BDBM305816 2-((1r,3s)-3-Methoxy-1-(4-(6-(1-methyl-1H-pyrazol-4-yl)pyrazolo[1,5-a]pyrazin-4-yl)-1H-pyrazol-1-yl)cyclobutyl)acetonitrile (trans isomer)::US10144738, Example 15::US10822341, Example 15::US11472809, Example 15

SMILES CO[C@H]1C[C@@](CC#N)(C1)n1cc(cn1)-c1nc(cn2nccc12)-c1cnn(C)c1

InChI Key InChIKey=VYWKECFAYKXBQW-UHFFFAOYSA-N

Data  21 IC50

  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 21 hits for monomerid = 305816   

TargetTyrosine-protein kinase JAK2(Human)
Pfizer

US Patent
LigandPNGBDBM305816(US10144738, Example 15 | 2-((1r,3s)-3-Methoxy-1-(4...)
Affinity DataIC50: 228nMAssay 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 Depth
Date in BDB:
6/21/2021
Entry Details
Go to US Patent

TargetTyrosine-protein kinase JAK3(Human)
Pfizer

US Patent
LigandPNGBDBM305816(US10144738, Example 15 | 2-((1r,3s)-3-Methoxy-1-(4...)
Affinity DataIC50: 9.12E+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 Depth
Date in BDB:
12/24/2022
Entry Details
Go to US Patent

TargetTyrosine-protein kinase JAK2(Human)
Pfizer

US Patent
LigandPNGBDBM305816(US10144738, Example 15 | 2-((1r,3s)-3-Methoxy-1-(4...)
Affinity DataIC50: 228nMAssay 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 Depth
Date in BDB:
12/24/2022
Entry Details
Go to US Patent

TargetTyrosine-protein kinase JAK1(Human)
Pfizer

US Patent
LigandPNGBDBM305816(US10144738, Example 15 | 2-((1r,3s)-3-Methoxy-1-(4...)
Affinity DataIC50: 1.50E+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 Depth
Date in BDB:
12/24/2022
Entry Details
Go to US Patent

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

US Patent
LigandPNGBDBM305816(US10144738, Example 15 | 2-((1r,3s)-3-Methoxy-1-(4...)
Affinity DataIC50: 22nMAssay 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 Depth
Date in BDB:
12/24/2022
Entry Details
Go to US Patent

TargetTyrosine-protein kinase JAK2(Human)
Pfizer

US Patent
LigandPNGBDBM305816(US10144738, Example 15 | 2-((1r,3s)-3-Methoxy-1-(4...)
Affinity DataIC50: 1.10E+3nMAssay 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 Depth
Date in BDB:
3/22/2022
Entry Details Article
PubMed
TargetTyrosine-protein kinase JAK3(Human)
Pfizer

US Patent
LigandPNGBDBM305816(US10144738, Example 15 | 2-((1r,3s)-3-Methoxy-1-(4...)
Affinity DataIC50: 9.12E+3nMAssay Description:Inhibition of recombinant human GST-tagged JAK3 catalytic domain (781 to 1124 residues) expressed in baculovirus expression system using FITC-KGGEEEE...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/22/2022
Entry Details Article
PubMed
TargetTyrosine-protein kinase JAK2(Human)
Pfizer

US Patent
LigandPNGBDBM305816(US10144738, Example 15 | 2-((1r,3s)-3-Methoxy-1-(4...)
Affinity DataIC50: 228nMAssay 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 Depth
Date in BDB:
3/22/2022
Entry Details Article
PubMed
TargetTyrosine-protein kinase JAK1(Human)
Pfizer

US Patent
LigandPNGBDBM305816(US10144738, Example 15 | 2-((1r,3s)-3-Methoxy-1-(4...)
Affinity DataIC50: 1.50E+3nMAssay Description:Inhibition of recombinant human GST-tagged JAK1 catalytic domain (866 to 1154 residues) expressed in baculovirus expression system using 5FAM-KKSRGDY...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/22/2022
Entry Details Article
PubMed
TargetNon-receptor tyrosine-protein kinase TYK2(Human)
Pfizer

