BDBM329924 US10463675, Example 7::US10980815, Ex. No. 7::US11197867, Example 7::US9663526, Example 7

SMILES Cn1cc(Nc2nccc(n2)N2C[C@@H]3CC[C@H](C2)N3C(=O)[C@@H]2CC2(F)F)cn1

InChI Key InChIKey=BUWBRTXGQRBBHG-UHFFFAOYSA-N

Data  54 IC50

PDB links: 2 PDB IDs match this monomer.

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
Find this compound or compounds like it in BindingDB:
   Substructure
Similarity at least:  must be >=0.5
Exact match

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 54 hits for monomerid = 329924   

TargetTyrosine-protein kinase JAK1(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM329924(US9663526, Example 7 | US10463675, Example 7 | US1...)
Affinity DataIC50: 17nMAssay Description:Inhibition of human JAK1 using fluorescence labeled peptide as substrate and using 1 mM ATP by microfluidic based mobility shift assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
TargetTyrosine-protein kinase JAK1/JAK2(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM329924(US9663526, Example 7 | US10463675, Example 7 | US1...)
Affinity DataIC50: 298nMAssay Description:Inhibition of JAK1/JAK2 signaling pathway in human CD14 +ve cells of whole blood assessed as reduction in IFN-gamma induced STAT1 phosphorylation pre...More data for this Ligand-Target Pair
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
TargetTyrosine-protein kinase JAK2(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM329924(US9663526, Example 7 | US10463675, Example 7 | US1...)
Affinity DataIC50: 577nMAssay Description:Inhibition of JAK2 homodimer signaling pathway in human spiked CD34 +ve cells of whole blood assessed as reduction in EPO induced STAT5 phosphorylati...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
LigandPNGBDBM329924(US9663526, Example 7 | US10463675, Example 7 | US1...)
Affinity DataIC50: 1.60E+3nMAssay Description:Inhibition of recombinant human VEGFR2 using Ulight-CAGAGAIETDKEYYTVKD as substrate after 60 minsMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
LigandPNGBDBM329924(US9663526, Example 7 | US10463675, Example 7 | US1...)
Affinity DataIC50: 3.00E+4nMAssay Description:Inhibition of VEGFR2 (unknown origin) by cell based assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
LigandPNGBDBM329924(US9663526, Example 7 | US10463675, Example 7 | US1...)
Affinity DataIC50: 305nMAssay Description:Inhibition of JAK1/TYK2 signaling pathway in human lymphocytes of whole blood assessed as reduction in IL-10 induced STAT3 phosphorylation preincubat...More data for this Ligand-Target Pair
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
TargetJAK3/JAK1(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM329924(US9663526, Example 7 | US10463675, Example 7 | US1...)
Affinity DataIC50: 204nMAssay Description:Inhibition of JAK1/JAK3 signaling pathway in human lymphocytes of whole blood assessed as reduction in IL-21 induced STAT3 phosphorylation preincubat...More data for this Ligand-Target Pair
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
LigandPNGBDBM329924(US9663526, Example 7 | US10463675, Example 7 | US1...)
Affinity DataIC50: 120nMAssay Description:Inhibition of JAK2/TYK2 signaling pathway in human lymphocytes of whole blood assessed as reduction in IL-23 induced STAT3 phosphorylation preincubat...More data for this Ligand-Target Pair
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
LigandPNGBDBM329924(US9663526, Example 7 | US10463675, Example 7 | US1...)
Affinity DataIC50: 3.00E+4nMAssay Description:Inhibition of VEGFR2 (unknown origin) by cell based assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetTyrosine-protein kinase JAK1/JAK2(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM329924(US9663526, Example 7 | US10463675, Example 7 | US1...)
Affinity DataIC50: 81nMAssay Description:Inhibition of JAK1/JAK2 signaling pathway in human CD3 +ve cells of whole blood assessed as reduction in IL-6 induced STAT1 phosphorylation preincuba...More data for this Ligand-Target Pair
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
TargetTyrosine-protein kinase JAK1/JAK2(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM329924(US9663526, Example 7 | US10463675, Example 7 | US1...)
Affinity DataIC50: 641nMAssay Description:Inhibition of JAK1/JAK2 signaling pathway in human CD3 +ve cells of whole blood assessed as reduction in IL-6 induced STAT3 phosphorylation preincuba...More data for this Ligand-Target Pair
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
TargetJAK3/JAK1(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM329924(US9663526, Example 7 | US10463675, Example 7 | US1...)
Affinity DataIC50: 204nMAssay Description:Inhibition of JAK1/JAK3 signaling pathway in human lymphocytes of whole blood assessed as reduction in IL-21 induced STAT3 phosphorylation preincubat...More data for this Ligand-Target Pair
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
TargetTyrosine-protein kinase JAK2(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM329924(US9663526, Example 7 | US10463675, Example 7 | US1...)
Affinity DataIC50: 77nMAssay Description:Inhibition of human JAK2 using fluorescence labeled peptide as substrate and using 1 mM ATP by microfluidic based mobility shift assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
LigandPNGBDBM329924(US9663526, Example 7 | US10463675, Example 7 | US1...)
Affinity DataIC50: 30nMAssay Description:Inhibition of JAK1/TYK2 signaling pathway in human lymphocytes of whole blood assessed as reduction in IFN-alpha induced STAT3 phosphorylation preinc...More data for this Ligand-Target Pair
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
LigandPNGBDBM329924(US9663526, Example 7 | US10463675, Example 7 | US1...)
Affinity DataIC50: 30nMAssay Description:Inhibition of JAK1/TYK2 signaling pathway in human lymphocytes of whole blood assessed as reduction in IFN-alpha induced STAT3 phosphorylation preinc...More data for this Ligand-Target Pair
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
TargetNon-receptor tyrosine-protein kinase TYK2(Human)
Pfizer

