Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB (change energy unit to kcal/mol)
Found 149 hits in this display
BDBM31539(pyrazolo[4,3-h]quinazoline-3-carboxamide, 22)
BDBM31541(pyrazolo[4,3-h]quinazoline-3-carboxamide, 24)
BDBM31532(pyrazolo[4,3-h]quinazoline-3-carboxamide, 1)
BDBM31532(pyrazolo[4,3-h]quinazoline-3-carboxamide, 1)
BDBM31539(pyrazolo[4,3-h]quinazoline-3-carboxamide, 22)
IC50: 2nMpH: 7.4 T: 2°CAssay Description:The biochemical activity of compounds was determined by incubation with specific enzymes and substrates, followed by quantitation of the phosphorylat...More data for this Ligand-Target Pair
BDBM50318088(8-[(3-Acetylphenyl)amino]-1-methyl-4,5-dihydro-1H-...)
BDBM31532(pyrazolo[4,3-h]quinazoline-3-carboxamide, 1)
IC50: 2nMpH: 7.4 T: 2°CAssay Description:The biochemical activity of compounds was determined by incubation with specific enzymes and substrates, followed by quantitation of the phosphorylat...More data for this Ligand-Target Pair
BDBM31532(pyrazolo[4,3-h]quinazoline-3-carboxamide, 1)
BDBM31539(pyrazolo[4,3-h]quinazoline-3-carboxamide, 22)
BDBM31545(Milciclib | pyrazolo[4,3-h]quinazoline-3-carboxami...)
BDBM31543(pyrazolo[4,3-h]quinazoline-3-carboxamide, 26)
BDBM31545(Milciclib | pyrazolo[4,3-h]quinazoline-3-carboxami...)
BDBM31545(Milciclib | pyrazolo[4,3-h]quinazoline-3-carboxami...)
BDBM31545(Milciclib | pyrazolo[4,3-h]quinazoline-3-carboxami...)
BDBM31532(pyrazolo[4,3-h]quinazoline-3-carboxamide, 1)
BDBM31539(pyrazolo[4,3-h]quinazoline-3-carboxamide, 22)
BDBM31532(pyrazolo[4,3-h]quinazoline-3-carboxamide, 1)
BDBM31543(pyrazolo[4,3-h]quinazoline-3-carboxamide, 26)
BDBM31532(pyrazolo[4,3-h]quinazoline-3-carboxamide, 1)
BDBM31542(pyrazolo[4,3-h]quinazoline-3-carboxamide, 25)
IC50: 14nMpH: 7.4 T: 2°CAssay Description:The biochemical activity of compounds was determined by incubation with specific enzymes and substrates, followed by quantitation of the phosphorylat...More data for this Ligand-Target Pair
BDBM31544(pyrazolo[4,3-h]quinazoline-3-carboxamide, 27)
IC50: 17nMpH: 7.4 T: 2°CAssay Description:The biochemical activity of compounds was determined by incubation with specific enzymes and substrates, followed by quantitation of the phosphorylat...More data for this Ligand-Target Pair
BDBM50307544(1-Methyl-8-{[4-(4-methylpiperazin-1-yl)benzyl]amin...)
