BDBM8126 N-phenyl-4-{pyrazolo[1,5-a]pyridazin-3-yl}pyrimidin-2-amine::pyrazolo[1,5-b]pyridazine deriv. 16

SMILES N(c1ccccc1)c1nccc(n1)-c1cnn2ncccc12

InChI Key InChIKey=LIYXXFOSHNQSRD-UHFFFAOYSA-N

Data  1 KI  10 IC50

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
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Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 11 hits for monomerid = 8126   

TargetGlycogen synthase kinase-3 beta(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM8126(N-phenyl-4-{pyrazolo[1,5-a]pyridazin-3-yl}pyrimidi...)
Affinity DataKi:  19nMAssay Description:Inhibition of GSK3beta expressed in Escherichia coli or baculovirus-infected insect cells using ATP as substrate by fluorescence polarization assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlycogen synthase kinase-3 beta(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM8126(N-phenyl-4-{pyrazolo[1,5-a]pyridazin-3-yl}pyrimidi...)
Affinity DataIC50:  19nMAssay Description:The biochemical activity of compounds was determined by incubation with specific enzyme and substrate in the presence 2.5 uM ATP/ [gamma-32P] ATP. Af...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCyclin-dependent kinase 4/G1/S-specific cyclin-D1(Homo sapiens (Human))
Glaxosmithkline

LigandPNGBDBM8126(N-phenyl-4-{pyrazolo[1,5-a]pyridazin-3-yl}pyrimidi...)
Affinity DataIC50:  158nMAssay Description:The biochemical activity of compounds was determined by incubation with specific enzyme and substrate in the presence 2.5 uM ATP/ [gamma-32P] ATP. Af...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCyclin-dependent kinase 4(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM8126(N-phenyl-4-{pyrazolo[1,5-a]pyridazin-3-yl}pyrimidi...)
Affinity DataIC50:  12nMAssay Description:Inhibition of CDK4 by radioactive glutathione plate-binding assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlycogen synthase kinase-3 beta(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM8126(N-phenyl-4-{pyrazolo[1,5-a]pyridazin-3-yl}pyrimidi...)
Affinity DataIC50:  32nMAssay Description:Inhibition of GSK3beta by scintillation proximity assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDual specificity tyrosine-phosphorylation-regulated kinase 1A(Homo sapiens (Human))
University Of Sussex

Curated by ChEMBL
LigandPNGBDBM8126(N-phenyl-4-{pyrazolo[1,5-a]pyridazin-3-yl}pyrimidi...)
Affinity DataIC50:  38nMAssay Description:Inhibition of recombinant human N-terminal Hex-tagged DYRK1A (127 to 485 residues) expressed in Escherichia coli BL21 (DE3) incubated for 1.5 hrs by ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCyclin-dependent kinase 4(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM8126(N-phenyl-4-{pyrazolo[1,5-a]pyridazin-3-yl}pyrimidi...)
Affinity DataIC50:  158nMAssay Description:Inhibition of human CDK4 using biotinylated-aminohexyl-Ala-Ala-Ala-Lys-Arg-Arg-Glu-Ile-Leu-Ser-Arg-Arg-Pro-Ser(PO3)-Tyr-Arg-amide as substrate after ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlycogen synthase kinase-3 beta(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM8126(N-phenyl-4-{pyrazolo[1,5-a]pyridazin-3-yl}pyrimidi...)
Affinity DataIC50:  20nMAssay Description:Inhibition of human GSK3beta using biotinylated-aminohexyl-Ala-Ala-Ala-Lys-Arg-Arg-Glu-Ile-Leu-Ser-Arg-Arg-Pro-Ser(PO3)-Tyr-Arg-amide as substrate af...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCyclin-dependent kinase 2(Homo sapiens (Human))
Northeastern University

Curated by ChEMBL
LigandPNGBDBM8126(N-phenyl-4-{pyrazolo[1,5-a]pyridazin-3-yl}pyrimidi...)
Affinity DataIC50:  5nMAssay Description:Inhibition of human CDK2 using biotinylated-aminohexyl-Ala-Ala-Ala-Lys-Arg-Arg-Glu-Ile-Leu-Ser-Arg-Arg-Pro-Ser(PO3)-Tyr-Arg-amide as substrate after ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCyclin-A2/Cyclin-dependent kinase 2(Homo sapiens (Human))
Glaxosmithkline

LigandPNGBDBM8126(N-phenyl-4-{pyrazolo[1,5-a]pyridazin-3-yl}pyrimidi...)
Affinity DataIC50:  5nMpH: 7.2 T: 2°CAssay Description:The biochemical activity of compounds was determined by incubation with specific enzyme and substrate in the presence 2.5 uM ATP/ [gamma-32P] ATP. Af...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCyclin-dependent kinase 2(Homo sapiens (Human))
Northeastern University

Curated by ChEMBL
LigandPNGBDBM8126(N-phenyl-4-{pyrazolo[1,5-a]pyridazin-3-yl}pyrimidi...)
Affinity DataIC50:  8nMAssay Description:Inhibition of human CDK2 by HTRF assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed