Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB (change energy unit to kcal/mol)

Found 26 hits in this display   

TargetMitogen-activated protein kinase kinase kinase 11(Homo sapiens (Human))
Cephalon

LigandPNGBDBM2581(3,13,23-triazahexacyclo[14.7.0.0^{2,10}.0^{4,9}.0^...)
Affinity DataIC50:  49nMAssay Description:The MLK1, MLK2, and MLK3 assays were performed using the Millipore multiscreen trichloroacetic acid (TCA) in-plate format. IC50 values were calculate...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK3(Homo sapiens (Human))
Johnson & Johnson Pharmaceutical Research & Development

Curated by ChEMBL
LigandPNGBDBM2581(3,13,23-triazahexacyclo[14.7.0.0^{2,10}.0^{4,9}.0^...)
Affinity DataIC50:  61nMAssay Description:Inhibition of JAK3 expressed in insect Sf21 cells assessed as inhibition of biotinylated substrate phosphorylationMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMitogen-activated protein kinase kinase kinase 9(Homo sapiens (Human))
Cephalon

LigandPNGBDBM2581(3,13,23-triazahexacyclo[14.7.0.0^{2,10}.0^{4,9}.0^...)
Affinity DataIC50:  138nMpH: 7.2 T: 2°CAssay Description:The MLK1, MLK2, and MLK3 assays were performed using the Millipore multiscreen trichloroacetic acid (TCA) in-plate format. IC50 values were calculate...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM2581(3,13,23-triazahexacyclo[14.7.0.0^{2,10}.0^{4,9}.0^...)
Affinity DataIC50:  184nMAssay Description:Inhibitory activity against Cyclin D1-cyclin-dependent kinase 4 by measuring the phosphorylation of RbINGMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetcGMP-dependent protein kinase 1(Bos taurus (bovine))
TBA

Curated by ChEMBL
LigandPNGBDBM2581(3,13,23-triazahexacyclo[14.7.0.0^{2,10}.0^{4,9}.0^...)
Affinity DataIC50:  650nMAssay Description:In vitro for inhibitory activity against cGMP-dependent protein kinase from bovine lung (G-kinase)More data for this Ligand-Target Pair
In DepthDetails Article
LigandPNGBDBM2581(3,13,23-triazahexacyclo[14.7.0.0^{2,10}.0^{4,9}.0^...)
Affinity DataIC50:  680nMAssay Description:In vitro for inhibitory activity against protein kinase C from rat brainMore data for this Ligand-Target Pair
In DepthDetails Article
TargetCyclin-dependent kinase 4/G1/S-specific cyclin-D1(Homo sapiens (Human))
Eli Lilly

LigandPNGBDBM2581(3,13,23-triazahexacyclo[14.7.0.0^{2,10}.0^{4,9}.0^...)
Affinity DataIC50:  830nMpH: 7.0 T: 2°CAssay Description:In vitro CDK assay using purified enzyme, was incubated at room temperature with substrate, and test compounds in the presence of ATP/[gamma-33P]ATP....More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCyclin-dependent kinase 4/G1/S-specific cyclin-D1(Homo sapiens (Human))
Eli Lilly

LigandPNGBDBM2581(3,13,23-triazahexacyclo[14.7.0.0^{2,10}.0^{4,9}.0^...)
Affinity DataIC50:  830nMAssay Description:Inhibitory activity against Cyclin D1-cyclin-dependent kinase 4 by measuring the phosphorylation of RbINGMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM2581(3,13,23-triazahexacyclo[14.7.0.0^{2,10}.0^{4,9}.0^...)
Affinity DataIC50: >1.00E+3nMAssay Description:Inhibitory activity against Cyclin D1-cyclin-dependent kinase 4 by measuring the phosphorylation of RbINGMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetZinc finger protein GLI1(Homo sapiens (Human))
St. Jude Children'S Research Hospital

Curated by ChEMBL
LigandPNGBDBM2581(3,13,23-triazahexacyclo[14.7.0.0^{2,10}.0^{4,9}.0^...)
Affinity DataIC50:  1.80E+3nMAssay Description:Inhibition of Gli1-mediated transcription expressed in human PANC1 cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetcAMP-dependent protein kinase catalytic subunit alpha/beta/gamma(Homo sapiens (Human))
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM2581(3,13,23-triazahexacyclo[14.7.0.0^{2,10}.0^{4,9}.0^...)
Affinity DataIC50: >2.00E+3nMAssay Description:Inhibitory activity against Cyclin D1-cyclin-dependent kinase 4 by measuring the phosphorylation of RbINGMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProtein kinase C alpha type(Homo sapiens (Human))
Université

