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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  • phosphatidylinositol 3-kinase catalytic subunit type 3/Phosphatidylinositol 3-kinase catalytic subunit type 3 in Human [ChEMBL: CHEMBL1075165] [GtoPdb: 2152] [UniProtKB: Q8NEB9]
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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: 2503, 2153] [UniProtKB: P27986, P42336]
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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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  • phosphatidylinositol 4-kinase alpha/PI4-kinase alpha subunit in Human [ChEMBL: CHEMBL3667] [GtoPdb: 2148] [UniProtKB: P42356]
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  • phosphatidylinositol 4-kinase beta/PI4-kinase beta subunit in Human [ChEMBL: CHEMBL3268] [GtoPdb: 2149] [UniProtKB: Q9UBF8]
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  • phosphatidylinositol 4-kinase type 2 alpha/PI4-kinase type II in Human [ChEMBL: CHEMBL2251] [GtoPdb: 2498] [UniProtKB: Q9BTU6]
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  • mechanistic target of rapamycin kinase/Serine/threonine-protein kinase mTOR in Human [ChEMBL: CHEMBL2842] [GtoPdb: 2109] [UniProtKB: P42345]
  • mechanistic target of rapamycin kinase/Serine/threonine-protein kinase mTOR in Rat [ChEMBL: CHEMBL1075134] [GtoPdb: 2109] [UniProtKB: P42346]
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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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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]
phosphatidylinositol 3-kinase catalytic subunit type 3/Phosphatidylinositol 3-kinase catalytic subunit type 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075165] [GtoPdb: 2152] [UniProtKB: Q8NEB9]
ChEMBL Inhibition of VPS34 (unknown origin) B 8.38 pIC50 4.2 nM IC50 Eur J Med Chem (2022) 244: 114846-114846 [PMID:36283182]
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: 2503, 2153] [UniProtKB: P27986, P42336]
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 human full-length recombinant p110alpha/p85alpha co-expressed in baculovirus expression system using PIP2:PS lipid as substrate incubated for 1 hr in presence of ATP by ADP-Glo assay B 8 pIC50 10.1 nM IC50 J Med Chem (2018) 61: 1552-1575 [PMID:29360358]
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]
phosphatidylinositol 4-kinase alpha/PI4-kinase alpha subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3667] [GtoPdb: 2148] [UniProtKB: P42356]
ChEMBL Inhibition of PI4KA catalytic domain (unknown origin) assessed as enzyme residual activity incubated for 60 mins using ATP as substrate by ATP-Glo luminescent assay B 6.55 pIC50 280 nM IC50 Bioorg Med Chem Lett (2022) 76: 129010-129010 [PMID:36184029]
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/PI4-kinase beta subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3268] [GtoPdb: 2149] [UniProtKB: Q9UBF8]
ChEMBL Inhibition of PI4KB catalytic domain (unknown origin) assessed as enzyme residual activity incubated for 60 mins using ATP as substrate by ATP-Glo luminescent assay B 6.36 pIC50 440 nM IC50 Bioorg Med Chem Lett (2022) 76: 129010-129010 [PMID:36184029]
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 type 2 alpha/PI4-kinase type II in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2251] [GtoPdb: 2498] [UniProtKB: Q9BTU6]
ChEMBL Inhibition of PI4K2A catalytic domain (unknown origin) assessed as enzyme residual activity incubated for 60 mins using ATP as substrate by ATP-Glo luminescent assay B 4.52 pIC50 >30000 nM IC50 Bioorg Med Chem Lett (2022) 76: 129010-129010 [PMID:36184029]
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]
mechanistic target of rapamycin kinase/Serine/threonine-protein kinase mTOR in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075134] [GtoPdb: 2109] [UniProtKB: P42346]
ChEMBL Inhibition of mTOR in rat brain by [3H]-thymidine incorporation based immunoblot assay B 6.52 pIC50 300 nM IC50 Eur J Med Chem (2020) 208: 112820-112820 [PMID:32966896]
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]

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]