dactolisib [Ligand Id: 7950] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1879463 (NVP-BEZ235-NX, Dactolisib, NVP-BEZ235, BEZ235, BEZ-235, Bez-235)
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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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  • phosphatidylinositol-4-phosphate 3-kinase catalytic subunit type 2 beta/Phosphatidylinositol-4-phosphate 3-kinase C2 domain-containing beta polypeptide in Human [ChEMBL: CHEMBL5554] [GtoPdb: 2151] [UniProtKB: O00750]
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  • phosphatidylinositol-4-phosphate 3-kinase catalytic subunit type 2 alpha/Phosphatidylinositol-4-phosphate 3-kinase C2 domain-containing subunit alpha in Human [ChEMBL: CHEMBL1075102] [GtoPdb: 2150] [UniProtKB: O00443]
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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/phosphoinositide-3-kinase regulatory subunit 1/PI3-kinase p110-delta/p85-alpha in Human [ChEMBL: CHEMBL2111432] [GtoPdb: 21552503] [UniProtKB: O00329P27986]
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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-4,5-bisphosphate 3-kinase catalytic subunit gamma/phosphoinositide-3-kinase regulatory subunit 5/PI3-kinase subunit gamma/Phosphoinositide 3-kinase regulatory subunit 5 in Human [ChEMBL: CHEMBL3430881] [GtoPdb: 21562506] [UniProtKB: P48736Q8WYR1]
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  • phosphoinositide-3-kinase regulatory subunit 1/phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit beta/PI3K p110 beta/p85 alpha in Human [ChEMBL: CHEMBL3038510] [GtoPdb: 25032154] [UniProtKB: P27986P42338]
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  • ATM serine/threonine kinase/Serine-protein kinase ATM in Human [ChEMBL: CHEMBL3797] [GtoPdb: 1934] [UniProtKB: Q13315]
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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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  • Janus kinase 3/Tyrosine-protein kinase JAK3 in Human [ChEMBL: CHEMBL2148] [GtoPdb: 2049] [UniProtKB: P52333]
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  • ATR serine/threonine kinase in Human [GtoPdb: 1935] [UniProtKB: Q13535]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
mechanistic target of rapamycin kinase/mTORC1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL4296661] [GtoPdb: 2109] [UniProtKB: P42345Q8N122Q9BVC4]
ChEMBL Inhibition of mTORC1 (unknown origin) incubated for 40 mins by luciferase based ATP depletion assay B 7.36 pIC50 44 nM IC50 Bioorg. Med. Chem. (2015) 23: 6477-6485 [PMID:26321603]
GtoPdb Measured as inhibition of downstream mTOR activated p70S6K - 8.22 pIC50 6 nM IC50 Mol Cancer Ther (2008) 7: 1851-63 [PMID:18606717]
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 human recombinant Vps34 using substrate PI incubated for 1 hr by Adapta kinase assay B 6.35 pIC50 450 nM IC50 J Med Chem (2017) 60: 47-65 [PMID:27644332]
phosphatidylinositol-4-phosphate 3-kinase catalytic subunit type 2 beta/Phosphatidylinositol-4-phosphate 3-kinase C2 domain-containing beta polypeptide in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5554] [GtoPdb: 2151] [UniProtKB: O00750]
ChEMBL Inhibition of human recombinant PI3KC2beta using substrate PI incubated for 1 hr by Adapta kinase assay B 7.36 pIC50 44 nM IC50 J Med Chem (2017) 60: 47-65 [PMID:27644332]
phosphatidylinositol-4-phosphate 3-kinase catalytic subunit type 2 alpha/Phosphatidylinositol-4-phosphate 3-kinase C2 domain-containing subunit alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075102] [GtoPdb: 2150] [UniProtKB: O00443]