Curated by ChEMBL
LigandPNGBDBM2581(3,13,23-triazahexacyclo[14.7.0.0^{2,10}.0^{4,9}.0^...)
Affinity DataIC50:  2.45E+3nMAssay Description:Inhibition of Protein Kinase C(PKC)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM2581(3,13,23-triazahexacyclo[14.7.0.0^{2,10}.0^{4,9}.0^...)
Affinity DataIC50:  2.45E+3nMAssay Description:Competitive inhibition of human MDH2 using oxaloacetic acid as substrate in presence of NADH after 30 mins by double reciprocal plot analysisMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProtein kinase C theta type(Homo sapiens (Human))
Zhejiang University

Curated by ChEMBL
LigandPNGBDBM2581(3,13,23-triazahexacyclo[14.7.0.0^{2,10}.0^{4,9}.0^...)
Affinity DataIC50: >2.50E+3nMAssay Description:Inhibition of PKCtheta (unknown origin) by HTRF assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetZinc finger protein GLI2(Homo sapiens (Human))
St. Jude Children'S Research Hospital

Curated by ChEMBL
LigandPNGBDBM2581(3,13,23-triazahexacyclo[14.7.0.0^{2,10}.0^{4,9}.0^...)
Affinity DataIC50:  2.70E+3nMAssay Description:Inhibition of Gli2-mediated transcription expressed in human PANC1 cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMyosin light chain kinase, smooth muscle(Gallus gallus (chicken))
TBA

Curated by ChEMBL
LigandPNGBDBM2581(3,13,23-triazahexacyclo[14.7.0.0^{2,10}.0^{4,9}.0^...)
Affinity DataIC50:  2.80E+3nMAssay Description:In vitro for inhibitory activity against myosin light-chain kinase from chicken gizzard (M-kinase)More data for this Ligand-Target Pair
In DepthDetails Article
TargetBeta-lactamase(Escherichia coli)
Northwestern University

Curated by ChEMBL
LigandPNGBDBM2581(3,13,23-triazahexacyclo[14.7.0.0^{2,10}.0^{4,9}.0^...)
Affinity DataIC50:  8.00E+3nMAssay Description:Inhibitory activity against Amp C beta-LactamaseMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMalate dehydrogenase(Thermus thermophilus)
Northwestern University

Curated by ChEMBL
LigandPNGBDBM2581(3,13,23-triazahexacyclo[14.7.0.0^{2,10}.0^{4,9}.0^...)
Affinity DataIC50:  8.00E+3nMAssay Description:Inhibitory activity against malate dehydrogenase (MDH) from Thermus flavusMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetChymotrypsinogen B(Homo sapiens (Human))
Northwestern University

Curated by ChEMBL
LigandPNGBDBM2581(3,13,23-triazahexacyclo[14.7.0.0^{2,10}.0^{4,9}.0^...)
Affinity DataIC50:  1.00E+4nMAssay Description:Inhibitory activity against Chymotrypsinogen from Thermus flavusMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetcAMP-dependent protein kinase catalytic subunit alpha(Bos taurus (bovine))
TBA

Curated by ChEMBL
LigandPNGBDBM2581(3,13,23-triazahexacyclo[14.7.0.0^{2,10}.0^{4,9}.0^...)
Affinity DataIC50: >1.00E+4nMAssay Description:In vitro for inhibitory activity against cAMP-dependent protein kinase from bovine heart (A-kinase)More data for this Ligand-Target Pair
In DepthDetails Article
TargetcAMP-dependent protein kinase catalytic subunit alpha(Bos taurus (bovine))
TBA

Curated by ChEMBL
LigandPNGBDBM2581(3,13,23-triazahexacyclo[14.7.0.0^{2,10}.0^{4,9}.0^...)
Affinity DataIC50: >2.50E+4nMpH: 7.4 T: 2°CAssay Description:IC50 is the inhibitor concentration which inhibits 50% of kinase activity that catalyzes the transfer of the terminal phosphate from [gamma-32P] labe...More data for this Ligand-Target Pair
In DepthDetails PubMed
LigandPNGBDBM2581(3,13,23-triazahexacyclo[14.7.0.0^{2,10}.0^{4,9}.0^...)
Affinity DataIC50:  2.57E+4nMAssay Description:Inhibition of protein kinase AMore data for this Ligand-Target Pair
In DepthDetails
TargetcAMP-dependent protein kinase catalytic subunit alpha/beta/gamma(Homo sapiens (Human))
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM2581(3,13,23-triazahexacyclo[14.7.0.0^{2,10}.0^{4,9}.0^...)
Affinity DataIC50:  2.57E+4nMAssay Description:Inhibition of Protein kinase AMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProtein kinase C beta type(Rattus norvegicus (rat))
Roche Products

LigandPNGBDBM2581(3,13,23-triazahexacyclo[14.7.0.0^{2,10}.0^{4,9}.0^...)
Affinity DatapH: 7.5 T: 2°CAssay Description:The activity of PKC, activated by phosphatidylerine and Ca2+, is measured by its ability to transfer phosphate from [gamma-32P]ATP to lysine-rich his...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed