wortmannin [Ligand Id: 6060] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL428496 (Wortmannin)
  • protein kinase, DNA-activated, catalytic subunit/DNA-dependent protein kinase in Human [ChEMBL: CHEMBL3142] [GtoPdb: 2800] [UniProtKB: P78527]
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  • Myosin light chain kinase, smooth muscle in Chicken [ChEMBL: CHEMBL3062] [UniProtKB: P11799]
  • myosin light chain kinase/Myosin light chain kinase, smooth muscle in Human [ChEMBL: CHEMBL2428] [GtoPdb: 1552] [UniProtKB: Q15746]
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  • phosphoinositide-3-kinase regulatory subunit 1/phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha/PI3-kinase p110-alpha/p85-alpha in Human [ChEMBL: CHEMBL2111367] [GtoPdb: 25032153] [UniProtKB: P27986P42336]
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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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  • phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma/PI3-kinase p110-gamma subunit in Human [ChEMBL: CHEMBL3267] [GtoPdb: 2156] [UniProtKB: P48736]
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  • mechanistic target of rapamycin kinase/Serine/threonine-protein kinase mTOR in Human [ChEMBL: CHEMBL2842] [GtoPdb: 2109] [UniProtKB: P42345]
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  • polo like kinase 1/Serine/threonine-protein kinase PLK1 in Human [ChEMBL: CHEMBL3024] [GtoPdb: 2168] [UniProtKB: P53350]
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  • polo like kinase 3/Serine/threonine-protein kinase PLK3 in Human [ChEMBL: CHEMBL4897] [GtoPdb: 2170] [UniProtKB: Q9H4B4]
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  • phosphatidylinositol 4-kinase alpha in Human [GtoPdb: 2148] [UniProtKB: P42356]
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  • phosphatidylinositol 4-kinase beta in Human [GtoPdb: 2149] [UniProtKB: Q9UBF8]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
protein kinase, DNA-activated, catalytic subunit/DNA-dependent protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3142] [GtoPdb: 2800] [UniProtKB: P78527]
GtoPdb - - 6.92 pKi 120 nM Ki Bioorg Med Chem Lett (2012) 22: 5352-9 [PMID:22835870]
ChEMBL Binding affinity for DNA dependent protein kinase isolated from HeLa cells; Range is 20-120 B 6.92 pKi 120 nM Ki J. Med. Chem. (2005) 48: 569-585 [PMID:15658870]
ChEMBL Inhibition of DNA-PK isolated from human HeLa cell extract B 6.92 pKi 120 nM Ki Bioorg. Med. Chem. Lett. (2012) 22: 5352-5359 [PMID:22835870]
Myosin light chain kinase, smooth muscle in Chicken (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3062] [UniProtKB: P11799]
ChEMBL Inhibition of chicken SmMLCK expressed in Escherichia coli B 6.59 pIC50 260 nM IC50 Biochem. J. (2000) 351: 95-105 [PMID:10998351]
myosin light chain kinase/Myosin light chain kinase, smooth muscle in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2428] [GtoPdb: 1552] [UniProtKB: Q15746]
ChEMBL Inhibition of SmMLCK in the presence of 50uM ATP B 5.3 pIC50 5000 nM IC50 Biochem. J. (2007) 408: 297-315 [PMID:17850214]
ChEMBL Inhibition of Smooth muscle myosin light chain kinase (mMLCK) B 5.72 pIC50 1900 nM IC50 J. Med. Chem. (2003) 46: 1478-1483 [PMID:12672248]
ChEMBL Inhibition of MLCK by HTRF assay B 6.77 pIC50 170 nM IC50 Bioorg. Med. Chem. (2011) 19: 429-439 [PMID:21130659]
phosphoinositide-3-kinase regulatory subunit 1/phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha/PI3-kinase p110-alpha/p85-alpha in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111367] [GtoPdb: 25032153] [UniProtKB: P27986P42336]
GtoPdb - - 8.27 pKd 5.4 nM Kd J Med Chem (2018) 61: 10463-10472 [PMID:30380865]
GtoPdb - - 6.92 pKi 120 nM Ki J Med Chem (2005) 48: 569-85 [PMID:15658870]
ChEMBL Inhibition of PI3K p110alpha/p85alpha (unknown origin) by ADP-Glo assay B 5.79 pIC50 1610 nM IC50 Eur. J. Med. Chem. (2013) 60: 187-198 [PMID:23291120]
ChEMBL Inhibition of human recombinant P110alpha/p85alpha using phosphatidyl inositol as substrate after 1 hr by ADP-Glo Kinase assay B 7.92 pIC50 11.9 nM IC50 Bioorg. Med. Chem. Lett. (2012) 22: 6919-6922 [PMID:23040731]
ChEMBL Inhibition of PI3 kinase p110alpha/p85-alpha complex B 8.92 pIC50 1.2 nM IC50 Bioorg. Med. Chem. Lett. (2006) 16: 2518-2521 [PMID:16464575]
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 Binding affinity to human PI3Kalpha after 1 hr by KINOMEscan assay B 8.27 pKd 5.4 nM Kd J Med Chem (2018) 61: 10463-10472 [PMID:30380865]
GtoPdb - - 8.27 pKd 5.4 nM Kd J Med Chem (2018) 61: 10463-10472 [PMID:30380865]
GtoPdb - - 6.92 pKi 120 nM Ki J Med Chem (2005) 48: 569-85 [PMID:15658870]
ChEMBL Binding affinity for Phosphatidylinositol 3-kinase isolated from HeLa cells; Range is 20-120 B 6.92 pKi 120 nM Ki J. Med. Chem. (2005) 48: 569-585 [PMID:15658870]
ChEMBL Inhibition of PI3K p110alpha (unknown origin) using PIP2 as substrate preincubated for 10 mins followed by substrate addition measured after 1 hr B 6 pIC50 >=1000 nM IC50 Bioorg Med Chem Lett (2017) 27: 2510-2514 [PMID:28462836]
ChEMBL Inhibition of PI3K by fluorescence energy transfer assay B 7.75 pIC50 17.6 nM IC50 J. Med. Chem. (2008) 51: 4699-4707 [PMID:18630894]
ChEMBL Inhibition of human p110alpha PI3K fragment by AlphaScreen assay B 7.89 pIC50 13 nM IC50 Bioorg. Med. Chem. Lett. (2011) 21: 829-835 [PMID:21169017]
ChEMBL Inhibition of human PI3Kalpha expressed in Sf9 cells by fluorescent polarization assay B 7.92 pIC50 12 nM IC50 J. Med. Chem. (2010) 53: 8523-8533 [PMID:21121631]
ChEMBL Inhibition of PI3Kalpha (unknown origin) by fluorescent polarization assay B 7.92 pIC50 12 nM IC50 MedChemComm (2012) 3: 1337-1355
ChEMBL Inhibition of PI3 kinase B 7.92 pIC50 12 nM IC50 Bioorg. Med. Chem. Lett. (2009) 19: 4223-4227 [PMID:19523825]
ChEMBL Inhibition of human PI3Kalpha B 9 pIC50 1 nM IC50 J. Med. Chem. (2006) 49: 3857-3871 [PMID:16789742]
ChEMBL Inhibition of PI3Kalpha B 9 pIC50 1 nM IC50 J. Med. Chem. (2012) 55: 8559-8581 [PMID:22924688]
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]
ChEMBL Binding affinity to human PI3Kbeta after 1 hr by KINOMEscan assay B 8.12 pKd 7.6 nM Kd J Med Chem (2018) 61: 10463-10472 [PMID:30380865]
GtoPdb - - 8.12 pKd 7.6 nM Kd J Med Chem (2018) 61: 10463-10472 [PMID:30380865]
ChEMBL Inhibition of human PI3K p110beta catalytic subunit by AlphaScreen competition assay B 7.82 pIC50 15 nM IC50 Bioorg. Med. Chem. Lett. (2011) 21: 829-835 [PMID:21169017]
ChEMBL Inhibition of PI3Kbeta B 7.85 pIC50 14 nM IC50 J. Med. Chem. (2012) 55: 8559-8581 [PMID:22924688]
ChEMBL Inhibition of human PI3Kbeta B 8 pIC50 10 nM IC50 J. Med. Chem. (2006) 49: 3857-3871 [PMID:16789742]
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 Binding affinity to human PI3Kdelta after 1 hr by KINOMEscan assay B 8.26 pKd 5.5 nM Kd J Med Chem (2018) 61: 10463-10472 [PMID:30380865]
GtoPdb - - 8.26 pKd 5.5 nM Kd J Med Chem (2018) 61: 10463-10472 [PMID:30380865]
ChEMBL Inhibition of human PI3Kdelta B 8.05 pIC50 9 nM IC50 J. Med. Chem. (2006) 49: 3857-3871 [PMID:16789742]
ChEMBL Inhibition of PI3Kdelta B 8.05 pIC50 9 nM IC50 J. Med. Chem. (2012) 55: 8559-8581 [PMID:22924688]
ChEMBL Inhibition of human PI3K p110delta catalytic subunit by AlphaScreen assay B 8.4 pIC50 4 nM IC50 Bioorg. Med. Chem. Lett. (2011) 21: 829-835 [PMID:21169017]
phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma/PI3-kinase p110-gamma subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3267] [GtoPdb: 2156] [UniProtKB: P48736]
GtoPdb - - 7.82 pKd 15 nM Kd J Med Chem (2018) 61: 10463-10472 [PMID:30380865]
ChEMBL Binding affinity to human PI3Kgamma after 1 hr by KINOMEscan assay B 7.82 pKd 15 nM Kd J Med Chem (2018) 61: 10463-10472 [PMID:30380865]
ChEMBL Inhibition of PI3Kgamma (unknown origin) assessed as decrease in fluorescence intensity using phosphorylated substrate B 4.26 pIC50 55000 nM IC50 Eur. J. Med. Chem. (2014) 84: 454-465 [PMID:25050878]
ChEMBL Inhibition of human PI3K p110gamma catalytic subunit by AlphaScreen assay B 7.05 pIC50 89 nM IC50 Bioorg. Med. Chem. Lett. (2011) 21: 829-835 [PMID:21169017]
ChEMBL Inhibition of PI3Kgamma assessed as inhibition of 32P-PIP3 formation B 7.72 pIC50 19 nM IC50 Bioorg. Med. Chem. Lett. (2007) 17: 756-760 [PMID:17095227]
ChEMBL Inhibition of human PI3Kgamma B 8.3 pIC50 5 nM IC50 J. Med. Chem. (2006) 49: 3857-3871 [PMID:16789742]
ChEMBL Inhibition of PI3Kgamma B 8.3 pIC50 5 nM IC50 J. Med. Chem. (2012) 55: 8559-8581 [PMID:22924688]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL Antiplasmodial activity against Plasmodium falciparum 3D7 after 72 hrs by SYBR green assay F 4.9 pIC50 12589.25 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum Dd2 after 72 hrs by SYBR green assay F 4.9 pIC50 12589.25 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by SYBR green assay F 4.9 pIC50 12589.25 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR green assay F 5 pIC50 10000 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay F 5 pIC50 10000 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
mechanistic target of rapamycin kinase/Serine/threonine-protein kinase mTOR in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2842] [GtoPdb: 2109] [UniProtKB: P42345]
ChEMBL Binding affinity to human mTOR after 1 hr by KINOMEscan assay B 5.04 pKd 9200 nM Kd J Med Chem (2018) 61: 10463-10472 [PMID:30380865]
GtoPdb - - 5.04 pKd 9200 nM Kd J Med Chem (2018) 61: 10463-10472 [PMID:30380865]
ChEMBL Inhibitory activity against MTOR B 7.4 pIC50 40 nM IC50 Bioorg. Med. Chem. Lett. (2005) 15: 4799-4802 [PMID:16143526]
polo like kinase 1/Serine/threonine-protein kinase PLK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3024] [GtoPdb: 2168] [UniProtKB: P53350]
ChEMBL Inhibition of PLK1 in the presence of 5uM ATP B 5.89 pIC50 1300 nM IC50 Biochem. J. (2007) 408: 297-315 [PMID:17850214]
ChEMBL Inhibition of GST-tagged Plk1 using recombinant protein X as a substrate containing threonine residues B 7.62 pIC50 24 nM IC50 J. Med. Chem. (2012) 55: 6243-6262 [PMID:22621397]
ChEMBL Inhibition of AX-7503 binding to recombinant Plk1 by Western blot B 8.24 pIC50 5.8 nM IC50 J. Biol. Chem. (2007) 282: 2505-2511 [PMID:17135248]
polo like kinase 3/Serine/threonine-protein kinase PLK3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4897] [GtoPdb: 2170] [UniProtKB: Q9H4B4]
ChEMBL Inhibition of Plk3 in human A549 cells assessed as casein substrate phosphorylation by Western blot B 6.66 pIC50 220 nM IC50 J. Biol. Chem. (2007) 282: 2505-2511 [PMID:17135248]
ChEMBL Inhibition of AX-7503 binding to recombinant Plk3 expressed in HeLa cells by Western blot B 7.31 pIC50 49 nM IC50 J. Biol. Chem. (2007) 282: 2505-2511 [PMID:17135248]
ChEMBL Inhibition of recombinant Plk3 assessed as casein substrate phosphorylation B 7.32 pIC50 48 nM IC50 J. Biol. Chem. (2007) 282: 2505-2511 [PMID:17135248]
phosphatidylinositol 4-kinase alpha in Human [GtoPdb: 2148] [UniProtKB: P42356]
GtoPdb - - 6.8 pIC50 - - - J Biol Chem (1997) 272: 4384-90 [PMID:9020160];
Biochim Biophys Acta (1999) 1437: 341-56 [PMID:10101268]
phosphatidylinositol 4-kinase beta in Human [GtoPdb: 2149] [UniProtKB: Q9UBF8]
GtoPdb - - 6.8 pIC50 - - - J Biol Chem (1997) 272: 4384-90 [PMID:9020160];
Biochim Biophys Acta (1999) 1437: 341-56 [PMID:10101268]

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]