PIK-75 [Ligand Id: 8012] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL393525 |
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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: O60563, P50750] | ||||||||
| 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: Q00535, Q15078] | ||||||||
| 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 1/Dual specificity 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] |
| 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] |
| 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] |
| ChEMBL | Inhibition of GSK-3beta (unknown origin) expressed in Sf9 cells by spectrometry based analysis | B | 8 | pIC50 | 10 | nM | IC50 | Bioorg Med Chem (2023) 92: 117406-117406 [PMID:37536264] |
| 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]