BDBM31533(pyrazolo[4,3-h]quinazoline-3-carboxamide, 16)
IC50: 19nMpH: 7.4 T: 2°CAssay Description:The biochemical activity of compounds was determined by incubation with specific enzymes and substrates, followed by quantitation of the phosphorylat...More data for this Ligand-Target Pair
BDBM31533(pyrazolo[4,3-h]quinazoline-3-carboxamide, 16)
BDBM31533(pyrazolo[4,3-h]quinazoline-3-carboxamide, 16)
BDBM31543(pyrazolo[4,3-h]quinazoline-3-carboxamide, 26)
IC50: 24nMpH: 7.4 T: 2°CAssay Description:The biochemical activity of compounds was determined by incubation with specific enzymes and substrates, followed by quantitation of the phosphorylat...More data for this Ligand-Target Pair
BDBM139107(US8614220, A85B1C4Z)
BDBM31541(pyrazolo[4,3-h]quinazoline-3-carboxamide, 24)
BDBM31546(pyrazolo[4,3-h]quinazoline-3-carboxamide, 29)
IC50: 31nMpH: 7.4 T: 2°CAssay Description:The biochemical activity of compounds was determined by incubation with specific enzymes and substrates, followed by quantitation of the phosphorylat...More data for this Ligand-Target Pair
BDBM31557(pyrazolo[4,3-h]quinazoline-3-carboxamide, 40)
IC50: 35nMpH: 7.4 T: 2°CAssay Description:The biochemical activity of compounds was determined by incubation with specific enzymes and substrates, followed by quantitation of the phosphorylat...More data for this Ligand-Target Pair
BDBM31553(pyrazolo[4,3-h]quinazoline-3-carboxamide, 36)
IC50: 36nMpH: 7.4 T: 2°CAssay Description:The biochemical activity of compounds was determined by incubation with specific enzymes and substrates, followed by quantitation of the phosphorylat...More data for this Ligand-Target Pair
BDBM31533(pyrazolo[4,3-h]quinazoline-3-carboxamide, 16)
BDBM31540(pyrazolo[4,3-h]quinazoline-3-carboxamide, 23)
IC50: 45nMpH: 7.4 T: 2°CAssay Description:The biochemical activity of compounds was determined by incubation with specific enzymes and substrates, followed by quantitation of the phosphorylat...More data for this Ligand-Target Pair
BDBM31545(Milciclib | pyrazolo[4,3-h]quinazoline-3-carboxami...)
IC50: 45nMpH: 7.4 T: 2°CAssay Description:The biochemical activity of compounds was determined by incubation with specific enzymes and substrates, followed by quantitation of the phosphorylat...More data for this Ligand-Target Pair
BDBM31545(Milciclib | pyrazolo[4,3-h]quinazoline-3-carboxami...)
BDBM31545(Milciclib | pyrazolo[4,3-h]quinazoline-3-carboxami...)
BDBM31532(pyrazolo[4,3-h]quinazoline-3-carboxamide, 1)
IC50: 50nMT: 2°CAssay Description:The biochemical activity of compounds was determined by incubation with specific enzymes and substrates, followed by quantitation of the phosphorylat...More data for this Ligand-Target Pair
BDBM31532(pyrazolo[4,3-h]quinazoline-3-carboxamide, 1)
BDBM31532(pyrazolo[4,3-h]quinazoline-3-carboxamide, 1)
BDBM31542(pyrazolo[4,3-h]quinazoline-3-carboxamide, 25)
IC50: 51nMT: 2°CAssay Description:The biochemical activity of compounds was determined by incubation with specific enzymes and substrates, followed by quantitation of the phosphorylat...More data for this Ligand-Target Pair
BDBM31545(Milciclib | pyrazolo[4,3-h]quinazoline-3-carboxami...)
