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| ChEMBL ligand: CHEMBL1229535 |
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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 catalytic subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3142] [GtoPdb: 2800] [UniProtKB: P78527] | ||||||||
| ChEMBL | Inhibition of human DNA-PK by non-radiometric ADP-Glo assay | B | 7.19 | pIC50 | 64 | nM | IC50 | ACS Med Chem Lett (2015) 6: 3-6 [PMID:25589915] |
| ChEMBL | Inhibition of DNA-PK (unknown origin) | B | 7.19 | pIC50 | 64 | nM | IC50 | J Med Chem (2017) 60: 47-65 [PMID:27644332] |
| 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 full length human recombinant VPS34 (unknown origin) using phosphatidylinositol and gamma-32P-ATP incubated for 20 mins by TLC assay or high-throughput membrane capture assay | B | 6.49 | pIC50 | 320 | nM | IC50 | J Med Chem (2017) 60: 47-65 [PMID:27644332] |
| ChEMBL | Inhibition of GST-tagged recombinant human full length VPS34 expressed in baculovirus preincubated for 15 mins followed by addition of cold ATP/gamma32P-ATP measured after 1 hr in presence of MnCl2 | B | 6.51 | pIC50 | 307 | nM | IC50 | J Med Chem (2016) 59: 1830-1839 [PMID:26885694] |
| ChEMBL | Inhibition of human VPS34 assessed as reduction in PIP3 product complex formation | B | 6.51 | pEC50 | 307 | nM | EC50 | Biochemistry (2017) 56: 4326-4334 [PMID:28719179] |
| ChEMBL | Inhibition of human VPS34 assessed as reduction in PIP3 product complex formation measured after 30 mins in presence of ATP by quantitative PI3P ELISA assay | B | 6.66 | pEC50 | 220 | nM | EC50 | Biochemistry (2017) 56: 4326-4334 [PMID:28719179] |
| phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha/Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4005] [GtoPdb: 2153] [UniProtKB: P42336] | ||||||||
| ChEMBL | Inhibition of PI3Kalpha (unknown origin) | B | 7.41 | pIC50 | 39 | nM | IC50 | Medchemcomm (2012) 3: 1337-1355 |
| ChEMBL | Inhibition of PI3K alpha (unknown origin) | B | 7.41 | pIC50 | 39 | nM | IC50 | J Med Chem (2022) 65: 893-921 [PMID:33539089] |
| ChEMBL | Inhibition of PI3K alpha (unknown origin) by membrane capture assay | B | 7.41 | pEC50 | 39 | nM | EC50 | Biochemistry (2017) 56: 4326-4334 [PMID:28719179] |
| phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit beta/Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3145] [GtoPdb: 2154] [UniProtKB: P42338] | ||||||||
| ChEMBL | Inhibition of PI3Kbeta (unknown origin) | B | 6.23 | pIC50 | 590 | nM | IC50 | Medchemcomm (2012) 3: 1337-1355 |
| ChEMBL | Inhibition of PI3K beta (unknown origin) by membrane capture assay | B | 6.23 | pEC50 | 590 | nM | EC50 | Biochemistry (2017) 56: 4326-4334 [PMID:28719179] |
| ChEMBL | Inhibition of human PI3Kbeta assessed as reduction in PIP3 product complex formation | B | 6.23 | pEC50 | 590 | nM | EC50 | Biochemistry (2017) 56: 4326-4334 [PMID:28719179] |
| ChEMBL | Inhibition of human PI3Kbeta assessed as reduction in PIP3 product complex formation measured after 30 mins in presence of ATP by quantitative PI3P ELISA assay | B | 6.27 | pEC50 | 539 | nM | EC50 | Biochemistry (2017) 56: 4326-4334 [PMID:28719179] |
| phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit delta/Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3130] [GtoPdb: 2155] [UniProtKB: O00329] | ||||||||
| ChEMBL | Inhibition of PI3Kdelta (unknown origin) | B | 6.92 | pIC50 | 120 | nM | IC50 | Medchemcomm (2012) 3: 1337-1355 |
| ChEMBL | Inhibition of histidine-tagged recombinant human full length PI3Kdelta expressed in baculovirus preincubated for 15 mins followed by addition of cold ATP/gamma32P-ATP measured after 20 mins in presence of MgCl2 | B | 7.11 | pIC50 | 77 | nM | IC50 | J Med Chem (2016) 59: 1830-1839 [PMID:26885694] |
| phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma/Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3267] [GtoPdb: 2156] [UniProtKB: P48736] | ||||||||
| ChEMBL | Inhibition of PI3K-gamma (unknown origin) | B | 8.15 | pKi | 7 | nM | Ki | J Med Chem (2015) 58: 517-521 [PMID:24754609] |
| ChEMBL | Binding affinity to PI3Kgamma (unknown origin) assessed as inhibition constant | B | 8.15 | pKi | 7 | nM | Ki | J Med Chem (2024) 67: 10530-10547 [PMID:38988222] |
