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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| 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] |
| ChEMBL | Inhibition of PI3Kgamma in C5a stimulated mouse RAW264.7 cells incubated for 10 mins by AlphaLisa assay | B | 5.39 | pIC50 | 4037.4 | nM | IC50 | J Med Chem (2022) 65: 8011-8028 [PMID:35609190] |
| 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) |
| ChEMBL | Inhibition of PI3Kalpha (unknown origin) using PIP2 as substrate measured after 1 hr in presence of ATP by ADP-glo luminescence assay | B | 7.12 | pIC50 | 75.5 | nM | IC50 | J Med Chem (2022) 65: 8011-8028 [PMID:35609190] |
| phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha/PI3-kinase p110-alpha subunit in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2499] [GtoPdb: 2153] [UniProtKB: P42337] | ||||||||
| ChEMBL | Inhibition of PI3Kalpha in IGF-1 stimulated mouse C2C12 cells incubated for 10 mins by AlphaLISA assay | B | 4.71 | pIC50 | 19628.2 | nM | IC50 | J Med Chem (2022) 65: 8011-8028 [PMID:35609190] |
| 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 in LPA stimulated human PC-3 cells incubated for 10 mins by AlphaLISA assay | B | 5.57 | pIC50 | 2683.7 | nM | IC50 | J Med Chem (2022) 65: 8011-8028 [PMID:35609190] |
| ChEMBL | Inhibition of PI3Kbeta (unknown origin) using PIP2 as substrate measured after 1 hr in presence of ATP by ADP-glo luminescence assay | B | 6.44 | pIC50 | 363 | nM | IC50 | J Med Chem (2022) 65: 8011-8028 [PMID:35609190] |
| 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 PI3Kdelta in IgM stimulated human Raji cells incubated for 10 mins by AlphaLISA assay | B | 7.2 | pIC50 | 62.8 | nM | IC50 | J Med Chem (2022) 65: 8011-8028 [PMID:35609190] |
| 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] |
| ChEMBL | Inhibition of PI3Kdelta (unknown origin) using PIP2 as substrate measured after 1 hr in presence of ATP by ADP-glo luminescence assay | B | 8.82 | pIC50 | 1.5 | nM | IC50 | J Med Chem (2022) 65: 8011-8028 [PMID:35609190] |
| 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] |
| ChEMBL | Inhibition of PI3Kgamma (unknown origin) using PIP2 as substrate measured after 1 hr in presence of ATP by ADP-glo luminescence assay | B | 6.04 | pIC50 | 902 | nM | IC50 | J Med Chem (2022) 65: 8011-8028 [PMID:35609190] |
| 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 mTOR (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2022) 65: 8011-8028 [PMID:35609190] |
| 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 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]
