Compile Data Set for Download or QSAR
Report error Found 63 Enz. Inhib. hit(s) with all data for entry = 50044594
TargetTyrosine-protein kinase JAK3(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50021655(VRT-831509 | VX-509 | DECERNOTINIB | US10112907, E...)
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
In Depth
Date in BDB:
2/12/2015
Entry Details Article
PubMed
TargetTyrosine-protein kinase JAK3(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50193995(CP-690550 | 3-((3R,4R)-4-methyl-3-(methyl(7H-pyrro...)
Affinity DataIC50: 1.60nMAssay Description:Inhibition of recombinant JAK3 kinase domain (unknown origin) using FITC-KGGEEEEYFELVKK as substrate assessed as inhibition of substrate phosphorylat...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/12/2015
Entry Details Article
PubMed
TargetTyrosine-protein kinase JAK3(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50021655(VRT-831509 | VX-509 | DECERNOTINIB | US10112907, E...)
Affinity DataKi:  2.5nMAssay Description:Inhibition of JAK3 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/12/2015
Entry Details Article
PubMed
TargetTyrosine-protein kinase JAK1(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50193995(CP-690550 | 3-((3R,4R)-4-methyl-3-(methyl(7H-pyrro...)
Affinity DataIC50: 3.20nMAssay Description:Inhibition of recombinant GST-fused JAK1 kinase domain (852 to 1142) (unknown origin) using 5-FAM-KKSRGDYMTMQIG as substrate assessed as inhibition o...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/12/2015
Entry Details Article
PubMed
TargetTyrosine-protein kinase JAK1(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50021656(LY-3009104 | INCB-028050 | BARICITINIB | US1011290...)
Affinity DataIC50: 4nMAssay Description:Inhibition of JAK1 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/12/2015
Entry Details Article
PubMed
TargetTyrosine-protein kinase JAK2(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50193995(CP-690550 | 3-((3R,4R)-4-methyl-3-(methyl(7H-pyrro...)
Affinity DataIC50: 4.10nMAssay Description:Inhibition of recombinant JAK2 kinase domain (unknown origin) using FITC-KGGEEEEYFELVKK as substrate assessed as inhibition of substrate phosphorylat...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/12/2015
Entry Details Article
PubMed
TargetTyrosine-protein kinase JAK1(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50355501(RUXOLITINIB PHOSPHATE | INCB-018424 | RUXOLITINIB ...)
Affinity DataIC50: 6.40nMAssay Description:Inhibition of JAK1 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/12/2015
Entry Details Article
PubMed
TargetTyrosine-protein kinase JAK2(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50021656(LY-3009104 | INCB-028050 | BARICITINIB | US1011290...)
Affinity DataIC50: 6.60nMAssay Description:Inhibition of JAK2 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/12/2015
Entry Details Article
PubMed
TargetTyrosine-protein kinase JAK2(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50355501(RUXOLITINIB PHOSPHATE | INCB-018424 | RUXOLITINIB ...)
Affinity DataIC50: 8.80nMAssay Description:Inhibition of JAK2 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/12/2015
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetTyrosine-protein kinase JAK1(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50021655(VRT-831509 | VX-509 | DECERNOTINIB | US10112907, E...)
Affinity DataIC50: 11nMAssay Description:Inhibition of JAK1 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/12/2015
Entry Details Article
PubMed
TargetTyrosine-protein kinase JAK1(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50021655(VRT-831509 | VX-509 | DECERNOTINIB | US10112907, E...)
Affinity DataIC50: 11nMAssay Description:Inhibition of JAK1 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/12/2015
Entry Details Article
PubMed
TargetTyrosine-protein kinase JAK1(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50021655(VRT-831509 | VX-509 | DECERNOTINIB | US10112907, E...)
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
In Depth
Date in BDB:
2/12/2015
Entry Details Article
PubMed
TargetTyrosine-protein kinase JAK2(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50021655(VRT-831509 | VX-509 | DECERNOTINIB | US10112907, E...)
Affinity DataKi:  13nMAssay Description:Inhibition of JAK2 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/12/2015
Entry Details Article
PubMed
TargetTyrosine-protein kinase JAK1(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50193995(CP-690550 | 3-((3R,4R)-4-methyl-3-(methyl(7H-pyrro...)
Affinity DataIC50: 15nMAssay Description:Inhibition of JAK1 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/12/2015
Entry Details Article
PubMed
LigandPNGBDBM50021656(LY-3009104 | INCB-028050 | BARICITINIB | US1011290...)
Affinity DataIC50: 21nMAssay 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
In Depth
Date in BDB:
2/12/2015
Entry Details Article
PubMed
TargetTyrosine-protein kinase JAK2(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50021655(VRT-831509 | VX-509 | DECERNOTINIB | US10112907, E...)