ChEMBL Inhibition of human recombinant PI3KC2alpha using substrate PI incubated for 1 hr by Adapta kinase assay B 7.47 pIC50 34 nM IC50 J Med Chem (2017) 60: 47-65 [PMID:27644332]
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]
ChEMBL Inhibition of P110alpha/p85alpha (unknown origin) using L-alpha-phosphatidylinositol as substrate after 40 mins by ATP depletion assay B 7.05 pIC50 89 nM IC50 Bioorg Med Chem (2015) 23: 7765-7776 [PMID:26652969]
ChEMBL Inhibition of p110alpha/p85alpha (unknown origin) incubated for 40 mins by luciferase based ATP depletion assay B 7.31 pIC50 49 nM IC50 Bioorg. Med. Chem. (2015) 23: 6477-6485 [PMID:26321603]
ChEMBL Inhibition of PI3K p110alpha/p85alpha (unknown origin) using PIP2 as substrate after 1 hr by luminescent kinase-Glo assay B 7.45 pIC50 35.15 nM IC50 Eur J Med Chem (2017) 127: 509-520 [PMID:28109945]
ChEMBL Inhibition of recombinant N-terminal His6-tagged full length PI3K p110alpha (unknown origin)/recombinant untagged full length p85alpha (unknown origin) expressed in baculovirus infected Sf21 insect cells by ELISA B 7.79 pIC50 16.4 nM IC50 Bioorg Med Chem (2018) 26: 1675-1685 [PMID:29475582]
ChEMBL Inhibition of PI3Kalpha/p85 iSH2 domain (unknown origin) expressed in baculovirus using l-alpha-phosphatidylinositol as substrate after 60 mins by kinase-glo assay B 8.4 pIC50 4 nM IC50 Eur J Med Chem (2016) 122: 731-743 [PMID:27479483]
GtoPdb - - 8.4 pIC50 4 nM IC50 Mol Cancer Ther (2008) 7: 1851-63 [PMID:18606717]
ChEMBL Inhibition of recombinant full length PI3K p110alpha/p85alpha (unknown origin) expressed in baculovirus infected sf9 cells using PIP2 as substrate preincubated for 10 mins followed by ATP addition and measured after 45 mins by HTRF assay B 7.4 pEC50 40 nM EC50 Eur J Med Chem (2018) 157: 37-49 [PMID:30071408]
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 PI3Kalpha (unknown origin) assessed as reduction in ATP depletion using lipid substrate after 40 mins by Kinase-Glo luminescent assay B 7.05 pIC50 89 nM IC50 Bioorg Med Chem Lett (2016) 26: 4408-4413 [PMID:27544401]
ChEMBL Inhibition of PI3Kalpha (unknown origin) assessed as reduction of ATP level after 40 mins by luciferase based luminescence assay B 7.27 pIC50 54 nM IC50 Bioorg. Med. Chem. (2015) 23: 5662-5671 [PMID:26210161]
ChEMBL Inhibition of human recombinant PI3Kalpha using PIP2 as substrate after 1 hr by Kinase-Glo luminescent assay B 7.46 pIC50 35 nM IC50 MedChemComm (2016) 7: 297-310
ChEMBL PIK3alpha Activity Assay: 1. Preparation of test reagents{circle around (1)} 1x kinase buffer (50 mM HEPES, pH 7.5, 3 mM MgCl2, 1 mM EGTA, 100 mM NaCl, 0.03% CHAPS, 2 mM DTT);{circle around (2)} 4x kinase solution (added PI3K a kinase to 1x kinase buffer to provide 4x kinase solution with a final concentration of 1.65 nM);{circle around (3)} 2x substrate solution (added the substrates of PIP2 and ATP into 1x kinase buffer to provide 2x substrate solution with PIP2 final concentration of 50 uM and ATP final concentration of 25 uM);{circle around (4)} 4x test substance solutions (100x test substance solutions with different concentration gradients were prepared using 100% DMSO, and diluted 25-fold with 1x kinase buffer to give 4x test substance solutions with different concentration gradients);{circle around (5)} Invitrogen's activity test kit with the test solution was kept stand to room temperature. 2. 2.5 uL of 4x test solution was added to a 384-well plate in parallel; 3. added 2.54 uL of 4x kinase solution and incubated for 10 min; 4. then added 5 uL of 2x solutions of PIP2 and ATP substrates and incubated for 1 h at room temperature; 5. finally, added 10 uL of test solution to quench the reaction, and read after 15 min; 6. IC50 value was obtained via curve fitting. Inhibition rate (%)=(sample value-minimum)/(maximum-minimum)x100. B 7.49 pIC50 32.5 nM IC50 US-9284315-B2. Three-ring PI3K and/or mTOR inhibitor (2016)