BDBM31539(pyrazolo[4,3-h]quinazoline-3-carboxamide, 22)
IC50: 53nMT: 2°CAssay Description:The biochemical activity of compounds was determined by incubation with specific enzymes and substrates, followed by quantitation of the phosphorylat...More data for this Ligand-Target Pair
BDBM31551(pyrazolo[4,3-h]quinazoline-3-carboxamide, 34)
IC50: 55nMpH: 7.4 T: 2°CAssay Description:The biochemical activity of compounds was determined by incubation with specific enzymes and substrates, followed by quantitation of the phosphorylat...More data for this Ligand-Target Pair
BDBM31532(pyrazolo[4,3-h]quinazoline-3-carboxamide, 1)
BDBM31552(pyrazolo[4,3-h]quinazoline-3-carboxamide, 35)
IC50: 59nMpH: 7.4 T: 2°CAssay Description:The biochemical activity of compounds was determined by incubation with specific enzymes and substrates, followed by quantitation of the phosphorylat...More data for this Ligand-Target Pair
BDBM31555(pyrazolo[4,3-h]quinazoline-3-carboxamide, 38)
IC50: 59nMpH: 7.4 T: 2°CAssay Description:The biochemical activity of compounds was determined by incubation with specific enzymes and substrates, followed by quantitation of the phosphorylat...More data for this Ligand-Target Pair
BDBM31532(pyrazolo[4,3-h]quinazoline-3-carboxamide, 1)
IC50: 68nMAssay Description:Inhibition of GST-tagged PLK1 expressed in H5 insect cells assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma countingMore data for this Ligand-Target Pair
BDBM31532(pyrazolo[4,3-h]quinazoline-3-carboxamide, 1)
BDBM31558(pyrazolo[4,3-h]quinazoline-3-carboxamide, 41)
IC50: 83nMpH: 7.4 T: 2°CAssay Description:The biochemical activity of compounds was determined by incubation with specific enzymes and substrates, followed by quantitation of the phosphorylat...More data for this Ligand-Target Pair
BDBM50318088(8-[(3-Acetylphenyl)amino]-1-methyl-4,5-dihydro-1H-...)
IC50: 100nMAssay Description:Inhibition of GST-tagged PLK1 expressed in H5 insect cells assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma countingMore data for this Ligand-Target Pair
BDBM31545(Milciclib | pyrazolo[4,3-h]quinazoline-3-carboxami...)
BDBM50307551(1-Methyl-8-{[3-(4-methylpiperazin-1-yl)benzyl]amin...)
BDBM50318079(8-{[2-Acetyl-5-(4-methylpiperazin-1-yl)phenyl]amin...)
IC50: 109nMAssay Description:Inhibition of GST-tagged PLK1 expressed in H5 insect cells assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma countingMore data for this Ligand-Target Pair
BDBM31545(Milciclib | pyrazolo[4,3-h]quinazoline-3-carboxami...)
BDBM31547(pyrazolo[4,3-h]quinazoline-3-carboxamide, 30)
IC50: 137nMpH: 7.4 T: 2°CAssay Description:The biochemical activity of compounds was determined by incubation with specific enzymes and substrates, followed by quantitation of the phosphorylat...More data for this Ligand-Target Pair
BDBM31545(Milciclib | pyrazolo[4,3-h]quinazoline-3-carboxami...)
BDBM31554(pyrazolo[4,3-h]quinazoline-3-carboxamide, 37)
IC50: 160nMpH: 7.4 T: 2°CAssay Description:The biochemical activity of compounds was determined by incubation with specific enzymes and substrates, followed by quantitation of the phosphorylat...More data for this Ligand-Target Pair
BDBM31545(Milciclib | pyrazolo[4,3-h]quinazoline-3-carboxami...)
BDBM31533(pyrazolo[4,3-h]quinazoline-3-carboxamide, 16)
BDBM31540(pyrazolo[4,3-h]quinazoline-3-carboxamide, 23)
IC50: 175nMT: 2°CAssay Description:The biochemical activity of compounds was determined by incubation with specific enzymes and substrates, followed by quantitation of the phosphorylat...More data for this Ligand-Target Pair
BDBM50318088(8-[(3-Acetylphenyl)amino]-1-methyl-4,5-dihydro-1H-...)
BDBM31556(pyrazolo[4,3-h]quinazoline-3-carboxamide, 39)
IC50: 220nMpH: 7.4 T: 2°CAssay Description:The biochemical activity of compounds was determined by incubation with specific enzymes and substrates, followed by quantitation of the phosphorylat...More data for this Ligand-Target Pair
BDBM31545(Milciclib | pyrazolo[4,3-h]quinazoline-3-carboxami...)
BDBM31548(pyrazolo[4,3-h]quinazoline-3-carboxamide, 31)
IC50: 248nMpH: 7.4 T: 2°CAssay Description:The biochemical activity of compounds was determined by incubation with specific enzymes and substrates, followed by quantitation of the phosphorylat...More data for this Ligand-Target Pair
BDBM31545(Milciclib | pyrazolo[4,3-h]quinazoline-3-carboxami...)
