BDBM419652 US10463675, Example 95::US10980815, Ex. No. 95::US11197867, Example 95

SMILES C[C@@H]1[C@@H]2CN(C[C@]12NC(=O)[C@@H]1C[C@H]1C#N)c1nc(Nc2cnn(C)c2)ncc1F

InChI Key InChIKey=AJIADPABISZKBM-UHFFFAOYSA-N

Data  18 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 18 hits for monomerid = 419652   

LigandPNGBDBM419652(US10463675, Example 95 | US10980815, Ex. No. 95 | ...)
Affinity DataIC50: 1.94E+3nMAssay Description:Inhibition of JAK1/TYK2 in human whole blood assessed as EPO signalling in CD34+ cells by flow cytometryMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/13/2021
Entry Details Article
PubMed
TargetTyrosine-protein kinase JAK3(Human)
Pfizer

US Patent
LigandPNGBDBM419652(US10463675, Example 95 | US10980815, Ex. No. 95 | ...)
Affinity DataIC50: 255nMAssay 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 Depth
Date in BDB:
4/24/2022
Entry Details
Go to US Patent

TargetTyrosine-protein kinase JAK2(Human)
Pfizer

US Patent
LigandPNGBDBM419652(US10463675, Example 95 | US10980815, Ex. No. 95 | ...)
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 M...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/24/2022
Entry Details
Go to US Patent

TargetTyrosine-protein kinase JAK1(Human)
Pfizer

US Patent
LigandPNGBDBM419652(US10463675, Example 95 | US10980815, Ex. No. 95 | ...)
Affinity DataIC50: 11nMAssay 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 Depth
Date in BDB:
4/24/2022
Entry Details
Go to US Patent

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

US Patent
LigandPNGBDBM419652(US10463675, Example 95 | US10980815, Ex. No. 95 | ...)
Affinity DataIC50: 35nMAssay 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 Depth
Date in BDB:
4/24/2022
Entry Details
Go to US Patent

TargetTyrosine-protein kinase JAK3(Human)
Pfizer

US Patent
LigandPNGBDBM419652(US10463675, Example 95 | US10980815, Ex. No. 95 | ...)
Affinity DataIC50: 255nMAssay 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:
10/26/2021
Entry Details
Go to US Patent

TargetTyrosine-protein kinase JAK2(Human)
Pfizer

US Patent
LigandPNGBDBM419652(US10463675, Example 95 | US10980815, Ex. No. 95 | ...)
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:
10/26/2021
Entry Details
Go to US Patent

TargetTyrosine-protein kinase JAK1(Human)
Pfizer

US Patent
LigandPNGBDBM419652(US10463675, Example 95 | US10980815, Ex. No. 95 | ...)
Affinity DataIC50: 11nMAssay 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:
10/26/2021
Entry Details
Go to US Patent

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

US Patent
LigandPNGBDBM419652(US10463675, Example 95 | US10980815, Ex. No. 95 | ...)
Affinity DataIC50: 35nMAssay 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:
10/26/2021
Entry Details
Go to US Patent

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

US Patent
LigandPNGBDBM419652(US10463675, Example 95 | US10980815, Ex. No. 95 | ...)
Affinity DataIC50: 35nMAssay 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:
9/8/2020
Entry Details
Go to US Patent

LigandPNGBDBM419652(US10463675, Example 95 | US10980815, Ex. No. 95 | ...)
Affinity DataIC50: 87nMAssay Description:Inhibition of JAK1/TYK2 in human whole blood assessed as reduction in IFNalpha-induced STAT phosphorylation by flow cytometryMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/13/2021
Entry Details Article
PubMed
TargetTyrosine-protein kinase JAK3(Human)
Pfizer

US Patent
LigandPNGBDBM419652(US10463675, Example 95 | US10980815, Ex. No. 95 | ...)
Affinity DataIC50: 255nMAssay Description:Inhibition of human recombinant JAK3 assessed as level of phosphorylation in presence of peptide substrate FITC-KGGEEEEYFELVKK and ATP by mobility sh...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/13/2021
Entry Details Article
PubMed
TargetTyrosine-protein kinase JAK2(Human)
Pfizer

US Patent
LigandPNGBDBM419652(US10463675, Example 95 | US10980815, Ex. No. 95 | ...)
Affinity DataIC50: 228nMAssay Description:Inhibition of human recombinant JAK2 assessed as level of phosphorylation in presence of peptide substrate FITC-KGGEEEEYFELVKK and ATP by mobility sh...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/13/2021
Entry Details Article
PubMed
TargetTyrosine-protein kinase JAK1(Human)
Pfizer

US Patent
LigandPNGBDBM419652(US10463675, Example 95 | US10980815, Ex. No. 95 | ...)
Affinity DataIC50: 11nMAssay Description:Inhibition of human recombinant JAK1 assessed as level of phosphorylation in presence of peptide substrate 5FAM-KKSRGDYMTMQUID and ATP by mobility sh...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/13/2021
Entry Details Article
PubMed
TargetNon-receptor tyrosine-protein kinase TYK2(Human)
Pfizer

US Patent
LigandPNGBDBM419652(US10463675, Example 95 | US10980815, Ex. No. 95 | ...)
Affinity DataIC50: 32nMAssay Description:Inhibition of human recombinant TYK2 assessed as level of phosphorylation in presence of peptide substrate 5FAM-KKSRGDYMTMQID and ATP by mobility shi...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/13/2021
Entry Details Article
PubMed
TargetTyrosine-protein kinase JAK3(Human)
Pfizer

US Patent
LigandPNGBDBM419652(US10463675, Example 95 | US10980815, Ex. No. 95 | ...)
Affinity DataIC50: 255nMAssay 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:
9/8/2020
Entry Details
Go to US Patent

TargetTyrosine-protein kinase JAK2(Human)
Pfizer

US Patent
LigandPNGBDBM419652(US10463675, Example 95 | US10980815, Ex. No. 95 | ...)
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:
9/8/2020
Entry Details
Go to US Patent

TargetTyrosine-protein kinase JAK1(Human)
Pfizer

US Patent
LigandPNGBDBM419652(US10463675, Example 95 | US10980815, Ex. No. 95 | ...)
Affinity DataIC50: 11nMAssay 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:
9/8/2020
Entry Details
Go to US Patent