| ChEMBL | Inhibition of histidine-tagged recombinant human full length PI3Kgamma expressed in insect cells preincubated for 15 mins followed by addition of cold ATP/gamma32P-ATP measured after 15 mins in presence of MgCl2 | B | 7.77 | pIC50 | 17 | nM | IC50 | J Med Chem (2016) 59: 1830-1839 [PMID:26885694] |
| ChEMBL | Inhibition of PI3Kgamma (unknown origin) | B | 7.8 | pIC50 | 16 | nM | IC50 | Medchemcomm (2012) 3: 1337-1355 |
| ChEMBL | Inhibition of human PI3KCgamma by non-radiometric ADP-Glo assay | B | 7.8 | pIC50 | 16 | nM | IC50 | ACS Med Chem Lett (2015) 6: 3-6 [PMID:25589915] |
| ChEMBL | Inhibition of PI3Kgamma (unknown origin) using phosphatidylinositol and gamma-32P-ATP incubated for 20 mins by TLC assay or high-throughput membrane capture assay | B | 7.8 | pIC50 | 16 | nM | IC50 | J Med Chem (2017) 60: 47-65 [PMID:27644332] |
| ChEMBL | Inhibition of PI3K gamma (unknown origin) by membrane capture assay | B | 8.4 | pEC50 | 4 | nM | EC50 | Biochemistry (2017) 56: 4326-4334 [PMID:28719179] |
| phosphatidylinositol 4-kinase alpha/Phosphatidylinositol 4-kinase alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3667] [GtoPdb: 2148] [UniProtKB: P42356] | ||||||||
| ChEMBL | Inhibition of PI4K3alpha (unknown origin) | B | 5.96 | pIC50 | 1100 | nM | IC50 | J Med Chem (2018) 61: 6705-6723 [PMID:29952567] |
| ChEMBL | Inhibition of PI4KA (unknown origin) by membrane capture assay | B | 5.96 | pEC50 | 1100 | nM | EC50 | Biochemistry (2017) 56: 4326-4334 [PMID:28719179] |
| phosphatidylinositol 4-kinase beta/Phosphatidylinositol 4-kinase beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3268] [GtoPdb: 2149] [UniProtKB: Q9UBF8] | ||||||||
| ChEMBL | Inhibition of PI4K3beta in human PBMC assessed as reduction in mitomycin-C treated human RPMI1788 cells-stimulated lymphocyte proliferation by measuring reduction in [3H]thymidine incorporation preincubated for 5 days followed by [3H]thymidine addition measured after 18 hrs by liquid scintillation counting method | B | 7.55 | pIC50 | 28 | nM | IC50 | J Med Chem (2018) 61: 6705-6723 [PMID:29952567] |
| GtoPdb | - | - | 7.72 | pIC50 | 19 | nM | IC50 |
Cell (2006) 125: 733-47 [PMID:16647110]; Mol Biol Cell (2008) 19: 711-21 [PMID:18077555] |
| ChEMBL | Inhibition of PI4K3beta (unknown origin) | B | 7.72 | pIC50 | 19 | nM | IC50 | J Med Chem (2018) 61: 6705-6723 [PMID:29952567] |
| ChEMBL | Inhibition of PI4KIIIbeta (unknown origin) | B | 7.72 | pIC50 | 19 | nM | IC50 | J Med Chem (2022) 65: 893-921 [PMID:33539089] |
| ChEMBL | Inhibition of PI4KB (unknown origin) by membrane capture assay | B | 7.77 | pEC50 | 17 | nM | EC50 | Biochemistry (2017) 56: 4326-4334 [PMID:28719179] |
| 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 PI3KC2alpha by non-radiometric ADP-Glo assay | B | 4.8 | pIC50 | 16000 | nM | IC50 | ACS Med Chem Lett (2015) 6: 3-6 [PMID:25589915] |
| ChEMBL | Inhibition of PI3KC2alpha (unknown origin) expressed in HEK293 cells using phosphatidylinositol and gamma-32P-ATP incubated for 20 mins by TLC assay or high-throughput membrane capture assay | B | 4.8 | pIC50 | 16000 | nM | IC50 | J Med Chem (2017) 60: 47-65 [PMID:27644332] |
| ChEMBL | Inhibition of PIK3C2A (unknown origin) by membrane capture assay | B | 4.8 | pEC50 | 16000 | nM | EC50 | Biochemistry (2017) 56: 4326-4334 [PMID:28719179] |
| phosphatidylinositol-4-phosphate 3-kinase catalytic subunit type 2 beta/Phosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5554] [GtoPdb: 2151] [UniProtKB: O00750] | ||||||||
| ChEMBL | Inhibition of PI3KC2beta (unknown origin) expressed in HEK293 cells using phosphatidylinositol and gamma-32P-ATP incubated for 20 mins by TLC assay or high-throughput membrane capture assay | B | 4.85 | pIC50 | 14000 | nM | IC50 | J Med Chem (2017) 60: 47-65 [PMID:27644332] |
| ChEMBL | Inhibition of human PI3KC2beta by non-radiometric ADP-Glo assay | B | 6.85 | pIC50 | 140 | nM | IC50 | ACS Med Chem Lett (2015) 6: 3-6 [PMID:25589915] |
| ChEMBL | Inhibition of PIK3C2B (unknown origin) by membrane capture assay | B | 6.85 | pEC50 | 140 | nM | EC50 | Biochemistry (2017) 56: 4326-4334 [PMID:28719179] |
ChEMBL data shown on this page come from version 36:
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]