PIK-75 [Ligand Id: 8012] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL393525
  • casein kinase 1 epsilon/Casein kinase I epsilon in Human [ChEMBL: CHEMBL4937] [GtoPdb: 1998] [UniProtKB: P49674]
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  • cyclin dependent kinase 2/Cyclin-dependent kinase 2 in Human [ChEMBL: CHEMBL301] [GtoPdb: 1973] [UniProtKB: P24941]
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  • cyclin dependent kinase 5/Cyclin-dependent kinase 5/CDK5 activator 1 in Human [ChEMBL: CHEMBL1907600] [GtoPdb: 1977] [UniProtKB: Q00535Q15078]
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  • cyclin dependent kinase 7/Cyclin-dependent kinase 7 in Human [ChEMBL: CHEMBL3055] [GtoPdb: 1979] [UniProtKB: P50613]
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  • cyclin dependent kinase 9/Cyclin-dependent kinase 9 in Human [ChEMBL: CHEMBL3116] [GtoPdb: 1981] [UniProtKB: P50750]
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  • CDC like kinase 2/Dual specificity protein kinase CLK2 in Human [ChEMBL: CHEMBL4225] [GtoPdb: 1991] [UniProtKB: P49760]
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  • CDC like kinase 3/Dual specificity protein kinase CLK3 in Human [ChEMBL: CHEMBL4226] [GtoPdb: 1992] [UniProtKB: P49761]
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  • CDC like kinase 4/Dual specificity protein kinase CLK4 in Human [ChEMBL: CHEMBL4203] [GtoPdb: 1993] [UniProtKB: Q9HAZ1]
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  • dual specificity tyrosine phosphorylation regulated kinase 1A/Dual-specificity tyrosine-phosphorylation regulated kinase 1A in Human [ChEMBL: CHEMBL2292] [GtoPdb: 2009] [UniProtKB: Q13627]
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  • dual specificity tyrosine phosphorylation regulated kinase 1B/Dual specificity tyrosine-phosphorylation-regulated kinase 1B in Human [ChEMBL: CHEMBL5543] [GtoPdb: 2010] [UniProtKB: Q9Y463]
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  • dual specificity tyrosine phosphorylation regulated kinase 2/Dual-specificity tyrosine-phosphorylation regulated kinase 2 in Human [ChEMBL: CHEMBL4376] [GtoPdb: 2011] [UniProtKB: Q92630]
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  • dual specificity tyrosine phosphorylation regulated kinase 3/Dual-specificity tyrosine-phosphorylation regulated kinase 3 in Human [ChEMBL: CHEMBL4575] [GtoPdb: 2012] [UniProtKB: O43781]
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  • dual specificity tyrosine phosphorylation regulated kinase 4/Dual specificity tyrosine-phosphorylation-regulated kinase 4 in Human [ChEMBL: CHEMBL1075115] [GtoPdb: 2013] [UniProtKB: Q9NR20]
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  • CDC like kinase 1/Dual specificty protein kinase CLK1 in Human [ChEMBL: CHEMBL4224] [GtoPdb: 1990] [UniProtKB: P49759]
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  • glycogen synthase kinase 3 beta/Glycogen synthase kinase-3 beta in Human [ChEMBL: CHEMBL262] [GtoPdb: 2030] [UniProtKB: P49841]
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  • phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha/PI3-kinase p110-alpha subunit in Human [ChEMBL: CHEMBL4005] [GtoPdb: 2153] [UniProtKB: P42336]
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  • phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit beta/PI3-kinase p110-beta subunit in Human [ChEMBL: CHEMBL3145] [GtoPdb: 2154] [UniProtKB: P42338]
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  • phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit delta/PI3-kinase p110-delta subunit in Human [ChEMBL: CHEMBL3130] [GtoPdb: 2155] [UniProtKB: O00329]