ChEMBL Inhibition of PI3Kalpha (unknown origin) using PIP2 as substrate measured after 1 hr by Kinase-Glo luminescent assay B 7.52 pIC50 30 nM IC50 Bioorg Med Chem (2018) 26: 3992-4000 [PMID:29945756]
ChEMBL Inhibition of human PI3K-alpha assessed as inhibition of Ptdlns(3,4,5)P3 phosphorylation after 1 hr by TR-FRET analysis B 7.7 pIC50 20 nM IC50 J. Med. Chem. (2014) 57: 4834-4848 [PMID:24805946]
ChEMBL Inhibition of recombinant PI3Kalpha (unknown origin) using phosphatidyl inositol as substrate after 30 to 60 mins in presence of ATP by Kinase Glo luminescence assay B 7.77 pIC50 17 nM IC50 ACS Med Chem Lett (2016) 7: 762-767 [PMID:27563400]
ChEMBL Inhibition of PI3K p110alpha (unknown origin) using PIP2 as substrate by ELISA B 7.79 pIC50 16.4 nM IC50 Eur J Med Chem (2018) 146: 460-470 [PMID:29407971]
ChEMBL Inhibition of recombinant human PI3K-alpha using PIP2:3PS as substrate preincubated for 15 mins followed by ATP addition measured after 1 hr by ADP-Glo assay B 7.79 pIC50 16.4 nM IC50 Bioorg Med Chem (2018) 26: 3982-3991 [PMID:29937355]
ChEMBL Inhibition of PI3Kalpha (unknown origin) using diC8-PI(4,5)P2 as substrate incubated for 3 hrs in presence of ATP by fluorescence polarization assay B 7.96 pIC50 11 nM IC50 Eur J Med Chem (2019) 182: 111630-111630 [PMID:31446244]
ChEMBL Inhibition of PI3Kalpha B 8 pIC50 <10 nM IC50 Bioorg. Med. Chem. Lett. (2012) 22: 6788-6793 [PMID:23063403]
ChEMBL Inhibition of PI3Kalpha (unknown origin) using substrate PI incubated for 1 hr by Adapta kinase assay B 8.15 pIC50 7 nM IC50 J Med Chem (2017) 60: 47-65 [PMID:27644332]
ChEMBL Inhibition of PI3Kalpha (unknown origin) using PIP2/PS as substrate after 1 hr by luciferase-based luminescence assay B 8.21 pIC50 6.2 nM IC50 ACS Med. Chem. Lett. (2015) 6: 434-438 [PMID:25893045]
ChEMBL Inhibition of PI3Kalpha (unknown origin) B 8.4 pIC50 4 nM IC50 Bioorg Med Chem (2018) 26: 4537-4543 [PMID:30077608]
ChEMBL Inhibition of PI3Kalpha (unknown origin) B 8.4 pIC50 4 nM IC50 MedChemComm (2012) 3: 1337-1355
GtoPdb - - 8.4 pIC50 4 nM IC50 Mol Cancer Ther (2008) 7: 1851-63 [PMID:18606717]
ChEMBL Inhibition of wild type PI3Kalpha (unknown origin) after 40 mins by kinase-Glo reagent based luminescence assay B 7.4 pEC50 40 nM EC50 Eur J Med Chem (2018) 158: 707-719 [PMID:30245395]
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 Inhibition of PI3Kbeta (unknown origin) assessed as reduction in ATP depletion using lipid substrate after 40 mins by Kinase-Glo luminescent assay B 6.38 pIC50 421 nM IC50 Bioorg Med Chem Lett (2016) 26: 4408-4413 [PMID:27544401]
ChEMBL Inhibition of PI3K beta (unknown origin) using lipid substrate measured after 40 mins in presence of ATP by Kinase-Glo plus reagent based luminescence assay B 6.38 pIC50 421 nM IC50 Bioorg Med Chem (2019) 27: 114930-114930 [PMID:31176568]
ChEMBL Inhibition of PI3Kbeta (unknown origin) assessed as reduction of ATP level after 40 mins by luciferase based luminescence assay B 6.4 pIC50 399 nM IC50 Bioorg. Med. Chem. (2015) 23: 5662-5671 [PMID:26210161]
ChEMBL Inhibition of human PI3K-beta assessed as inhibition of Ptdlns(3,4,5)P3 phosphorylation after 1 hr by TR-FRET analysis B 6.5 pIC50 316 nM IC50 J. Med. Chem. (2014) 57: 4834-4848 [PMID:24805946]