IC50: 265nMpH: 7.4 T: 2°CAssay Description:The biochemical activity of compounds was determined by incubation with specific enzymes and substrates, followed by quantitation of the phosphorylat...More data for this Ligand-Target Pair
BDBM31545(Milciclib | pyrazolo[4,3-h]quinazoline-3-carboxami...)
BDBM31542(pyrazolo[4,3-h]quinazoline-3-carboxamide, 25)
BDBM31533(pyrazolo[4,3-h]quinazoline-3-carboxamide, 16)
BDBM31533(pyrazolo[4,3-h]quinazoline-3-carboxamide, 16)
BDBM31533(pyrazolo[4,3-h]quinazoline-3-carboxamide, 16)
IC50: 312nMT: 2°CAssay Description:The biochemical activity of compounds was determined by incubation with specific enzymes and substrates, followed by quantitation of the phosphorylat...More data for this Ligand-Target Pair
BDBM50321581(1-METHYL-8-{[4-(4-METHYLPIPERAZIN-1-YL)PHENYL]AMIN...)
BDBM31542(pyrazolo[4,3-h]quinazoline-3-carboxamide, 25)
BDBM31542(pyrazolo[4,3-h]quinazoline-3-carboxamide, 25)
BDBM31545(Milciclib | pyrazolo[4,3-h]quinazoline-3-carboxami...)
IC50: 363nMT: 2°CAssay Description:The biochemical activity of compounds was determined by incubation with specific enzymes and substrates, followed by quantitation of the phosphorylat...More data for this Ligand-Target Pair
BDBM31538(pyrazolo[4,3-h]quinazoline-3-carboxamide, 21)
BDBM31538(pyrazolo[4,3-h]quinazoline-3-carboxamide, 21)
IC50: 374nMT: 2°CAssay Description:The biochemical activity of compounds was determined by incubation with specific enzymes and substrates, followed by quantitation of the phosphorylat...More data for this Ligand-Target Pair
BDBM31545(Milciclib | pyrazolo[4,3-h]quinazoline-3-carboxami...)
BDBM31545(Milciclib | pyrazolo[4,3-h]quinazoline-3-carboxami...)
IC50: 398nMT: 2°CAssay Description:The biochemical activity of compounds was determined by incubation with specific enzymes and substrates, followed by quantitation of the phosphorylat...More data for this Ligand-Target Pair
BDBM50318073(8-{[2-Acetyl-4-(4-methylpiperazin-1-yl)phenyl]amin...)
IC50: 464nMAssay Description:Inhibition of GST-tagged PLK1 expressed in H5 insect cells assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma countingMore data for this Ligand-Target Pair
BDBM31532(pyrazolo[4,3-h]quinazoline-3-carboxamide, 1)
BDBM31553(pyrazolo[4,3-h]quinazoline-3-carboxamide, 36)
IC50: 535nMT: 2°CAssay Description:The biochemical activity of compounds was determined by incubation with specific enzymes and substrates, followed by quantitation of the phosphorylat...More data for this Ligand-Target Pair
BDBM31544(pyrazolo[4,3-h]quinazoline-3-carboxamide, 27)
IC50: 582nMT: 2°CAssay Description:The biochemical activity of compounds was determined by incubation with specific enzymes and substrates, followed by quantitation of the phosphorylat...More data for this Ligand-Target Pair
BDBM31545(Milciclib | pyrazolo[4,3-h]quinazoline-3-carboxami...)