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  • fms related receptor tyrosine kinase 3/Tyrosine-protein kinase receptor FLT3 in Human [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888]
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  • phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma in Human [GtoPdb: 2156] [UniProtKB: P48736]
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  • protein kinase, DNA-activated, catalytic subunit in Human [GtoPdb: 2800] [UniProtKB: P78527]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
casein kinase 1 epsilon/Casein kinase I epsilon in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4937] [GtoPdb: 1998] [UniProtKB: P49674]
ChEMBL Inhibition of recombinant human CK1epsilon expressed in Sf9 insect cells incubated for 60 mins in presence of ATP and [gamma33-P] ATP by radiometric scintillation counter analysis B 6.39 pIC50 405 nM IC50 J Med Chem (2023) 66: 4106-4130 [PMID:36876904]
cyclin dependent kinase 9/CDK9/cyclin T1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111389] [GtoPdb: 1981] [UniProtKB: O60563P50750]
ChEMBL Inhibition of recombinant human CDK9/cyclin-T1 using H-YSPTSPSYSPTSPSYSPTSPS-KKKK-OH as substrate after 90 mins by luminescence assay B 8.86 pIC50 1.37 nM IC50 Bioorg Med Chem (2015) 23: 6280-6296 [PMID:26349627]
cyclin dependent kinase 2/Cyclin-dependent kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL301] [GtoPdb: 1973] [UniProtKB: P24941]
ChEMBL Binding affinity to full length human CDK2 (1 to 298 residues) expressed in bacterial expression system by KINOMEscan competition assay B 6.27 pKd 540 nM Kd J Med Chem (2016) 59: 8667-8684 [PMID:27171036]
cyclin dependent kinase 5/Cyclin-dependent kinase 5/CDK5 activator 1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907600] [GtoPdb: 1977] [UniProtKB: Q00535Q15078]
ChEMBL Inhibition of recombinant human CDK5/p25 expressed in Sf9 insect cells incubated for 60 mins in presence of ATP and [gamma33-P] ATP by radiometric scintillation counter analysis B 7.61 pIC50 24.5 nM IC50 J Med Chem (2023) 66: 4106-4130 [PMID:36876904]
cyclin dependent kinase 7/Cyclin-dependent kinase 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3055] [GtoPdb: 1979] [UniProtKB: P50613]
ChEMBL Binding affinity to full length human CDK7 (1 to 344 residues) expressed in mammalian expression system by KINOMEscan competition assay B 8.6 pKd 2.5 nM Kd J Med Chem (2016) 59: 8667-8684 [PMID:27171036]
cyclin dependent kinase 9/Cyclin-dependent kinase 9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3116] [GtoPdb: 1981] [UniProtKB: P50750]
ChEMBL Binding affinity to full length human CDK9 (1 to 372 residues) expressed in bacterial expression system by KINOMEscan competition assay B 8.39 pKd 4.1 nM Kd J Med Chem (2016) 59: 8667-8684 [PMID:27171036]
ChEMBL Inhibition of CDK9 (unknown origin) B 8.85 pIC50 1.4 nM IC50 J Med Chem (2016) 59: 8667-8684 [PMID:27171036]
CDC like kinase 2/Dual specificity protein kinase CLK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4225] [GtoPdb: 1991] [UniProtKB: P49760]
ChEMBL Inhibition of recombinant human CLK2 expressed in Sf9 insect cells incubated for 60 mins in presence of ATP and [gamma33-P] ATP by radiometric scintillation counter analysis B 8.96 pIC50 1.1 nM IC50 J Med Chem (2023) 66: 4106-4130 [PMID:36876904]
CDC like kinase 3/Dual specificity protein kinase CLK3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4226] [GtoPdb: 1992] [UniProtKB: P49761]
ChEMBL Inhibition of recombinant human CLK3 expressed in Sf9 insect cells incubated for 60 mins in presence of ATP and [gamma33-P] ATP by radiometric scintillation counter analysis B 7.92 pIC50 11.9 nM IC50 J Med Chem (2023) 66: 4106-4130 [PMID:36876904]
CDC like kinase 4/Dual specificity protein kinase CLK4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4203] [GtoPdb: 1993] [UniProtKB: Q9HAZ1]
