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-MJBXVCDLSA-N

Data  50 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 50 hits for monomerid = 329924   

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

US Patent
LigandPNGBDBM329924(US10463675, Example 7 | US10980815, Ex. No. 7 | US...)
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
TargetTyrosine-protein kinase JAK3(Homo sapiens (Human))
Pfizer

US Patent
LigandPNGBDBM329924(US10463675, Example 7 | US10980815, Ex. No. 7 | US...)
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 JAK2(Homo sapiens (Human))
Pfizer

US Patent
LigandPNGBDBM329924(US10463675, Example 7 | US10980815, Ex. No. 7 | US...)
Affinity DataIC50:  77nMMore data for this Ligand-Target Pair
In DepthDetails US Patent
TargetTyrosine-protein kinase JAK3(Homo sapiens (Human))
Pfizer

US Patent
LigandPNGBDBM329924(US10463675, Example 7 | US10980815, Ex. No. 7 | US...)
Affinity DataIC50:  6.49E+3nMMore data for this Ligand-Target Pair
In DepthDetails US Patent
TargetNon-receptor tyrosine-protein kinase TYK2(Homo sapiens (Human))
Pfizer

US Patent
LigandPNGBDBM329924(US10463675, Example 7 | US10980815, Ex. No. 7 | US...)
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
TargetTyrosine-protein kinase JAK1(Homo sapiens (Human))
Pfizer

US Patent
LigandPNGBDBM329924(US10463675, Example 7 | US10980815, Ex. No. 7 | US...)
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
TargetTyrosine-protein kinase JAK2(Homo sapiens (Human))
Pfizer

US Patent
LigandPNGBDBM329924(US10463675, Example 7 | US10980815, Ex. No. 7 | US...)
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(Homo sapiens (Human))
Pfizer

US Patent
LigandPNGBDBM329924(US10463675, Example 7 | US10980815, Ex. No. 7 | US...)
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(US10463675, Example 7 | US10980815, Ex. No. 7 | US...)
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
TargetTyrosine-protein kinase JAK3(Homo sapiens (Human))
Pfizer

US Patent
LigandPNGBDBM329924(US10463675, Example 7 | US10980815, Ex. No. 7 | US...)
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 ArticlePubMed
LigandPNGBDBM329924(US10463675, Example 7 | US10980815, Ex. No. 7 | US...)
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
TargetTyrosine-protein kinase JAK1/JAK2(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM329924(US10463675, Example 7 | US10980815, Ex. No. 7 | US...)
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
TargetVascular endothelial growth factor receptor 2(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM329924(US10463675, Example 7 | US10980815, Ex. No. 7 | US...)
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 ArticlePubMed
LigandPNGBDBM329924(US10463675, Example 7 | US10980815, Ex. No. 7 | US...)
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
TargetJAK3/JAK1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM329924(US10463675, Example 7 | US10980815, Ex. No. 7 | US...)
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
LigandPNGBDBM329924(US10463675, Example 7 | US10980815, Ex. No. 7 | US...)
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
TargetTyrosine-protein kinase JAK1/JAK2(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM329924(US10463675, Example 7 | US10980815, Ex. No. 7 | US...)
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
TargetNon-receptor tyrosine-protein kinase TYK2(Homo sapiens (Human))
Pfizer

US Patent
LigandPNGBDBM329924(US10463675, Example 7 | US10980815, Ex. No. 7 | US...)
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
TargetTyrosine-protein kinase JAK1(Homo sapiens (Human))
Pfizer

US Patent
LigandPNGBDBM329924(US10463675, Example 7 | US10980815, Ex. No. 7 | US...)
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
TargetTyrosine-protein kinase JAK1/JAK2(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM329924(US10463675, Example 7 | US10980815, Ex. No. 7 | US...)
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
TargetTyrosine-protein kinase JAK1/JAK2(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM329924(US10463675, Example 7 | US10980815, Ex. No. 7 | US...)
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
TargetJAK3/JAK1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM329924(US10463675, Example 7 | US10980815, Ex. No. 7 | US...)
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
TargetTyrosine-protein kinase JAK1/JAK2(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM329924(US10463675, Example 7 | US10980815, Ex. No. 7 | US...)
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
TargetTyrosine-protein kinase JAK2(Homo sapiens (Human))
Pfizer

US Patent
LigandPNGBDBM329924(US10463675, Example 7 | US10980815, Ex. No. 7 | US...)
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 ArticlePubMed
TargetNon-receptor tyrosine-protein kinase TYK2(Homo sapiens (Human))
Pfizer

US Patent
LigandPNGBDBM329924(US10463675, Example 7 | US10980815, Ex. No. 7 | US...)
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
TargetTyrosine-protein kinase JAK2(Homo sapiens (Human))
Pfizer

US Patent
LigandPNGBDBM329924(US10463675, Example 7 | US10980815, Ex. No. 7 | US...)
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 ArticlePubMed
TargetTyrosine-protein kinase JAK3(Homo sapiens (Human))
Pfizer

US Patent
LigandPNGBDBM329924(US10463675, Example 7 | US10980815, Ex. No. 7 | US...)
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 ArticlePubMed
LigandPNGBDBM329924(US10463675, Example 7 | US10980815, Ex. No. 7 | US...)
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
TargetTyrosine-protein kinase JAK1/JAK2(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM329924(US10463675, Example 7 | US10980815, Ex. No. 7 | US...)
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
TargetTyrosine-protein kinase JAK2(Homo sapiens (Human))
Pfizer

US Patent
LigandPNGBDBM329924(US10463675, Example 7 | US10980815, Ex. No. 7 | US...)
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 ArticlePubMed
TargetVascular endothelial growth factor receptor 2(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM329924(US10463675, Example 7 | US10980815, Ex. No. 7 | US...)
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 ArticlePubMed
TargetVascular endothelial growth factor receptor 2(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM329924(US10463675, Example 7 | US10980815, Ex. No. 7 | US...)
Affinity DataIC50: >3.00E+4nMAssay Description:Inhibition of VEGFR2 (unknown origin) by cell based assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM329924(US10463675, Example 7 | US10980815, Ex. No. 7 | US...)
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
TargetJAK3/JAK1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM329924(US10463675, Example 7 | US10980815, Ex. No. 7 | US...)
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
LigandPNGBDBM329924(US10463675, Example 7 | US10980815, Ex. No. 7 | US...)
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
TargetVascular endothelial growth factor receptor 2(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM329924(US10463675, Example 7 | US10980815, Ex. No. 7 | US...)
Affinity DataIC50: >3.00E+4nMAssay Description:Inhibition of VEGFR2 (unknown origin) by cell based assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK1/JAK2(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM329924(US10463675, Example 7 | US10980815, Ex. No. 7 | US...)
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
TargetTyrosine-protein kinase JAK1/JAK2(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM329924(US10463675, Example 7 | US10980815, Ex. No. 7 | US...)
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
TargetJAK3/JAK1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM329924(US10463675, Example 7 | US10980815, Ex. No. 7 | US...)
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
TargetTyrosine-protein kinase JAK2(Homo sapiens (Human))
Pfizer

US Patent
LigandPNGBDBM329924(US10463675, Example 7 | US10980815, Ex. No. 7 | US...)
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 ArticlePubMed
LigandPNGBDBM329924(US10463675, Example 7 | US10980815, Ex. No. 7 | US...)
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
TargetTyrosine-protein kinase JAK1(Homo sapiens (Human))
Pfizer

US Patent
LigandPNGBDBM329924(US10463675, Example 7 | US10980815, Ex. No. 7 | US...)
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
TargetNon-receptor tyrosine-protein kinase TYK2(Homo sapiens (Human))
Pfizer

US Patent
LigandPNGBDBM329924(US10463675, Example 7 | US10980815, Ex. No. 7 | US...)
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
TargetTyrosine-protein kinase JAK1(Homo sapiens (Human))
Pfizer

US Patent
LigandPNGBDBM329924(US10463675, Example 7 | US10980815, Ex. No. 7 | US...)
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
TargetTyrosine-protein kinase JAK2(Homo sapiens (Human))
Pfizer

US Patent
LigandPNGBDBM329924(US10463675, Example 7 | US10980815, Ex. No. 7 | US...)
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(Homo sapiens (Human))
Pfizer

US Patent
LigandPNGBDBM329924(US10463675, Example 7 | US10980815, Ex. No. 7 | US...)
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(Homo sapiens (Human))
Pfizer

US Patent
LigandPNGBDBM329924(US10463675, Example 7 | US10980815, Ex. No. 7 | US...)
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
TargetTyrosine-protein kinase JAK1(Homo sapiens (Human))
Pfizer

US Patent
LigandPNGBDBM329924(US10463675, Example 7 | US10980815, Ex. No. 7 | US...)
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
TargetTyrosine-protein kinase JAK2(Homo sapiens (Human))
Pfizer

US Patent
LigandPNGBDBM329924(US10463675, Example 7 | US10980815, Ex. No. 7 | US...)
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 JAK1(Homo sapiens (Human))
Pfizer

US Patent
LigandPNGBDBM329924(US10463675, Example 7 | US10980815, Ex. No. 7 | US...)
Affinity DataIC50:  17nMMore data for this Ligand-Target Pair