Article
PubMed
LigandPNGBDBM50519518(CHEMBL4557190)
Affinity DataIC50: 4nMAssay Description:Inhibition of JAK1/TYK2 in human Kit225 T cells assessed as inhibition of STAT phosphorylation by luciferase reporter assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/23/2021
Entry Details Article
PubMed
TargetTyrosine-protein kinase JAK1(Human)
TBA

Curated by ChEMBL
LigandPNGBDBM50463838(CHEMBL4238926)
Affinity DataIC50: 4nMAssay Description:Inhibition of JAK1 (unknown origin) in presence of Km ATPMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/23/2021
Entry Details Article
PubMed
TargetTyrosine-protein kinase JAK2(Human)
TBA

Curated by ChEMBL
LigandPNGBDBM50463838(CHEMBL4238926)
Affinity DataIC50: 5nMAssay Description:Inhibition of JAK2 (unknown origin) in presence of Km ATPMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/23/2021
Entry Details Article
PubMed
LigandPNGBDBM50463838(CHEMBL4238926)
Affinity DataIC50: 5nMAssay Description:Inhibition of TYK2 JH1 domain (unknown origin) in presence of Km ATPMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/23/2021
Entry Details Article
PubMed
LigandPNGBDBM50507816(Bms-986165 | Deucravacitinib | US12351572, Example...)
Affinity DataIC50: 5nMAssay Description:Inhibition of JAK1/TYK2 in human Kit225 T cells assessed as inhibition of STAT phosphorylation by luciferase reporter assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/23/2021
Entry Details Article
PubMed
LigandPNGBDBM50519537(CHEMBL4469750)
Affinity DataIC50: 6nMAssay Description:Inhibition of JAK1/TYK2 in human Kit225 T cells assessed as inhibition of STAT phosphorylation by luciferase reporter assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/23/2021
Entry Details Article
PubMed
LigandPNGBDBM50519543(CHEMBL4457060)
Affinity DataIC50: 7nMAssay Description:Inhibition of JAK1/TYK2 in human Kit225 T cells assessed as inhibition of STAT phosphorylation by luciferase reporter assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/23/2021
Entry Details Article
PubMed
LigandPNGBDBM50519520(CHEMBL4571117)
Affinity DataIC50: 8nMAssay Description:Inhibition of JAK1/TYK2 in human Kit225 T cells assessed as inhibition of STAT phosphorylation by luciferase reporter assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/23/2021
Entry Details Article
PubMed
LigandPNGBDBM50519542(CHEMBL4572855)
Affinity DataIC50: 8nMAssay Description:Inhibition of JAK1/TYK2 in human Kit225 T cells assessed as inhibition of STAT phosphorylation by luciferase reporter assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/23/2021
Entry Details Article
PubMed
LigandPNGBDBM50519519(CHEMBL4566158)
Affinity DataIC50: 9nMAssay Description:Inhibition of JAK1/TYK2 in human Kit225 T cells assessed as inhibition of STAT phosphorylation by luciferase reporter assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/23/2021
Entry Details Article
PubMed
LigandPNGBDBM50507816(Bms-986165 | Deucravacitinib | US12351572, Example...)
Affinity DataIC50: 9nMAssay Description:Inhibition of TYK2 in human PBMC assessed as decrease in IL23-induced STAT3 phosphorylation in CD161+/CD3+ T cells preincubated for 1 hr followed by ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/23/2021
Entry Details Article
PubMed
LigandPNGBDBM50519518(CHEMBL4557190)
Affinity DataIC50: 12nMAssay Description:Inhibition of TYK2 in human whole blood assessed as decrease in IFNalpha-induced STAT5 phosphorylation preincubated for 1 hr followed by stimulation ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/23/2021
Entry Details Article
PubMed
LigandPNGBDBM50519532(CHEMBL4443834)
Affinity DataIC50: 12nMAssay Description:Inhibition of JAK1/TYK2 in human Kit225 T cells assessed as inhibition of STAT phosphorylation by luciferase reporter assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/23/2021
Entry Details Article
PubMed
LigandPNGBDBM50519536(CHEMBL4559585)
Affinity DataIC50: 12nMAssay Description:Inhibition of JAK1/TYK2 in human Kit225 T cells assessed as inhibition of STAT phosphorylation by luciferase reporter assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/23/2021
Entry Details Article
PubMed
LigandPNGBDBM50519538(CHEMBL4580625)
Affinity DataIC50: 12nMAssay Description:Inhibition of JAK1/TYK2 in human Kit225 T cells assessed as inhibition of STAT phosphorylation by luciferase reporter assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/23/2021
