leniolisib [Ligand Id: 9424] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3643413 (Cdz-173 free base, Cdz173 free base, CDZ-173-NX, CDZ173-NX, Leniolisib)
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  • protein kinase, DNA-activated, catalytic subunit/DNA-dependent protein kinase in Human [ChEMBL: CHEMBL3142] [GtoPdb: 2800] [UniProtKB: P78527]
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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-4,5-bisphosphate 3-kinase catalytic subunit delta in Human [GtoPdb: 2155] [UniProtKB: O00329]
  • phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit delta/Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform in Mouse [ChEMBL: CHEMBL2216745] [GtoPdb: 2155] [UniProtKB: O35904]
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  • phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma/Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform in Mouse [ChEMBL: CHEMBL2189158] [GtoPdb: 2156] [UniProtKB: Q9JHG7]
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  • phosphodiesterase 4D/Phosphodiesterase 4D in Human [ChEMBL: CHEMBL288] [GtoPdb: 1303] [UniProtKB: Q08499]
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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 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 beta/PI4-kinase beta subunit in Human [ChEMBL: CHEMBL3268] [GtoPdb: 2149] [UniProtKB: Q9UBF8]
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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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  • 5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Cellular tumor antigen p53 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4096] [UniProtKB: P04637]
ChEMBL Inhibition of p53 in human HCT116 cells assessed as reduction in nutlin-induced p53 transcriptional response by FRET assay B 5.52 pIC50 >3000 nM IC50 ACS Med Chem Lett (2017) 8: 975-980 [PMID:28947947]
protein kinase, DNA-activated, catalytic subunit/DNA-dependent protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3142] [GtoPdb: 2800] [UniProtKB: P78527]
ChEMBL Inhibition of DNA-PK (unknown origin) using peptide substrate assessed as reduction in incorporation of radioactive 33p into substrate by liquid scintillation counting method B 6.06 pIC50 880 nM IC50 ACS Med Chem Lett (2017) 8: 975-980 [PMID:28947947]
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) using phosphatidyl inositol/n-Octyl-glucoside as substrate measured after 30 mins by KinaseGlo assay B 5.04 pIC50 >9100 nM IC50 ACS Med Chem Lett (2017) 8: 975-980 [PMID:28947947]
phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit delta in Human [GtoPdb: 2155] [UniProtKB: O00329]
GtoPdb In vitro enzyme assay - 7.64 pIC50 23 nM IC50 WO2012004299. Tetrahydro-pyrido-pyrimidine derivatives (2012)
phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit delta/Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2216745] [GtoPdb: 2155] [UniProtKB: O35904]
ChEMBL Inhibition of PI3Kdelta in anti-CD3/CD28 stimulated mouse CD4-positive T cells assessed as reduction in T cell differentiation to Th17 cells by measuring IL-17A level after 72 hrs by ELISA B 7 pIC50 101 nM IC50 ACS Med Chem Lett (2017) 8: 975-980 [PMID:28947947]
ChEMBL Inhibition of PI3Kdelta in Balb/c mouse splenocytes assessed as reduction in anti-IgM stimulated CD86 expression pretreated for 1 hr followed by anti-IgM stimulation after 24 hrs by flow cytometric analysis B 7.32 pIC50 48 nM IC50 ACS Med Chem Lett (2017) 8: 975-980 [PMID:28947947]