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
In Depth
Date in BDB:
2/12/2015
Entry Details Article
PubMed
LigandPNGBDBM50021656(LY-3009104 | INCB-028050 | BARICITINIB | US1011290...)
Affinity DataIC50: 29nMAssay 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
In Depth
Date in BDB:
2/12/2015
Entry Details Article
PubMed
LigandPNGBDBM50355501(RUXOLITINIB PHOSPHATE | INCB-018424 | RUXOLITINIB ...)
Affinity DataIC50: 30nMAssay Description:Inhibition of TYK2 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/12/2015
Entry Details Article
PubMed
LigandPNGBDBM50193995(CP-690550 | 3-((3R,4R)-4-methyl-3-(methyl(7H-pyrro...)
Affinity DataIC50: 34nMAssay Description:Inhibition of recombinant GST-fused TYK2 kinase domain (870 to 1187) (unknown origin) harboring C1187S modification using 5-FAM-KKSRGDYMTMQIG as subs...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/12/2015
Entry Details Article
PubMed
LigandPNGBDBM50193995(CP-690550 | 3-((3R,4R)-4-methyl-3-(methyl(7H-pyrro...)
Affinity DataIC50: 35nMAssay 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
In Depth
Date in BDB:
2/12/2015
Entry Details Article
PubMed
TargetTyrosine-protein kinase JAK3(Mouse)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50021655(VRT-831509 | VX-509 | DECERNOTINIB | US10112907, E...)
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
In Depth
Date in BDB:
2/12/2015
Entry Details Article
PubMed
TargetTyrosine-protein kinase JAK1(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50021655(VRT-831509 | VX-509 | DECERNOTINIB | US10112907, E...)
Affinity DataIC50: 50nMAssay Description:Inhibition of JAK1 (unknown origin) by cell-based assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/12/2015
Entry Details Article
PubMed
TargetTyrosine-protein kinase JAK3(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50193995(CP-690550 | 3-((3R,4R)-4-methyl-3-(methyl(7H-pyrro...)
Affinity DataIC50: 55nMAssay Description:Inhibition of JAK3 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/12/2015
Entry Details Article
PubMed
TargetJAK3/JAK1(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50193995(CP-690550 | 3-((3R,4R)-4-methyl-3-(methyl(7H-pyrro...)
Affinity DataIC50: 56nMAssay 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
In Depth
Date in BDB:
2/12/2015
Entry Details Article
PubMed
LigandPNGBDBM50021656(LY-3009104 | INCB-028050 | BARICITINIB | US1011290...)
Affinity DataIC50: 61nMAssay Description:Inhibition of TYK2 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/12/2015
Entry Details Article
PubMed
TargetTyrosine-protein kinase JAK3(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50021655(VRT-831509 | VX-509 | DECERNOTINIB | US10112907, E...)
Affinity DataIC50: 74nMAssay Description:Inhibition of JAK3 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/12/2015
Entry Details Article
PubMed
LigandPNGBDBM50193995(CP-690550 | 3-((3R,4R)-4-methyl-3-(methyl(7H-pyrro...)
Affinity DataIC50: 75nMAssay 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
In Depth
Date in BDB:
2/12/2015
Entry Details Article
PubMed
TargetTyrosine-protein kinase JAK2(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50193995(CP-690550 | 3-((3R,4R)-4-methyl-3-(methyl(7H-pyrro...)
Affinity DataIC50: 77nMAssay Description:Inhibition of JAK2 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/12/2015
Entry Details Article
PubMed
LigandPNGBDBM50021656(LY-3009104 | INCB-028050 | BARICITINIB | US1011290...)
Affinity DataIC50: 82nMAssay 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
In Depth
Date in BDB:
2/12/2015
Entry Details Article
PubMed
TargetTyrosine-protein kinase JAK2(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50021656(LY-3009104 | INCB-028050 | BARICITINIB | US1011290...)
Affinity DataIC50: 88nMAssay 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
In Depth
Date in BDB:
2/12/2015
Entry Details Article
PubMed
LigandPNGBDBM50021656(LY-3009104 | INCB-028050 | BARICITINIB | US1011290...)
Affinity DataIC50: 149nMAssay 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
In Depth
Date in BDB:
2/12/2015
Entry Details Article
PubMed
LigandPNGBDBM50355501(RUXOLITINIB PHOSPHATE | INCB-018424 | RUXOLITINIB ...)
Affinity DataIC50: 194nMAssay 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
In Depth
Date in BDB:
2/12/2015
Entry Details Article
PubMed
LigandPNGBDBM50193995(CP-690550 | 3-((3R,4R)-4-methyl-3-(methyl(7H-pyrro...)