Entry Details Article
PubMed
LigandPNGBDBM50507816(Bms-986165 | Deucravacitinib | US12351572, Example...)
Affinity DataIC50: 13nMAssay Description:Inhibition of TYK2 in human whole blood assessed as decrease in IFNalpha-induced STAT5 phosphorylation preincubated for 1 hr followed by stimulation ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/23/2021
Entry Details Article
PubMed
LigandPNGBDBM50519520(CHEMBL4571117)
Affinity DataIC50: 13nMAssay Description:Inhibition of TYK2 in human whole blood assessed as decrease in IFNalpha-induced STAT5 phosphorylation preincubated for 1 hr followed by stimulation ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/23/2021
Entry Details Article
PubMed
LigandPNGBDBM50519539(CHEMBL4476261)
Affinity DataIC50: 14nMAssay Description:Inhibition of JAK1/TYK2 in human Kit225 T cells assessed as inhibition of STAT phosphorylation by luciferase reporter assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/23/2021
Entry Details Article
PubMed
LigandPNGBDBM50519535(CHEMBL4565054)
Affinity DataIC50: 15nMAssay Description:Inhibition of JAK1/TYK2 in human Kit225 T cells assessed as inhibition of STAT phosphorylation by luciferase reporter assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/23/2021
Entry Details Article
PubMed
LigandPNGBDBM50519548(CHEMBL4543984)
Affinity DataIC50: 15nMAssay Description:Inhibition of JAK1/TYK2 in human Kit225 T cells assessed as inhibition of STAT phosphorylation by luciferase reporter assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/23/2021
Entry Details Article
PubMed
LigandPNGBDBM50519537(CHEMBL4469750)
Affinity DataIC50: 15nMAssay Description:Inhibition of TYK2 in human whole blood assessed as decrease in IFNalpha-induced STAT5 phosphorylation preincubated for 1 hr followed by stimulation ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/23/2021
Entry Details Article
PubMed
LigandPNGBDBM50519534(CHEMBL4435079)
Affinity DataIC50: 16nMAssay Description:Inhibition of JAK1/TYK2 in human Kit225 T cells assessed as inhibition of STAT phosphorylation by luciferase reporter assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/23/2021
Entry Details Article
PubMed
LigandPNGBDBM50519539(CHEMBL4476261)
Affinity DataIC50: 16nMAssay Description:Inhibition of TYK2 in human whole blood assessed as decrease in IFNalpha-induced STAT5 phosphorylation preincubated for 1 hr followed by stimulation ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/23/2021
Entry Details Article
PubMed
LigandPNGBDBM305821(US10144738, Example 20 | (1r,3r)-3-(Cyanomethyl)-3...)
Affinity DataIC50: 17nMAssay Description:Inhibition of recombinant human TYK2 JH1 kinase domain using 5FAM-KKSRGDYMTMQID as substrate incubated for 135 mins by caliper methodMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/23/2021
Entry Details Article
PubMed
LigandPNGBDBM50519538(CHEMBL4580625)
Affinity DataIC50: 19nMAssay Description:Inhibition of TYK2 in human whole blood assessed as decrease in IFNalpha-induced STAT5 phosphorylation preincubated for 1 hr followed by stimulation ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/23/2021
Entry Details Article
PubMed
LigandPNGBDBM50519531(CHEMBL4474729)
Affinity DataIC50: 22nMAssay Description:Inhibition of JAK1/TYK2 in human Kit225 T cells assessed as inhibition of STAT phosphorylation by luciferase reporter assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/23/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
LigandPNGBDBM50519542(CHEMBL4572855)
Affinity DataIC50: 23nMAssay Description:Inhibition of TYK2 in human whole blood assessed as decrease in IFNalpha-induced STAT5 phosphorylation preincubated for 1 hr followed by stimulation ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/23/2021
Entry Details Article
PubMed
LigandPNGBDBM50519529(CHEMBL4441840)
Affinity DataIC50: 28nMAssay Description:Inhibition of JAK1/TYK2 in human Kit225 T cells assessed as inhibition of STAT phosphorylation by luciferase reporter assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/23/2021
Entry Details Article
PubMed
LigandPNGBDBM50519528(CHEMBL4537259)
Affinity DataIC50: 30nMAssay Description:Inhibition of JAK1/TYK2 in human Kit225 T cells assessed as inhibition of STAT phosphorylation by luciferase reporter assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/23/2021
Entry Details Article
PubMed
TargetTyrosine-protein kinase JAK3(Human)
TBA

Curated by ChEMBL
LigandPNGBDBM209866(PF-06651600 | US9617258, Example 5 | US11111242, E...)
Affinity DataIC50: 33nMAssay Description:Inhibition of JAK3 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/23/2021
Entry Details Article
PubMed
LigandPNGBDBM50519524(CHEMBL4587924)
Affinity DataIC50: 34nMAssay Description:Inhibition of JAK1/TYK2 in human Kit225 T cells assessed as inhibition of STAT phosphorylation by luciferase reporter assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/23/2021
Entry Details Article
PubMed
LigandPNGBDBM50519543(CHEMBL4457060)
Affinity DataIC50: 40nMAssay Description:Inhibition of TYK2 in human whole blood assessed as decrease in IFNalpha-induced STAT5 phosphorylation preincubated for 1 hr followed by stimulation ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/23/2021
Entry Details Article
PubMed
TargetTyrosine-protein kinase JAK1(Human)
TBA

Curated by ChEMBL
LigandPNGBDBM50503287(ABT-494 | Rinvoq | Upadacitinib | US10961228, Exam...)
Affinity DataIC50: 47nMAssay Description:Inhibition of GST-fused recombinant human JAK1 catalytic domain (845-1142 residues) expressed in Sf9 cells in presence of 0.1 mM ATPMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/23/2021
Entry Details Article
PubMed
LigandPNGBDBM50519540(CHEMBL4468025)
Affinity DataIC50: 47nMAssay Description:Inhibition of JAK1/TYK2 in human Kit225 T cells assessed as inhibition of STAT phosphorylation by luciferase reporter assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/23/2021
Entry Details Article
PubMed
LigandPNGBDBM50519522(CHEMBL4578980)
Affinity DataIC50: 51nMAssay Description:Inhibition of JAK1/TYK2 in human Kit225 T cells assessed as inhibition of STAT phosphorylation by luciferase reporter assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/23/2021
Entry Details Article
PubMed
LigandPNGBDBM50519528(CHEMBL4537259)
Affinity DataIC50: 62nMAssay Description:Inhibition of TYK2 in human whole blood assessed as decrease in IFNalpha-induced STAT5 phosphorylation preincubated for 1 hr followed by stimulation ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/23/2021
Entry Details Article
PubMed
LigandPNGBDBM50519521(CHEMBL4582205)
Affinity DataIC50: 63nMAssay Description:Inhibition of JAK1/TYK2 in human Kit225 T cells assessed as inhibition of STAT phosphorylation by luciferase reporter assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/23/2021
Entry Details Article
PubMed
LigandPNGBDBM50519541(CHEMBL4527672)
Affinity DataIC50: 64nMAssay Description:Inhibition of JAK1/TYK2 in human Kit225 T cells assessed as inhibition of STAT phosphorylation by luciferase reporter assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/23/2021
Entry Details Article
PubMed
LigandPNGBDBM50519536(CHEMBL4559585)
Affinity DataIC50: 69nMAssay Description:Inhibition of TYK2 in human whole blood assessed as decrease in IFNalpha-induced STAT5 phosphorylation preincubated for 1 hr followed by stimulation ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/23/2021
Entry Details Article
PubMed
LigandPNGBDBM50519533(CHEMBL4572426)
Affinity DataIC50: 70nMAssay Description:Inhibition of JAK1/TYK2 in human Kit225 T cells assessed as inhibition of STAT phosphorylation by luciferase reporter assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/23/2021
Entry Details Article
PubMed
TargetTyrosine-protein kinase JAK2(Human)
TBA

Curated by ChEMBL
LigandPNGBDBM305821(US10144738, Example 20 | (1r,3r)-3-(Cyanomethyl)-3...)
Affinity DataIC50: 74nMAssay Description:Inhibition of recombinant human JAK2 kinase domain using FITC-KGGEEEEYFELVKK as substrate incubated for 60 mins by caliper methodMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/23/2021
Entry Details Article
PubMed
LigandPNGBDBM50519526(CHEMBL4524832)
Affinity DataIC50: 78nMAssay Description:Inhibition of JAK1/TYK2 in human Kit225 T cells assessed as inhibition of STAT phosphorylation by luciferase reporter assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/23/2021
Entry Details Article
PubMed
LigandPNGBDBM50519519(CHEMBL4566158)
Affinity DataIC50: 79nMAssay Description:Inhibition of TYK2 in human whole blood assessed as decrease in IFNalpha-induced STAT5 phosphorylation preincubated for 1 hr followed by stimulation ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/23/2021
Entry Details Article
PubMed
LigandPNGBDBM50519535(CHEMBL4565054)
Affinity DataIC50: 87nMAssay Description:Inhibition of TYK2 in human whole blood assessed as decrease in IFNalpha-induced STAT5 phosphorylation preincubated for 1 hr followed by stimulation ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/23/2021
Entry Details Article
PubMed
LigandPNGBDBM50519520(CHEMBL4571117)
Affinity DataIC50: 100nMAssay Description:Inhibition of TYK2 in mouse whole blood assessed as decrease in IFNalpha-induced STAT1 phosphorylation preincubated for 1 hr followed by stimulation ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/23/2021
Entry Details Article
PubMed
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