BDBM305821 (1r,3r)-3-(Cyanomethyl)-3-(4-(6-(1-methyl-1H-pyrazol-4-yl)pyrazolo[1,5-a]pyrazin-4-yl)-1H-pyrazol-1-yl)cyclobutane-1-carbonitrile::US10144738, Example 20::US10822341, Example 20::US11472809, Example 20

SMILES Cn1cc(cn1)-c1cn2nccc2c(n1)-c1cnn(c1)[C@@]1(CC#N)C[C@@H](C1)C#N

InChI Key InChIKey=XPLZTJWZDBFWDE-OYOVHJISSA-N

Data  36 IC50

PDB links: 1 PDB ID matches this monomer.

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Similarity at least:  must be >=0.5
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Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 7 hits for monomerid = 305821   

TargetTyrosine-protein kinase JAK2(Homo sapiens (Human))
Pfizer

US Patent
LigandPNGBDBM305821((1r,3r)-3-(Cyanomethyl)-3-(4-(6-(1-methyl-1H-pyraz...)
Affinity DataIC50:  74nMAssay 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 JAK2(Homo sapiens (Human))
Pfizer

US Patent
LigandPNGBDBM305821((1r,3r)-3-(Cyanomethyl)-3-(4-(6-(1-methyl-1H-pyraz...)
Affinity DataIC50:  74nMAssay 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 JAK2(Homo sapiens (Human))
Pfizer

US Patent
LigandPNGBDBM305821((1r,3r)-3-(Cyanomethyl)-3-(4-(6-(1-methyl-1H-pyraz...)
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 DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK2(Homo sapiens (Human))
Pfizer

US Patent
LigandPNGBDBM305821((1r,3r)-3-(Cyanomethyl)-3-(4-(6-(1-methyl-1H-pyraz...)
Affinity DataIC50:  74nMAssay 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 JAK2(Homo sapiens (Human))
Pfizer

US Patent
LigandPNGBDBM305821((1r,3r)-3-(Cyanomethyl)-3-(4-(6-(1-methyl-1H-pyraz...)
Affinity DataIC50:  74nMAssay Description:Inhibition of recombinant human GST-tagged JAK2 catalytic domain (809 to 1153+9 residues) expressed in baculovirus expression system using FITC-KGGEE...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK2(Homo sapiens (Human))
Pfizer

US Patent
LigandPNGBDBM305821((1r,3r)-3-(Cyanomethyl)-3-(4-(6-(1-methyl-1H-pyraz...)
Affinity DataIC50:  148nMAssay Description:Inhibition of JAK2 homodimer signaling pathway in human whole blood spiked with CD34 +ve cells assessed as reduction in EPO induced STAT5 phosphoryla...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK2(Homo sapiens (Human))
Pfizer

US Patent
LigandPNGBDBM305821((1r,3r)-3-(Cyanomethyl)-3-(4-(6-(1-methyl-1H-pyraz...)
Affinity DataIC50:  74nMAssay 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