ChEMBL Inhibition of recombinant human CLK4 expressed in Sf9 insect cells incubated for 60 mins in presence of ATP and [gamma33-P] ATP by radiometric scintillation counter analysis B 8.16 pIC50 6.9 nM IC50 J Med Chem (2023) 66: 4106-4130 [PMID:36876904]
dual specificity tyrosine phosphorylation regulated kinase 1A/Dual-specificity tyrosine-phosphorylation regulated kinase 1A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2292] [GtoPdb: 2009] [UniProtKB: Q13627]
ChEMBL Binding affinity to human DYRK1A assessed as equilibrium dissociation constant measured upto 240 min by TR-FRET assay B 10.05 pKd 0.09 nM Kd J Med Chem (2023) 66: 4106-4130 [PMID:36876904]
ChEMBL Inhibition of recombinant human DYRK1A expressed in Escherichia coli using DYRKtide peptide as substrate incubated for 110 mins in presence of ATP by non-radioactive ADP-Glo luminescence microplate reader assay B 8.15 pIC50 7 nM IC50 J Med Chem (2023) 66: 4106-4130 [PMID:36876904]
ChEMBL Inhibition of recombinant human DYRK1A expressed in Sf9 insect cells incubated for 60 mins in presence of ATP and [gamma33-P] ATP by radiometric scintillation counter analysis B 8.2 pIC50 6.3 nM IC50 J Med Chem (2023) 66: 4106-4130 [PMID:36876904]
dual specificity tyrosine phosphorylation regulated kinase 1B/Dual specificity tyrosine-phosphorylation-regulated kinase 1B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5543] [GtoPdb: 2010] [UniProtKB: Q9Y463]
ChEMBL Inhibition of recombinant human DYRK1B expressed in Sf9 insect cells incubated for 60 mins in presence of ATP and [gamma33-P] ATP by radiometric scintillation counter analysis B 8.43 pIC50 3.7 nM IC50 J Med Chem (2023) 66: 4106-4130 [PMID:36876904]
ChEMBL Inhibition of recombinant human DYRK1B expressed in Sf9 insect cells using DYRKtide peptide as substrate incubated for 110 mins in presence of ATP by non-radioactive ADP-Glo luminescence microplate reader assay B 8.47 pIC50 3.4 nM IC50 J Med Chem (2023) 66: 4106-4130 [PMID:36876904]
dual specificity tyrosine phosphorylation regulated kinase 2/Dual-specificity tyrosine-phosphorylation regulated kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4376] [GtoPdb: 2011] [UniProtKB: Q92630]
ChEMBL Inhibition of recombinant human DYRK2 expressed in Sf9 insect cells incubated for 60 mins in presence of ATP and [gamma33-P] ATP by radiometric scintillation counter analysis B 6.93 pIC50 117.6 nM IC50 J Med Chem (2023) 66: 4106-4130 [PMID:36876904]
dual specificity tyrosine phosphorylation regulated kinase 3/Dual-specificity tyrosine-phosphorylation regulated kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4575] [GtoPdb: 2012] [UniProtKB: O43781]
ChEMBL Inhibition of recombinant human DYRK3 expressed in Sf9 insect cells incubated for 60 mins in presence of ATP and [gamma33-P] ATP by radiometric scintillation counter analysis B 7.98 pIC50 10.4 nM IC50 J Med Chem (2023) 66: 4106-4130 [PMID:36876904]
dual specificity tyrosine phosphorylation regulated kinase 4/Dual specificity tyrosine-phosphorylation-regulated kinase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075115] [GtoPdb: 2013] [UniProtKB: Q9NR20]
ChEMBL Inhibition of recombinant human DYRK4 expressed in Sf9 insect cells incubated for 60 mins in presence of ATP and [gamma33-P] ATP by radiometric scintillation counter analysis B 5.59 pIC50 2589 nM IC50 J Med Chem (2023) 66: 4106-4130 [PMID:36876904]
CDC like kinase 1/Dual specificty protein kinase CLK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4224] [GtoPdb: 1990] [UniProtKB: P49759]
ChEMBL Binding affinity to human CLK1 assessed as equilibrium dissociation constant measured upto 240 min by TR-FRET assay B 10.25 pKd 0.06 nM Kd J Med Chem (2023) 66: 4106-4130 [PMID:36876904]