ChEMBL Inhibition of PI3Kdelta in mouse spleen cells assessed as reduction in cell proliferation by measuring [3H]thymidine incorporation by beta counting based mixed lymphocyte reaction assay B 7.48 pIC50 33 nM IC50 ACS Med Chem Lett (2017) 8: 975-980 [PMID:28947947]
ChEMBL Inhibition of PI3Kdelta in anti-CD3/CD28 stimulated mouse CD4-positive T cells assessed as reduction in T cell differentiation to Th2 cells by measuring IL-13 level after 72 hrs by ELISA B 8 pIC50 10 nM IC50 ACS Med Chem Lett (2017) 8: 975-980 [PMID:28947947]
ChEMBL Inhibition of PI3Kdelta in mouse B cells assessed as reduction in anti-IgM-induced cell proliferation measured last 16 hrs of 88 hrs incubation by [3H]thymidine incorporation assay B 8.15 pIC50 7 nM IC50 ACS Med Chem Lett (2017) 8: 975-980 [PMID:28947947]
phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma/Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2189158] [GtoPdb: 2156] [UniProtKB: Q9JHG7]
ChEMBL Inhibition of PI3Kgamma in C57/Bl6 mouse BMMC assessed as reduction in adenosine stimulated ATK phosphorylation at ser473 residue pretreated for 30 mins followed by adenosine addition measured after 3 minutes B 5.11 pIC50 7800 nM IC50 ACS Med Chem Lett (2017) 8: 975-980 [PMID:28947947]
phosphodiesterase 4D/Phosphodiesterase 4D in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL288] [GtoPdb: 1303] [UniProtKB: Q08499]
ChEMBL Inhibition of recombinant human PDE4D B 5.33 pIC50 4700 nM IC50 ACS Med Chem Lett (2017) 8: 975-980 [PMID:28947947]
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]
GtoPdb In vitro enzyme assay - 6.58 pIC50 262 nM IC50 WO2012004299. Tetrahydro-pyrido-pyrimidine derivatives (2012)
ChEMBL Enzyme Assay: Test of Lipid Kinase Activity: The kinase reaction is performed in a final volume of 50 μl per well of a half area COSTAR, 96 well plate. The final concentrations of ATP and phosphatidyl inositol in the assay are 5 μM and 6 μg/mL, respectively. The reaction is started by the addition of PI3 kinase, e.g. PI3 kinase δ. Refer to the patent for more info. B 6.58 pIC50 262 nM IC50 US-8653092-B2. Tetrahydro-pyrido-pyrimidine derivatives (2014)
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 in anti-CD3/CD28 stimulated human PBMC derived CD4-positive T cells assessed as reduction in cell proliferation by measuring [3H]thymidine incorporation by beta counting method B 5.94 pIC50 1150 nM IC50 ACS Med Chem Lett (2017) 8: 975-980 [PMID:28947947]
ChEMBL Inhibition of PI3Kdelta in 90% human whole blood assessed as reduction in anti-IgM/IL4 stimulated CD86 expression pretreated for 1 hr followed by anti-IgM/IL4 stimulation after 24 hrs by flow cytometric analysis B 6.69 pIC50 202 nM IC50 ACS Med Chem Lett (2017) 8: 975-980 [PMID:28947947]
ChEMBL Inhibition of PI3Kdelta in 90% human whole blood assessed as reduction in anti-IgM/IL4 stimulated CD69 expression pretreated for 1 hr followed by anti-IgM/IL4 stimulation after 24 hrs by flow cytometric analysis B 6.71 pIC50 193 nM IC50 ACS Med Chem Lett (2017) 8: 975-980 [PMID:28947947]
ChEMBL Inhibition of PI3Kdelta in anti-CD3 stimulated human PBMC assessed as reduction in cell proliferation by measuring [3H]thymidine incorporation pretreated for 1 hr followed by anti-CD3 addition measured last 16 hrs of 56 hrs incubation by beta counting method B 6.8 pIC50 159 nM IC50 ACS Med Chem Lett (2017) 8: 975-980 [PMID:28947947]
ChEMBL Inhibition of PI3Kdelta in human B cells assessed as reduction in anti-IgM-induced AKT phosphorylation at ser473 residue pretreated for 1.5 hrs followed by anti-IgM stimulation after 20 mins by flow cytometric analysis B 6.84 pIC50 144 nM IC50 ACS Med Chem Lett (2017) 8: 975-980 [PMID:28947947]