ChEMBL Inhibition of recombinant PI3Kbeta (unknown origin) using phosphatidyl inositol as substrate after 30 to 60 mins in presence of ATP by Kinase Glo luminescence assay B 6.72 pIC50 192 nM IC50 ACS Med Chem Lett (2016) 7: 762-767 [PMID:27563400]
ChEMBL Inhibition of human PI3Kbeta using PIP2 as substrate after 1 hr B 7.1 pIC50 79 nM IC50 Bioorg Med Chem Lett (2019) 29: 1313-1319 [PMID:30975623]
ChEMBL Inhibition of PI3Kbeta (unknown origin) expressed in baculovirus co-expressing p85 using l-alpha-phosphatidylinositol as substrate after 60 mins by kinase-glo assay B 7.12 pIC50 76 nM IC50 Eur J Med Chem (2016) 122: 731-743 [PMID:27479483]
ChEMBL Inhibition of PI3Kbeta (unknown origin) B 7.12 pIC50 75 nM IC50 MedChemComm (2012) 3: 1337-1355
ChEMBL Inhibition of PI3Kbeta (unknown origin) using diC8-PI(4,5)P2 as substrate incubated for 3 hrs in presence of ATP by fluorescence polarization assay B 7.19 pIC50 64 nM IC50 Eur J Med Chem (2019) 182: 111630-111630 [PMID:31446244]
ChEMBL Inhibition of recombinant human PI3K-beta using PIP2:3PS as substrate preincubated for 15 mins followed by ATP addition measured after 1 hr by ADP-Glo assay B 7.44 pIC50 35.9 nM IC50 Bioorg Med Chem (2018) 26: 3982-3991 [PMID:29937355]
ChEMBL Inhibition of PI3K p110beta (unknown origin) using PIP2 as substrate by ELISA B 7.44 pIC50 35.9 nM IC50 Eur J Med Chem (2018) 146: 460-470 [PMID:29407971]
ChEMBL Inhibition of PI3Kbeta B 8 pIC50 <10 nM IC50 Bioorg. Med. Chem. Lett. (2012) 22: 6788-6793 [PMID:23063403]
ChEMBL Inhibition of PI3Kbeta (unknown origin) B 8.22 pIC50 6 nM IC50 Bioorg Med Chem (2018) 26: 4537-4543 [PMID:30077608]
ChEMBL Inhibition of PI3Kbeta (unknown origin) after 40 mins by kinase-Glo reagent based luminescence assay B 7.82 pEC50 15 nM EC50 Eur J Med Chem (2018) 158: 707-719 [PMID:30245395]
phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit delta/phosphoinositide-3-kinase regulatory subunit 1/PI3-kinase p110-delta/p85-alpha in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111432] [GtoPdb: 21552503] [UniProtKB: O00329P27986]
ChEMBL Inhibition of P110delta/p85alpha (unknown origin) using L-alpha-phosphatidylinositol as substrate after 40 mins by ATP depletion assay B 6.69 pIC50 204 nM IC50 Bioorg Med Chem (2015) 23: 7765-7776 [PMID:26652969]
ChEMBL Inhibition of p110delta/p85alpha (unknown origin) incubated for 40 mins by luciferase based ATP depletion assay B 6.86 pIC50 138 nM IC50 Bioorg. Med. Chem. (2015) 23: 6477-6485 [PMID:26321603]
ChEMBL Inhibition of recombinant human full length N-terminal GST-tagged PI3Kalpha (1 to 1068 residues)/PIK3R1 (1 to 724 residues) expressed in baculovirus expression system using PIP2 as substrate incubated for 1 hr by ADP-Glo assay B 7.09 pIC50 80.5 nM IC50 Eur J Med Chem (2019) 178: 667-686 [PMID:31228810]
ChEMBL Inhibition of recombinant human full length N-terminal GST-tagged PI3Kdelta (1 to 1044 residues)/PIK3R1 (1 to 724 residues) expressed in baculovirus expression system using PIP2 as substrate incubated for 2 hrs by ADP-Glo assay B 7.1 pIC50 80 nM IC50 Eur J Med Chem (2019) 178: 667-686 [PMID:31228810]
ChEMBL Inhibition of recombinant N-terminal full length human PI3K p110delta/recombinant untagged full length human p85alpha expressed in baculovirus infected Sf21 insect cells by ELISA B 7.11 pIC50 78.4 nM IC50 Bioorg Med Chem (2018) 26: 1675-1685 [PMID:29475582]
ChEMBL Inhibition of recombinant human full length N-terminal His-tagged PI3K p110delta/p85alpha using lipid substrate after 60 mins by ADP-Glo assay B 7.66 pIC50 22 nM IC50 Bioorg Med Chem (2018) 26: 4537-4543 [PMID:30077608]
GtoPdb - - 8.15 pIC50 7 nM IC50 Mol Cancer Ther (2008) 7: 1851-63 [PMID:18606717]
