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

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ChEMBL ligand: CHEMBL393525
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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 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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  • 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
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 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]
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]
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 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]