US Patent
LigandPNGBDBM329924(US9663526, Example 7 | US10463675, Example 7 | US1...)
Affinity DataIC50: 23nMAssay Description:Compounds were added to a 384-well plate. Reaction mixtures contained 10 mM HEPES, pH 7.4, 10 mM MgCl2, 0.01% BSA, 0.0005% Tween 20, 1 mM ATP and 1 &...More data for this Ligand-Target Pair
In DepthDetails
US Patent
PDB3D3D Structure (crystal)
TargetTyrosine-protein kinase JAK1(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM329924(US9663526, Example 7 | US10463675, Example 7 | US1...)
Affinity DataIC50: 17nMAssay Description:Compounds were added to a 384-well plate. Reaction mixtures contained 10 mM HEPES, pH 7.4, 10 mM MgCl2, 0.01% BSA, 0.0005% Tween 20, 1 mM ATP and 1 &...More data for this Ligand-Target Pair
In DepthDetails
US Patent
PDB3D3D Structure (crystal)
TargetTyrosine-protein kinase JAK2(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM329924(US9663526, Example 7 | US10463675, Example 7 | US1...)
Affinity DataIC50: 77nMAssay Description:Compounds were added to a 384-well plate. Reaction mixtures contained 10 mM HEPES, pH 7.4, 10 mM MgCl2, 0.01% BSA, 0.0005% Tween 20, 1 mM ATP and 1 &...More data for this Ligand-Target Pair
In DepthDetails
US Patent

TargetTyrosine-protein kinase JAK3(Human)
Pfizer

US Patent
LigandPNGBDBM329924(US9663526, Example 7 | US10463675, Example 7 | US1...)
Affinity DataIC50: 6.49E+3nMAssay Description:Compounds were added to a 384-well plate. Reaction mixtures contained 10 mM HEPES, pH 7.4, 10 mM MgCl2, 0.01% BSA, 0.0005% Tween 20, 1 mM ATP and 1 &...More data for this Ligand-Target Pair
In DepthDetails
US Patent

TargetNon-receptor tyrosine-protein kinase TYK2(Human)
Pfizer

US Patent
LigandPNGBDBM329924(US9663526, Example 7 | US10463675, Example 7 | US1...)
Affinity DataIC50: 23nMAssay Description:Compounds were added to a 384-well plate. Reaction mixtures contained 10 mM HEPES, pH 7.4, 10 mM MgCl2, 0.01% BSA, 0.0005% Tween 20, 1 mM ATP and 1 M...More data for this Ligand-Target Pair
In DepthDetails
US Patent
PDB3D3D Structure (crystal)
TargetTyrosine-protein kinase JAK1(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM329924(US9663526, Example 7 | US10463675, Example 7 | US1...)
Affinity DataIC50: 17nMAssay Description:Compounds were added to a 384-well plate. Reaction mixtures contained 10 mM HEPES, pH 7.4, 10 mM MgCl2, 0.01% BSA, 0.0005% Tween 20, 1 mM ATP and 1 M...More data for this Ligand-Target Pair
In DepthDetails
US Patent
PDB3D3D Structure (crystal)
TargetTyrosine-protein kinase JAK2(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM329924(US9663526, Example 7 | US10463675, Example 7 | US1...)
Affinity DataIC50: 77nMAssay Description:Compounds were added to a 384-well plate. Reaction mixtures contained 10 mM HEPES, pH 7.4, 10 mM MgCl2, 0.01% BSA, 0.0005% Tween 20, 1 mM ATP and 1 M...More data for this Ligand-Target Pair
In DepthDetails
US Patent

TargetTyrosine-protein kinase JAK3(Human)
Pfizer

US Patent
LigandPNGBDBM329924(US9663526, Example 7 | US10463675, Example 7 | US1...)
Affinity DataIC50: 6.49E+3nMAssay Description:Compounds were added to a 384-well plate. Reaction mixtures contained 10 mM HEPES, pH 7.4, 10 mM MgCl2, 0.01% BSA, 0.0005% Tween 20, 1 mM ATP and 1 M...More data for this Ligand-Target Pair
In DepthDetails
US Patent

TargetTyrosine-protein kinase JAK1(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM329924(US9663526, Example 7 | US10463675, Example 7 | US1...)
Affinity DataIC50: 17nMAssay Description:Inhibition of JAK1 JH1 domain (unknown origin) in presence of 1 mM of ATPMore data for this Ligand-Target Pair
In DepthDetails
PubMedPDB3D3D Structure (crystal)
TargetTyrosine-protein kinase JAK2(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM329924(US9663526, Example 7 | US10463675, Example 7 | US1...)
Affinity DataIC50: 77nMAssay Description:Inhibition of JAK2 JH1 domain (unknown origin) in presence of 1 mM of ATPMore data for this Ligand-Target Pair
In DepthDetails
PubMed
TargetTyrosine-protein kinase JAK3(Human)
Pfizer

US Patent
LigandPNGBDBM329924(US9663526, Example 7 | US10463675, Example 7 | US1...)
Affinity DataIC50: 6.49E+3nMAssay Description:Inhibition of JAK3 JH1 domain (unknown origin) in presence of 1 mM of ATPMore data for this Ligand-Target Pair
In DepthDetails
PubMed
TargetNon-receptor tyrosine-protein kinase TYK2(Human)
Pfizer

US Patent
LigandPNGBDBM329924(US9663526, Example 7 | US10463675, Example 7 | US1...)
Affinity DataIC50: 23nMAssay Description:Inhibition of TYK2 JH1 domain (unknown origin) in presence of 1 mM of ATPMore data for this Ligand-Target Pair
In DepthDetails
PubMedPDB3D3D Structure (crystal)
TargetJAK3/JAK1(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM329924(US9663526, Example 7 | US10463675, Example 7 | US1...)
Affinity DataIC50: 238nMAssay Description:Inhibition of JAK1/JAK3 signaling pathway in human lymphocytes of whole blood assessed as reduction in IL-15 induced STAT5 phosphorylation preincubat...More data for this Ligand-Target Pair
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
TargetTyrosine-protein kinase JAK1(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM329924(US9663526, Example 7 | US10463675, Example 7 | US1...)
Affinity DataIC50: 17nMMore data for this Ligand-Target Pair
In DepthDetails
US Patent
PDB3D3D Structure (crystal)
TargetTyrosine-protein kinase JAK2(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM329924(US9663526, Example 7 | US10463675, Example 7 | US1...)
Affinity DataIC50: 77nMMore data for this Ligand-Target Pair
In DepthDetails
US Patent