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 PI3Kdelta (unknown origin) assessed as reduction in ATP depletion using lipid substrate after 40 mins by Kinase-Glo luminescent assay B 6.69 pIC50 204 nM IC50 Bioorg Med Chem Lett (2016) 26: 4408-4413 [PMID:27544401]
ChEMBL Inhibition of PI3K delta (unknown origin) using lipid substrate measured after 40 mins in presence of ATP by Kinase-Glo plus reagent based luminescence assay B 6.69 pIC50 204 nM IC50 Bioorg Med Chem (2019) 27: 114930-114930 [PMID:31176568]
ChEMBL Inhibition of PI3Kdelta (unknown origin) assessed as reduction of ATP level after 40 mins by luciferase based luminescence assay B 6.79 pIC50 164 nM IC50 Bioorg. Med. Chem. (2015) 23: 5662-5671 [PMID:26210161]
ChEMBL Inhibition of PI3K p110delta (unknown origin) using PIP2 as substrate after 1 hr by ADP-Glo kinase assay B 7.05 pIC50 89.06 nM IC50 Eur J Med Chem (2017) 127: 509-520 [PMID:28109945]
ChEMBL Inhibition of PI3K p110delta (unknown origin) using PIP2 as substrate by ELISA B 7.11 pIC50 78.4 nM IC50 Eur J Med Chem (2018) 146: 460-470 [PMID:29407971]
ChEMBL Inhibition of recombinant human PI3K-delta using PIP2:3PS as substrate preincubated for 15 mins followed by ATP addition measured after 1 hr by ADP-Glo assay B 7.11 pIC50 78.4 nM IC50 Bioorg Med Chem (2018) 26: 3982-3991 [PMID:29937355]
ChEMBL Inhibition of PI3Kdelta (unknown origin) assessed as reduction in ADP formation using phosphatidyl inositol as substrate after 30 to 60 mins by TR-FRET assay B 7.6 pIC50 25 nM IC50 ACS Med Chem Lett (2016) 7: 762-767 [PMID:27563400]
ChEMBL Inhibition of PI3Kdelta (unknown origin) by ADP-gloassay B 7.66 pIC50 22 nM IC50 Eur J Med Chem (2019) 164: 304-316 [PMID:30605829]
ChEMBL Inhibition of PI3Kdelta (unknown origin) using diC8-PI(4,5)P2 as substrate incubated for 3 hrs in presence of ATP by fluorescence polarization assay B 7.68 pIC50 21 nM IC50 Eur J Med Chem (2019) 182: 111630-111630 [PMID:31446244]
ChEMBL Inhibition of human PI3K-delta assessed as inhibition of Ptdlns(3,4,5)P3 phosphorylation after 1 hr by TR-FRET analysis B 7.89 pIC50 13 nM IC50 J. Med. Chem. (2014) 57: 4834-4848 [PMID:24805946]
ChEMBL Inhibition of PI3Kdelta B 8 pIC50 <10 nM IC50 Bioorg. Med. Chem. Lett. (2012) 22: 6788-6793 [PMID:23063403]
ChEMBL Inhibition of human PI3Kdelta using PIP2 as substrate after 1 hr B 8.1 pIC50 8 nM IC50 Bioorg Med Chem Lett (2019) 29: 1313-1319 [PMID:30975623]
GtoPdb - - 8.15 pIC50 7 nM IC50 Mol Cancer Ther (2008) 7: 1851-63 [PMID:18606717]
ChEMBL Inhibition of PI3Kdelta (unknown origin) B 8.15 pIC50 7 nM IC50 Bioorg Med Chem (2018) 26: 4537-4543 [PMID:30077608]
ChEMBL Inhibition of PI3Kdelta (unknown origin) B 8.15 pIC50 7 nM IC50 MedChemComm (2012) 3: 1337-1355
ChEMBL Inhibition of human PI3Kalpha using PIP2 as substrate after 1 hr B 8.3 pIC50 5 nM IC50 Bioorg Med Chem Lett (2019) 29: 1313-1319 [PMID:30975623]
ChEMBL Inhibition of PI3Kdelta (unknown origin) expressed in baculovirus co-expressing p85 using l-alpha-phosphatidylinositol as substrate after 120 mins by kinase-glo assay B 8.3 pIC50 5 nM IC50 Eur J Med Chem (2016) 122: 731-743 [PMID:27479483]
ChEMBL Inhibition of PI3Kdelta (unknown origin) after 40 mins by kinase-Glo reagent based luminescence assay B 7.03 pEC50 93 nM EC50 Eur J Med Chem (2018) 158: 707-719 [PMID:30245395]
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]
ChEMBL Inhibition of PI3Kgamma (unknown origin) assessed as reduction in ADP formation using phosphatidyl inositol as substrate after 30 to 60 mins by TR-FRET assay B 6.5 pIC50 313 nM IC50 ACS Med Chem Lett (2016) 7: 762-767 [PMID:27563400]