BDBM31548(pyrazolo[4,3-h]quinazoline-3-carboxamide, 31)
IC50: 625nMT: 2°CAssay Description:The biochemical activity of compounds was determined by incubation with specific enzymes and substrates, followed by quantitation of the phosphorylat...More data for this Ligand-Target Pair
BDBM31554(pyrazolo[4,3-h]quinazoline-3-carboxamide, 37)
IC50: 638nMT: 2°CAssay Description:The biochemical activity of compounds was determined by incubation with specific enzymes and substrates, followed by quantitation of the phosphorylat...More data for this Ligand-Target Pair
BDBM31547(pyrazolo[4,3-h]quinazoline-3-carboxamide, 30)
IC50: 649nMT: 2°CAssay Description:The biochemical activity of compounds was determined by incubation with specific enzymes and substrates, followed by quantitation of the phosphorylat...More data for this Ligand-Target Pair
BDBM31555(pyrazolo[4,3-h]quinazoline-3-carboxamide, 38)
IC50: 855nMT: 2°CAssay Description:The biochemical activity of compounds was determined by incubation with specific enzymes and substrates, followed by quantitation of the phosphorylat...More data for this Ligand-Target Pair
BDBM31546(pyrazolo[4,3-h]quinazoline-3-carboxamide, 29)
IC50: 1.00E+3nMT: 2°CAssay Description:The biochemical activity of compounds was determined by incubation with specific enzymes and substrates, followed by quantitation of the phosphorylat...More data for this Ligand-Target Pair
BDBM31533(pyrazolo[4,3-h]quinazoline-3-carboxamide, 16)
BDBM31545(Milciclib | pyrazolo[4,3-h]quinazoline-3-carboxami...)
IC50: 1.05E+3nMT: 2°CAssay Description:The biochemical activity of compounds was determined by incubation with specific enzymes and substrates, followed by quantitation of the phosphorylat...More data for this Ligand-Target Pair
BDBM31538(pyrazolo[4,3-h]quinazoline-3-carboxamide, 21)
IC50: 1.05E+3nMpH: 7.4 T: 2°CAssay Description:The biochemical activity of compounds was determined by incubation with specific enzymes and substrates, followed by quantitation of the phosphorylat...More data for this Ligand-Target Pair
BDBM31538(pyrazolo[4,3-h]quinazoline-3-carboxamide, 21)
BDBM50318068(8-{[2-Acetyl-3-(4-methylpiperazin-1-yl)phenyl]amin...)
IC50: 1.12E+3nMAssay Description:Inhibition of CDK2/Cyclin A assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma countingMore data for this Ligand-Target Pair
BDBM31552(pyrazolo[4,3-h]quinazoline-3-carboxamide, 35)
IC50: 1.18E+3nMT: 2°CAssay Description:The biochemical activity of compounds was determined by incubation with specific enzymes and substrates, followed by quantitation of the phosphorylat...More data for this Ligand-Target Pair
BDBM31545(Milciclib | pyrazolo[4,3-h]quinazoline-3-carboxami...)
BDBM50307544(1-Methyl-8-{[4-(4-methylpiperazin-1-yl)benzyl]amin...)
BDBM31556(pyrazolo[4,3-h]quinazoline-3-carboxamide, 39)
IC50: 1.44E+3nMT: 2°CAssay Description:The biochemical activity of compounds was determined by incubation with specific enzymes and substrates, followed by quantitation of the phosphorylat...More data for this Ligand-Target Pair
BDBM31551(pyrazolo[4,3-h]quinazoline-3-carboxamide, 34)
IC50: 1.62E+3nMT: 2°CAssay Description:The biochemical activity of compounds was determined by incubation with specific enzymes and substrates, followed by quantitation of the phosphorylat...More data for this Ligand-Target Pair
BDBM50318068(8-{[2-Acetyl-3-(4-methylpiperazin-1-yl)phenyl]amin...)
IC50: 2.05E+3nMAssay Description:Inhibition of GST-tagged PLK1 expressed in H5 insect cells assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma countingMore data for this Ligand-Target Pair
BDBM50307551(1-Methyl-8-{[3-(4-methylpiperazin-1-yl)benzyl]amin...)