Affinity DataIC50: 229nMAssay 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
In Depth
Date in BDB:
2/12/2015
Entry Details Article
PubMed
TargetJAK3/JAK1(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50021656(LY-3009104 | INCB-028050 | BARICITINIB | US1011290...)
Affinity DataIC50: 259nMAssay 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
In Depth
Date in BDB:
2/12/2015
Entry Details Article
PubMed
LigandPNGBDBM50355501(RUXOLITINIB PHOSPHATE | INCB-018424 | RUXOLITINIB ...)
Affinity DataIC50: 298nMAssay 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
In Depth
Date in BDB:
2/12/2015
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetTyrosine-protein kinase JAK2(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50193995(CP-690550 | 3-((3R,4R)-4-methyl-3-(methyl(7H-pyrro...)
Affinity DataIC50: 302nMAssay 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
In Depth
Date in BDB:
2/12/2015
Entry Details Article
PubMed
TargetTyrosine-protein kinase JAK1(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50021657(CHEMBL3297839)
Affinity DataIC50: 363nMAssay Description:Inhibition of JAK1 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/12/2015
Entry Details Article
PubMed
LigandPNGBDBM50193995(CP-690550 | 3-((3R,4R)-4-methyl-3-(methyl(7H-pyrro...)
Affinity DataIC50: 409nMAssay 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
In Depth
Date in BDB:
2/12/2015
Entry Details Article
PubMed
TargetTyrosine-protein kinase JAK3(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50355501(RUXOLITINIB PHOSPHATE | INCB-018424 | RUXOLITINIB ...)
Affinity DataIC50: 487nMAssay Description:Inhibition of JAK3 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/12/2015
Entry Details Article
PubMed
LigandPNGBDBM50193995(CP-690550 | 3-((3R,4R)-4-methyl-3-(methyl(7H-pyrro...)
Affinity DataIC50: 489nMAssay Description:Inhibition of TYK2 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/12/2015
Entry Details Article
PubMed
TargetTyrosine-protein kinase JAK2(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50021655(VRT-831509 | VX-509 | DECERNOTINIB | US10112907, E...)
Affinity DataIC50: 619nMAssay Description:Inhibition of JAK2 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/12/2015
Entry Details Article
PubMed
TargetTyrosine-protein kinase JAK2(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50355501(RUXOLITINIB PHOSPHATE | INCB-018424 | RUXOLITINIB ...)
Affinity DataIC50: 677nMAssay 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
In Depth
Date in BDB:
2/12/2015
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetTyrosine-protein kinase JAK3(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50021656(LY-3009104 | INCB-028050 | BARICITINIB | US1011290...)
Affinity DataIC50: 787nMAssay Description:Inhibition of JAK3 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/12/2015
Entry Details Article
PubMed
LigandPNGBDBM50355501(RUXOLITINIB PHOSPHATE | INCB-018424 | RUXOLITINIB ...)
Affinity DataIC50: 818nMAssay 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
In Depth
Date in BDB:
2/12/2015
Entry Details Article
PubMedPDB3D3D Structure (crystal)
LigandPNGBDBM50021657(CHEMBL3297839)
Affinity DataIC50: 918nMAssay 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
In Depth
Date in BDB:
2/12/2015
Entry Details Article
PubMed
TargetJAK3/JAK1(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50021655(VRT-831509 | VX-509 | DECERNOTINIB | US10112907, E...)
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
In Depth
Date in BDB:
2/12/2015
Entry Details Article
PubMed
LigandPNGBDBM50355501(RUXOLITINIB PHOSPHATE | INCB-018424 | RUXOLITINIB ...)
Affinity DataIC50: 1.09E+3nMAssay 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
In Depth
Date in BDB:
2/12/2015
Entry Details Article
PubMedPDB3D3D Structure (crystal)
LigandPNGBDBM50021655(VRT-831509 | VX-509 | DECERNOTINIB | US10112907, E...)
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
In Depth
Date in BDB:
2/12/2015
Entry Details Article
PubMed
TargetTyrosine-protein kinase JAK2(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50193995(CP-690550 | 3-((3R,4R)-4-methyl-3-(methyl(7H-pyrro...)
Affinity DataIC50: 1.38E+3nMAssay Description:Inhibition of JAK2 homodimer in human monocytes assessed as inhibition of GM-CSF-induced STAT-5 phosphorylation preincubated for 60 mins followed by ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/12/2015
Entry Details Article
PubMed
LigandPNGBDBM50021657(CHEMBL3297839)
Affinity DataIC50: 1.50E+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
In Depth
Date in BDB:
2/12/2015
Entry Details Article
PubMed
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