ChEMBL Inhibition of PI3Kgamma (unknown origin) assessed as reduction in ATP depletion using lipid substrate after 40 mins by Kinase-Glo luminescent assay B 6.77 pIC50 169 nM IC50 Bioorg Med Chem Lett (2016) 26: 4408-4413 [PMID:27544401]
ChEMBL Inhibition of PI3K gamma (unknown origin) using lipid substrate measured after 40 mins in presence of ATP by Kinase-Glo plus reagent based luminescence assay B 6.77 pIC50 169 nM IC50 Bioorg Med Chem (2019) 27: 114930-114930 [PMID:31176568]
ChEMBL Inhibition of recombinant human full length N-terminal DYKDDDDK-tagged PI3Kgamma (1 to 1102 residues) expressed in baculovirus expression system using PIP2 as substrate incubated for 2 hrs by ADP-Glo assay B 6.98 pIC50 104.2 nM IC50 Eur J Med Chem (2019) 178: 667-686 [PMID:31228810]
ChEMBL Inhibition of human PI3K-gamma assessed as inhibition of Ptdlns(3,4,5)P3 phosphorylation after 1 hr by TR-FRET analysis B 7 pIC50 100 nM IC50 J. Med. Chem. (2014) 57: 4834-4848 [PMID:24805946]
ChEMBL Inhibition of PI3Kgamma (unknown origin) assessed as reduction of ATP level after 40 mins by luciferase based luminescence assay B 7.02 pIC50 95 nM IC50 Bioorg. Med. Chem. (2015) 23: 5662-5671 [PMID:26210161]
ChEMBL Inhibition of PI3Kgamma (unknown origin) using diC8-PI(4,5)P2 as substrate incubated for 3 hrs in presence of ATP by fluorescence polarization assay B 7.57 pIC50 27 nM IC50 Eur J Med Chem (2019) 182: 111630-111630 [PMID:31446244]
ChEMBL Inhibition of recombinant full length His-tagged human PI3K p110gamma expressed in baculovirus expression system using PIP2 as substrate after 1 hr by ADP-Glo kinase assay B 7.59 pIC50 25.53 nM IC50 Eur J Med Chem (2017) 127: 509-520 [PMID:28109945]
ChEMBL Inhibition of recombinant human PI3K-gamma using PIP2:3PS as substrate preincubated for 15 mins followed by ATP addition measured after 1 hr by ADP-Glo assay B 7.63 pIC50 23.6 nM IC50 Bioorg Med Chem (2018) 26: 3982-3991 [PMID:29937355]
ChEMBL Inhibition of PI3K p110gamma (unknown origin) using PIP2 as substrate by ELISA B 7.63 pIC50 23.6 nM IC50 Eur J Med Chem (2018) 146: 460-470 [PMID:29407971]
ChEMBL Inhibition of recombinant human N-terminal His6-tagged full length PI3K p120gamma expressed in baculovirus infected Sf21 insect cells by ELISA B 7.63 pIC50 23.6 nM IC50 Bioorg Med Chem (2018) 26: 1675-1685 [PMID:29475582]
ChEMBL Inhibition of PI3Kgamma B 8 pIC50 <10 nM IC50 Bioorg. Med. Chem. Lett. (2012) 22: 6788-6793 [PMID:23063403]
ChEMBL Inhibition of PI3Kgamma (unknown origin) expressed in baculovirus co-expressing p85 using l-alpha-phosphatidylinositol as substrate after 120 mins by kinase-glo assay B 8.15 pIC50 7 nM IC50 Eur J Med Chem (2016) 122: 731-743 [PMID:27479483]
ChEMBL Inhibition of human PI3Kgamma using PIP2 as substrate after 1 hr B 8.22 pIC50 6 nM IC50 Bioorg Med Chem Lett (2019) 29: 1313-1319 [PMID:30975623]
GtoPdb - - 8.3 pIC50 5 nM IC50 Mol Cancer Ther (2008) 7: 1851-63 [PMID:18606717]
ChEMBL Inhibition of PI3Kgamma (unknown origin) B 8.3 pIC50 5 nM IC50 Bioorg Med Chem (2018) 26: 4537-4543 [PMID:30077608]
ChEMBL Inhibition of PI3Kgamma (unknown origin) B 8.3 pIC50 5 nM IC50 MedChemComm (2012) 3: 1337-1355
ChEMBL Inhibition of PI3Kgamma (unknown origin) after 40 mins by kinase-Glo reagent based luminescence assay B 7.17 pEC50 67 nM EC50 Eur J Med Chem (2018) 158: 707-719 [PMID:30245395]
phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma/phosphoinositide-3-kinase regulatory subunit 5/PI3-kinase subunit gamma/Phosphoinositide 3-kinase regulatory subunit 5 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3430881] [GtoPdb: 21562506] [UniProtKB: P48736Q8WYR1]