ChEMBL Inhibition of recombinant human CLK1 expressed in Sf9 insect cells using myelin basic protein as substrate incubated for 110 mins in presence of ATP by non-radioactive ADP-Glo luminescence microplate reader assay B 7.51 pIC50 30.8 nM IC50 J Med Chem (2023) 66: 4106-4130 [PMID:36876904]
ChEMBL Inhibition of recombinant human CLK1 expressed in Sf9 insect cells incubated for 60 mins in presence of ATP and [gamma33-P] ATP by radiometric scintillation counter analysis B 7.73 pIC50 18.8 nM IC50 J Med Chem (2023) 66: 4106-4130 [PMID:36876904]
glycogen synthase kinase 3 beta/Glycogen synthase kinase-3 beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL262] [GtoPdb: 2030] [UniProtKB: P49841]
ChEMBL Binding affinity to human GSK-3beta assessed as equilibrium dissociation constant measured upto 240 min by TR-FRET assay B 8.41 pKd 3.93 nM Kd J Med Chem (2023) 66: 4106-4130 [PMID:36876904]
ChEMBL Inhibition of recombinant human GSK-3beta expressed in Sf9 insect cells incubated for 60 mins in presence of ATP and [gamma33-P] ATP by radiometric scintillation counter analysis B 7.75 pIC50 17.6 nM IC50 J Med Chem (2023) 66: 4106-4130 [PMID:36876904]
phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha/PI3-kinase p110-alpha subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4005] [GtoPdb: 2153] [UniProtKB: P42336]
ChEMBL Inhibition of human recombinant p110alpha B 8.11 pIC50 7.8 nM IC50 Bioorg Med Chem (2007) 15: 7677-7687 [PMID:17869522]
ChEMBL Inhibition of PI3K alpha (unknown origin) B 8.24 pIC50 5.8 nM IC50 J Med Chem (2022) 65: 893-921 [PMID:33539089]
GtoPdb - - 8.24 pIC50 5.8 nM IC50 Cell (2006) 125: 733-47 [PMID:16647110]
ChEMBL Inhibition of PI3Kalpha (unknown origin) by radiometric assay B 9.3 pIC50 0.5 nM IC50 Bioorg Med Chem (2015) 23: 6280-6296 [PMID:26349627]
ChEMBL Inhibition of PI3Kalpha (unknown origin) B 9.3 pIC50 0.5 nM IC50 J Med Chem (2016) 59: 8667-8684 [PMID:27171036]
GtoPdb - - 9.52 pIC50 0.3 nM IC50 Bioorg Med Chem (2007) 15: 5837-44 [PMID:17601739]
phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit beta/PI3-kinase p110-beta subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3145] [GtoPdb: 2154] [UniProtKB: P42338]
GtoPdb - - 5.89 pIC50 1300 nM IC50 Cell (2006) 125: 733-47 [PMID:16647110]
GtoPdb - - 6.07 pIC50 850 nM IC50 Bioorg Med Chem (2007) 15: 5837-44 [PMID:17601739]
ChEMBL Inhibition of human recombinant p110beta B 6.47 pIC50 340 nM IC50 Bioorg Med Chem (2007) 15: 7677-7687 [PMID:17869522]
phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit delta/PI3-kinase p110-delta subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3130] [GtoPdb: 2155] [UniProtKB: O00329]
ChEMBL Inhibition of human recombinant p110delta B 6.04 pIC50 910 nM IC50 Bioorg Med Chem (2007) 15: 7677-7687 [PMID:17869522]
GtoPdb - - 6.29 pIC50 510 nM IC50 Cell (2006) 125: 733-47 [PMID:16647110]
fms related receptor tyrosine kinase 3/Tyrosine-protein kinase receptor FLT3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888]
ChEMBL Inhibition of FLT3 (unknown origin) using biotin-Glu-Gly-Pro-Trp-Leu-Glu-Glu-Glu-Glu-Glu-Ala-Tyr-Gly-Trp-Met-Asp-Phe-NH2 as substrate after 90 mins by luminescence assay B 8.29 pIC50 5.15 nM IC50 Bioorg Med Chem (2015) 23: 6280-6296 [PMID:26349627]
phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma in Human [GtoPdb: 2156] [UniProtKB: P48736]
GtoPdb - - 7.12 pIC50 76 nM IC50 Cell (2006) 125: 733-47 [PMID:16647110]
GtoPdb - - 7.4 pIC50 40 nM IC50 Bioorg Med Chem (2007) 15: 5837-44 [PMID:17601739]
protein kinase, DNA-activated, catalytic subunit in Human [GtoPdb: 2800] [UniProtKB: P78527]
GtoPdb - - 8.7 pIC50 2 nM IC50 Cell (2006) 125: 733-47 [PMID:16647110]

ChEMBL data shown on this page come from version 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]