ChEMBL Inhibition of PI3Kdelta in anti-CD3/CD28 stimulated human PBMC derived CD4-positive T cells assessed as reduction in T cell differentiation to Th2 cells by measuring IL-13 level after 72 hrs by ELISA B 7.02 pIC50 95 nM IC50 ACS Med Chem Lett (2017) 8: 975-980 [PMID:28947947]
ChEMBL Inhibition of PI3Kdelta in human PBMC assessed as reduction in cell proliferation by measuring [3H]thymidine incorporation measured last 16 hrs of 4 days incubation by beta counting based mixed lymphocyte reaction assay B 7.1 pIC50 79 nM IC50 ACS Med Chem Lett (2017) 8: 975-980 [PMID:28947947]
ChEMBL Inhibition of PI3Kdelta in anti-CD3/CD28 stimulated human PBMC derived CD4-positive T cells assessed as reduction in T cell differentiation to Th17 cells by measuring IL-17A level after 72 hrs by ELISA B 7.14 pIC50 73 nM IC50 ACS Med Chem Lett (2017) 8: 975-980 [PMID:28947947]
ChEMBL Inhibition of recombinant human myristoylated PI3Kdelta catalytic domain expressed in Rat1 cells assessed as reduction in Akt phosphorylation at Ser47 residue after 1 hr by alpha screen Surefire assay B 7.25 pIC50 56 nM IC50 ACS Med Chem Lett (2017) 8: 975-980 [PMID:28947947]
ChEMBL Enzyme Assay: Test of Lipid Kinase Activity: The kinase reaction is performed in a final volume of 50 μl per well of a half area COSTAR, 96 well plate. The final concentrations of ATP and phosphatidyl inositol in the assay are 5 μM and 6 μg/mL, respectively. The reaction is started by the addition of PI3 kinase, e.g. PI3 kinase δ. Refer to the patent for more info. B 7.64 pIC50 23 nM IC50 US-8653092-B2. Tetrahydro-pyrido-pyrimidine derivatives (2014)
GtoPdb In vitro enzyme assay - 7.64 pIC50 23 nM IC50 WO2012004299. Tetrahydro-pyrido-pyrimidine derivatives (2012)
ChEMBL Inhibition of PI3Kdelta (unknown origin) using phosphatidyl inositol as substrate measured after 60 mins by Alexa Fluor647-labelled ADP tracer based TR-FRET assay B 7.96 pIC50 11 nM IC50 ACS Med Chem Lett (2017) 8: 975-980 [PMID:28947947]
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 in human U937 cells assessed as reduction in MIP-1 alpha stimulated ATK phosphorylation at ser473 residue pretreated for 30 mins followed by MIP-1 alpha addition measured after 3 mins by fluorescence assay B 5.13 pIC50 >7400 nM IC50 ACS Med Chem Lett (2017) 8: 975-980 [PMID:28947947]
ChEMBL Inhibition of PI3Kgamma (unknown origin) using phosphatidyl inositol as substrate measured after 30 mins by Alexa Fluor647-labelled ADP tracer based TR-FRET assay B 5.65 pIC50 2230 nM IC50 ACS Med Chem Lett (2017) 8: 975-980 [PMID:28947947]
phosphatidylinositol 4-kinase beta/PI4-kinase beta subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3268] [GtoPdb: 2149] [UniProtKB: Q9UBF8]
ChEMBL Inhibition of PI4Kbeta (unknown origin) using phosphatidyl inositol/n-Octyl-glucoside as substrate measured after 30 mins by KinaseGlo assay B 5.04 pIC50 >9100 nM IC50 ACS Med Chem Lett (2017) 8: 975-980 [PMID:28947947]
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 recombinant mTOR (unknown origin) using 4EBP1 as substrate by TR-FRET assay B 5.04 pIC50 >9100 nM IC50 ACS Med Chem Lett (2017) 8: 975-980 [PMID:28947947]
5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
ChEMBL Inhibition of 5-HT2B (unknown origin) by calcium flux assay F 5.11 pIC50 7700 nM IC50 ACS Med Chem Lett (2017) 8: 975-980 [PMID:28947947]

ChEMBL data shown on this page come from version 33:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]