ChEMBL Inhibition of P110gamma/PIK3R5 (unknown origin) using L-alpha-phosphatidylinositol as substrate after 40 mins by ATP depletion assay B 6.77 pIC50 169 nM IC50 Bioorg Med Chem (2015) 23: 7765-7776 [PMID:26652969]
ChEMBL Inhibition of p110gamma/PIK3R5 (unknown origin) incubated for 40 mins by luciferase based ATP depletion assay B 7.14 pIC50 72 nM IC50 Bioorg. Med. Chem. (2015) 23: 6477-6485 [PMID:26321603]
GtoPdb - - 8.3 pIC50 5 nM IC50 Mol Cancer Ther (2008) 7: 1851-63 [PMID:18606717]
phosphoinositide-3-kinase regulatory subunit 1/phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit beta/PI3K p110 beta/p85 alpha in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3038510] [GtoPdb: 25032154] [UniProtKB: P27986P42338]
ChEMBL Inhibition of recombinant human full length N-terminal GST-tagged PI3Kbeta (1 to 1070 residues)/PIK3R1 (1 to 724 residues) expressed in baculovirus expression system using PIP2 as substrate incubated for 2 hrs by ADP-Glo assay B 6.15 pIC50 703.9 nM IC50 Eur J Med Chem (2019) 178: 667-686 [PMID:31228810]
ChEMBL Inhibition of p110beta/p85alpha (unknown origin) incubated for 40 mins by luciferase based ATP depletion assay B 6.32 pIC50 478 nM IC50 Bioorg. Med. Chem. (2015) 23: 6477-6485 [PMID:26321603]
ChEMBL Inhibition of P110beta/p85alpha (unknown origin) using L-alpha-phosphatidylinositol as substrate after 40 mins by ATP depletion assay B 6.38 pIC50 421 nM IC50 Bioorg Med Chem (2015) 23: 7765-7776 [PMID:26652969]
ChEMBL Inhibition of N-terminal His6-tagged recombinant full-length PI3Kbeta (unknown origin)/untagged recombinant full length p85alpha expressed in baculovirus infected Sf21 insect cells by ELISA B 7.44 pIC50 35.9 nM IC50 Bioorg Med Chem (2018) 26: 1675-1685 [PMID:29475582]
ChEMBL Inhibition of recombinant full length human N-terminal His6-tagged PI3K p110beta/p85alpha expressed in baculovirus infected Sf21 cells using PIP2 as substrate after 1 hr by ADP-Glo kinase assay B 7.79 pIC50 16.23 nM IC50 Eur J Med Chem (2017) 127: 509-520 [PMID:28109945]
ATM serine/threonine kinase/Serine-protein kinase ATM in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3797] [GtoPdb: 1934] [UniProtKB: Q13315]
ChEMBL Inhibition of ATM (unknown origin) B 8.15 pIC50 7 nM IC50 J. Med. Chem. (2016) 59: 559-577 [PMID:26632965]
mechanistic target of rapamycin kinase/Serine/threonine-protein kinase mTOR in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2842] [GtoPdb: 2109] [UniProtKB: P42345]
ChEMBL Inhibition of mTOR (unknown origin) using L-alpha-phosphatidylinositol as substrate after 40 mins by ATP depletion assay B 7.01 pIC50 97 nM IC50 Bioorg Med Chem (2015) 23: 7765-7776 [PMID:26652969]
ChEMBL Inhibition of mTOR (unknown origin) assessed as reduction of ATP level after 40 mins by luciferase based luminescence assay B 7.05 pIC50 89 nM IC50 Bioorg. Med. Chem. (2015) 23: 5662-5671 [PMID:26210161]
ChEMBL Inhibition of mTOR (unknown origin) using ULight-4E-BP1 peptide as substrate after 1 hr by lance ultra assay B 7.68 pIC50 21 nM IC50 Bioorg. Med. Chem. (2015) 23: 7585-7596 [PMID:26596710]
ChEMBL Inhibition of mTOR (unknown origin) B 7.68 pIC50 21 nM IC50 MedChemComm (2012) 3: 1337-1355
ChEMBL Inhibition of human mTOR using ULight-4E-BP1 peptide as substrate after 1 hr by Lance ultra assay B 7.68 pIC50 21 nM IC50 MedChemComm (2016) 7: 297-310
ChEMBL Inhibition of mTOR (unknown origin) expressed in baculovirus after 60 mins by kinase-glo assay B 7.68 pIC50 21 nM IC50 Eur J Med Chem (2016) 122: 731-743 [PMID:27479483]
ChEMBL Inhibition of recombinant human N-terminal FLAG-tagged mTOR (1362-end residues) using ULight-4E-BP1 peptide substrate after 1 hr in presence of ATP by Lance Ultra assay B 7.68 pIC50 20.74 nM IC50 Eur J Med Chem (2017) 127: 509-520 [PMID:28109945]