US Patent
LigandPNGBDBM305816(US10144738, Example 15 | 2-((1r,3s)-3-Methoxy-1-(4...)
Affinity DataIC50: 22nMAssay Description:Inhibition of recombinant human His-tagged TYK2 expressed in baculovirus infected Sf21 cells using 5FAM-KKSRGDYMTMQID as substrate in presence of ATP...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/22/2022
Entry Details Article
PubMed
TargetTyrosine-protein kinase JAK3(Human)
Pfizer

US Patent
LigandPNGBDBM305816(US10144738, Example 15 | 2-((1r,3s)-3-Methoxy-1-(4...)
Affinity DataIC50: 9.12E+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 Depth
Date in BDB:
6/21/2021
Entry Details
Go to US Patent

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

US Patent
LigandPNGBDBM305816(US10144738, Example 15 | 2-((1r,3s)-3-Methoxy-1-(4...)
Affinity DataIC50: 22nMAssay 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 Depth
Date in BDB:
3/30/2019
Entry Details
Go to US Patent

TargetTyrosine-protein kinase JAK1(Human)
Pfizer

US Patent
LigandPNGBDBM305816(US10144738, Example 15 | 2-((1r,3s)-3-Methoxy-1-(4...)
Affinity DataIC50: 1.50E+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 Depth
Date in BDB:
6/21/2021
Entry Details
Go to US Patent

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

US Patent
LigandPNGBDBM305816(US10144738, Example 15 | 2-((1r,3s)-3-Methoxy-1-(4...)
Affinity DataIC50: 22nMAssay 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 Depth
Date in BDB:
6/21/2021
Entry Details
Go to US Patent

TargetTyrosine-protein kinase JAK3(Human)
Pfizer

US Patent
LigandPNGBDBM305816(US10144738, Example 15 | 2-((1r,3s)-3-Methoxy-1-(4...)
Affinity DataIC50: 9.12E+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 Depth
Date in BDB:
3/30/2019
Entry Details
Go to US Patent

TargetTyrosine-protein kinase JAK2(Human)
Pfizer

US Patent
LigandPNGBDBM305816(US10144738, Example 15 | 2-((1r,3s)-3-Methoxy-1-(4...)
Affinity DataIC50: 228nMAssay 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 Depth
Date in BDB:
3/30/2019
Entry Details
Go to US Patent

TargetTyrosine-protein kinase JAK1(Human)
Pfizer

US Patent
LigandPNGBDBM305816(US10144738, Example 15 | 2-((1r,3s)-3-Methoxy-1-(4...)
Affinity DataIC50: 1.50E+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 Depth
Date in BDB:
3/30/2019
Entry Details
Go to US Patent

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

US Patent
LigandPNGBDBM305816(US10144738, Example 15 | 2-((1r,3s)-3-Methoxy-1-(4...)
Affinity DataIC50: 22nMAssay 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 Depth
Date in BDB:
3/30/2019
Entry Details
Go to US Patent

TargetTyrosine-protein kinase JAK3(Human)
Pfizer

US Patent
LigandPNGBDBM305816(US10144738, Example 15 | 2-((1r,3s)-3-Methoxy-1-(4...)
Affinity DataIC50: 9.12E+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 Depth
Date in BDB:
3/30/2019
Entry Details
Go to US Patent

TargetTyrosine-protein kinase JAK2(Human)
Pfizer

US Patent
LigandPNGBDBM305816(US10144738, Example 15 | 2-((1r,3s)-3-Methoxy-1-(4...)
Affinity DataIC50: 228nMAssay 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 Depth
Date in BDB:
3/30/2019
Entry Details
Go to US Patent

TargetTyrosine-protein kinase JAK1(Human)
Pfizer

US Patent
LigandPNGBDBM305816(US10144738, Example 15 | 2-((1r,3s)-3-Methoxy-1-(4...)
Affinity DataIC50: 1.50E+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 Depth
Date in BDB:
3/30/2019
Entry Details
Go to US Patent