TargetTyrosine-protein kinase JAK3(Human)
Pfizer

US Patent
LigandPNGBDBM329924(US9663526, Example 7 | US10463675, Example 7 | US1...)
Affinity DataIC50: 6.49E+3nMMore data for this Ligand-Target Pair
In DepthDetails
US Patent

TargetNon-receptor tyrosine-protein kinase TYK2(Human)
Pfizer

US Patent
LigandPNGBDBM329924(US9663526, Example 7 | US10463675, Example 7 | US1...)
Affinity DataIC50: 23nMAssay Description:Compounds were added to a 384-well plate. Reaction mixtures contained 10 mM HEPES, pH 7.4, 10 mM MgCl2, 0.01% BSA, 0.0005% Tween 20, 1 mM ATP and 1 &...More data for this Ligand-Target Pair
In DepthDetails
US Patent
PDB3D3D Structure (crystal)
TargetTyrosine-protein kinase JAK1(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM329924(US9663526, Example 7 | US10463675, Example 7 | US1...)
Affinity DataIC50: 17nMAssay Description:Compounds were added to a 384-well plate. Reaction mixtures contained 10 mM HEPES, pH 7.4, 10 mM MgCl2, 0.01% BSA, 0.0005% Tween 20, 1 mM ATP and 1 &...More data for this Ligand-Target Pair
In DepthDetails
US Patent
PDB3D3D Structure (crystal)
TargetTyrosine-protein kinase JAK2(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM329924(US9663526, Example 7 | US10463675, Example 7 | US1...)
Affinity DataIC50: 77nMAssay Description:Compounds were added to a 384-well plate. Reaction mixtures contained 10 mM HEPES, pH 7.4, 10 mM MgCl2, 0.01% BSA, 0.0005% Tween 20, 1 mM ATP and 1 &...More data for this Ligand-Target Pair
In DepthDetails
US Patent

TargetTyrosine-protein kinase JAK3(Human)
Pfizer

US Patent
LigandPNGBDBM329924(US9663526, Example 7 | US10463675, Example 7 | US1...)
Affinity DataIC50: 6.49E+3nMAssay Description:Compounds were added to a 384-well plate. Reaction mixtures contained 10 mM HEPES, pH 7.4, 10 mM MgCl2, 0.01% BSA, 0.0005% Tween 20, 1 mM ATP and 1 &...More data for this Ligand-Target Pair
In DepthDetails
US Patent

LigandPNGBDBM329924(US9663526, Example 7 | US10463675, Example 7 | US1...)
Affinity DataIC50: 65nMAssay Description:Inhibition of JAK1/TYK2 signaling pathway in human lymphocytes of whole blood assessed as reduction in IL-12 induced STAT4 phosphorylation preincubat...More data for this Ligand-Target Pair
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
TargetTyrosine-protein kinase JAK3(Human)
Pfizer

US Patent
LigandPNGBDBM329924(US9663526, Example 7 | US10463675, Example 7 | US1...)
Affinity DataIC50: 6.49E+3nMAssay Description:Inhibition of human JAK3 using fluorescence labeled peptide as substrate and using 1 mM ATP by microfluidic based mobility shift assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
LigandPNGBDBM329924(US9663526, Example 7 | US10463675, Example 7 | US1...)
Affinity DataIC50: 65nMAssay Description:Inhibition of JAK1/TYK2 signaling pathway in human lymphocytes of whole blood assessed as reduction in IL-12 induced STAT4 phosphorylation preincubat...More data for this Ligand-Target Pair
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
TargetTyrosine-protein kinase JAK1/JAK2(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM329924(US9663526, Example 7 | US10463675, Example 7 | US1...)
Affinity DataIC50: 298nMAssay Description:Inhibition of JAK1/JAK2 signaling pathway in human CD14 +ve cells of whole blood assessed as reduction in IFN-gamma induced STAT1 phosphorylation pre...More data for this Ligand-Target Pair
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
LigandPNGBDBM329924(US9663526, Example 7 | US10463675, Example 7 | US1...)
Affinity DataIC50: 1.60E+3nMAssay Description:Inhibition of recombinant human VEGFR2 using Ulight-CAGAGAIETDKEYYTVKD as substrate after 60 minsMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
LigandPNGBDBM329924(US9663526, Example 7 | US10463675, Example 7 | US1...)
Affinity DataIC50: 305nMAssay Description:Inhibition of JAK1/TYK2 signaling pathway in human lymphocytes of whole blood assessed as reduction in IL-10 induced STAT3 phosphorylation preincubat...More data for this Ligand-Target Pair
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
TargetNon-receptor tyrosine-protein kinase TYK2(Human)
Pfizer