ChEMBL Inhibition of mTOR (unknown origin) assessed as reduction in p70S6K phosphorylation B 7.85 pIC50 14 nM IC50 Bioorg Med Chem Lett (2019) 29: 1313-1319 [PMID:30975623]
ChEMBL Inhibition of mTOR (unknown origin) B 7.92 pIC50 12 nM IC50 Eur J Med Chem (2019) 182: 111630-111630 [PMID:31446244]
ChEMBL Inhibition of mTOR (unknown origin) using GFP-4E-BP1 as substrate after 1 hr by TR-FRET assay B 7.94 pIC50 11.5 nM IC50 ACS Med. Chem. Lett. (2015) 6: 434-438 [PMID:25893045]
ChEMBL Inhibition of mTOR B 8 pIC50 <10 nM IC50 Bioorg. Med. Chem. Lett. (2012) 22: 6788-6793 [PMID:23063403]
GtoPdb Measured as inhibition of downstream mTOR activated p70S6K - 8.22 pIC50 6 nM IC50 Mol Cancer Ther (2008) 7: 1851-63 [PMID:18606717]
ChEMBL Inhibition of mTOR (unknown origin) B 8.22 pIC50 6 nM IC50 Bioorg Med Chem (2018) 26: 4537-4543 [PMID:30077608]
ChEMBL Inhibition of human mTOR after 60 mins in presence of [gamma-33P]-ATP by microplate scintillation counting B 8.22 pIC50 6 nM IC50 ACS Med Chem Lett (2016) 7: 762-767 [PMID:27563400]
ChEMBL Inhibition of human recombinant mTOR assessed as inhibition of 4EBP1 phosphorylation after 30 mins by TR-FRET analysis B 8.3 pIC50 5 nM IC50 J. Med. Chem. (2014) 57: 4834-4848 [PMID:24805946]
ChEMBL mTOR Activity Assay: 1. Preparation of test reagents {circle around (1)} 1x kinase buffer (50 mM HEPES, pH 7.5, 10 mM MgCl2, 1 mM EGTA, 3 mM MnCl, 0.01% Tween-20, 2 mM DTT); {circle around (2)} 4x kinase solution (added mTOR kinase to 1x kinase buffer to provide 4x kinase solution with a final concentration of 2.5 nM); {circle around (3)} 2x substrate solution (added the substrates of 4EBP1 and ATP into 1x kinase buffer to provide 2x substrate solution with 4EBP1 final concentration of 50 nM and ATP final concentration of 10.8 uM); {circle around (4)} 4x test substance solutions (100x test substance solutions with different concentration gradients were prepared using 100% DMSO, and diluted 25-fold with 1x kinase buffer to give 4x test substance solutions with different concentration gradients) {circle around (5)} preparation of test solution (test solution containing EDTA and 4EBP1 phosphorylated antibody was prepared using activity test kit with assay buffer, the final concentration of EDTA was 8 mM, and the final concentration of 4EBP1 phosphorylated antibody was 2 nM) 2. 2.5 uL of 4x test solution was added to a 384-well plate in parallel; 3. added 2.54 uL of 4x kinase solution and incubated for 10 min; 4. then added 5 uL of 2x solutions of 4EBP1 and ATP substrates and incubated for 1 h at room temperature; 5. finally, added 10 uL of test solution to quench the reaction, and read after 60 min; 6. IC50 value was obtained via curve fitting. B 8.49 pIC50 3.23 nM IC50 US-9284315-B2. Three-ring PI3K and/or mTOR inhibitor (2016)
ChEMBL Inhibition of human recombinant mTOR using substrate PI incubated for 1 hr by Adapta kinase assay B 8.7 pIC50 2 nM IC50 J Med Chem (2017) 60: 47-65 [PMID:27644332]
ChEMBL Inhibition of recombinant human N-terminal FLAG-tagged mTOR (1362 to end residues) using Ulight-4E-BP1 as substrate incubated for 30 mins by fluorescence assay B 8.84 pIC50 1.43 nM IC50 Eur J Med Chem (2019) 178: 667-686 [PMID:31228810]
Janus kinase 3/Tyrosine-protein kinase JAK3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2148] [GtoPdb: 2049] [UniProtKB: P52333]
ChEMBL Inhibition of JAK3 (unknown origin) B 6 pIC50 1000 nM IC50 J. Med. Chem. (2013) 56: 6991-7002 [PMID:23937569]
ATR serine/threonine kinase in Human [GtoPdb: 1935] [UniProtKB: Q13535]
GtoPdb - - 7.68 pIC50 21 nM IC50