BDBM31533(pyrazolo[4,3-h]quinazoline-3-carboxamide, 16)
BDBM50318073(8-{[2-Acetyl-4-(4-methylpiperazin-1-yl)phenyl]amin...)
BDBM31543(pyrazolo[4,3-h]quinazoline-3-carboxamide, 26)
BDBM31558(pyrazolo[4,3-h]quinazoline-3-carboxamide, 41)
IC50: 2.94E+3nMT: 2°CAssay Description:The biochemical activity of compounds was determined by incubation with specific enzymes and substrates, followed by quantitation of the phosphorylat...More data for this Ligand-Target Pair
BDBM31533(pyrazolo[4,3-h]quinazoline-3-carboxamide, 16)
BDBM31533(pyrazolo[4,3-h]quinazoline-3-carboxamide, 16)
IC50: 4.22E+3nMAssay Description:Inhibition of GST-tagged PLK1 expressed in H5 insect cells assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma countingMore data for this Ligand-Target Pair
BDBM31557(pyrazolo[4,3-h]quinazoline-3-carboxamide, 40)
IC50: >5.00E+3nMT: 2°CAssay Description:The biochemical activity of compounds was determined by incubation with specific enzymes and substrates, followed by quantitation of the phosphorylat...More data for this Ligand-Target Pair
BDBM31545(Milciclib | pyrazolo[4,3-h]quinazoline-3-carboxami...)
BDBM50318068(8-{[2-Acetyl-3-(4-methylpiperazin-1-yl)phenyl]amin...)
BDBM31538(pyrazolo[4,3-h]quinazoline-3-carboxamide, 21)
BDBM31543(pyrazolo[4,3-h]quinazoline-3-carboxamide, 26)
IC50: >1.00E+4nMT: 2°CAssay Description:The biochemical activity of compounds was determined by incubation with specific enzymes and substrates, followed by quantitation of the phosphorylat...More data for this Ligand-Target Pair
BDBM50318079(8-{[2-Acetyl-5-(4-methylpiperazin-1-yl)phenyl]amin...)
IC50: >1.00E+4nMAssay Description:Inhibition of CDK2/Cyclin A assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma countingMore data for this Ligand-Target Pair
BDBM50318073(8-{[2-Acetyl-4-(4-methylpiperazin-1-yl)phenyl]amin...)
IC50: >1.00E+4nMAssay Description:Inhibition of CDK2/Cyclin A assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma countingMore data for this Ligand-Target Pair
BDBM50318079(8-{[2-Acetyl-5-(4-methylpiperazin-1-yl)phenyl]amin...)
BDBM50318068(8-{[2-Acetyl-3-(4-methylpiperazin-1-yl)phenyl]amin...)
BDBM50318068(8-{[2-Acetyl-3-(4-methylpiperazin-1-yl)phenyl]amin...)
BDBM50318073(8-{[2-Acetyl-4-(4-methylpiperazin-1-yl)phenyl]amin...)
BDBM50318073(8-{[2-Acetyl-4-(4-methylpiperazin-1-yl)phenyl]amin...)
BDBM50318079(8-{[2-Acetyl-5-(4-methylpiperazin-1-yl)phenyl]amin...)
BDBM50318079(8-{[2-Acetyl-5-(4-methylpiperazin-1-yl)phenyl]amin...)
BDBM31538(pyrazolo[4,3-h]quinazoline-3-carboxamide, 21)
BDBM31545(Milciclib | pyrazolo[4,3-h]quinazoline-3-carboxami...)
BDBM31545(Milciclib | pyrazolo[4,3-h]quinazoline-3-carboxami...)
BDBM31545(Milciclib | pyrazolo[4,3-h]quinazoline-3-carboxami...)
Kd: 990nMAssay Description:Binding affinity to recombinant human N-terminal His6-tagged Myt1 kinase domain (75 to 361 residues) by isothermal titration calorimetryMore data for this Ligand-Target Pair
BDBM31545(Milciclib | pyrazolo[4,3-h]quinazoline-3-carboxami...)
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