US Patent
LigandPNGBDBM329924(US9663526, Example 7 | US10463675, Example 7 | US1...)
Affinity DataIC50: 23nMAssay Description:Compounds were added to a 384-well plate. Reaction mixtures contained 10 mM HEPES, pH 7.4, 10 mM MgCl2, 0.01% BSA, 0.0005% Tween 20, 1 mM ATP and 1 &...More data for this Ligand-Target Pair
In DepthDetails
US Patent
PDB3D3D Structure (crystal)
LigandPNGBDBM329924(US9663526, Example 7 | US10463675, Example 7 | US1...)
Affinity DataIC50: 120nMAssay Description:Inhibition of JAK2/TYK2 signaling pathway in human lymphocytes of whole blood assessed as reduction in IL-23 induced STAT3 phosphorylation preincubat...More data for this Ligand-Target Pair
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
TargetTyrosine-protein kinase JAK1/JAK2(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM329924(US9663526, Example 7 | US10463675, Example 7 | US1...)
Affinity DataIC50: 86nMAssay Description:Inhibition of JAK1/JAK2 signaling pathway in human lymphocytes of whole blood assessed as reduction in IL-27 induced STAT3 phosphorylation preincubat...More data for this Ligand-Target Pair
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
TargetNon-receptor tyrosine-protein kinase TYK2(Human)
Pfizer

US Patent
LigandPNGBDBM329924(US9663526, Example 7 | US10463675, Example 7 | US1...)
Affinity DataIC50: 23nMAssay Description:Inhibition of human TYK2 using fluorescence labeled peptide as substrate and using 1 mM ATP level by microfluidic based mobility shift assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
TargetTyrosine-protein kinase JAK1(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM329924(US9663526, Example 7 | US10463675, Example 7 | US1...)
Affinity DataIC50: 17nMAssay Description:Inhibition of human JAK1 using fluorescence labeled peptide as substrate and using 1 mM ATP by microfluidic based mobility shift assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
TargetTyrosine-protein kinase JAK1/JAK2(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM329924(US9663526, Example 7 | US10463675, Example 7 | US1...)
Affinity DataIC50: 81nMAssay Description:Inhibition of JAK1/JAK2 signaling pathway in human CD3 +ve cells of whole blood assessed as reduction in IL-6 induced STAT1 phosphorylation preincuba...More data for this Ligand-Target Pair
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
TargetTyrosine-protein kinase JAK1/JAK2(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM329924(US9663526, Example 7 | US10463675, Example 7 | US1...)
Affinity DataIC50: 641nMAssay Description:Inhibition of JAK1/JAK2 signaling pathway in human CD3 +ve cells of whole blood assessed as reduction in IL-6 induced STAT3 phosphorylation preincuba...More data for this Ligand-Target Pair
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
TargetJAK3/JAK1(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM329924(US9663526, Example 7 | US10463675, Example 7 | US1...)
Affinity DataIC50: 238nMAssay Description:Inhibition of JAK1/JAK3 signaling pathway in human lymphocytes of whole blood assessed as reduction in IL-15 induced STAT5 phosphorylation preincubat...More data for this Ligand-Target Pair
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
TargetTyrosine-protein kinase JAK1/JAK2(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM329924(US9663526, Example 7 | US10463675, Example 7 | US1...)
Affinity DataIC50: 86nMAssay Description:Inhibition of JAK1/JAK2 signaling pathway in human lymphocytes of whole blood assessed as reduction in IL-27 induced STAT3 phosphorylation preincubat...More data for this Ligand-Target Pair
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
Displayed 1 to 50 (of 54 total ) | Next | Last >>