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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 |
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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 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] |
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 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] |
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] |
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) | B | 7.41 | pIC50 | 39 | nM | IC50 | Medchemcomm (2012) 3: 1337-1355 |
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) | B | 6.23 | pIC50 | 590 | nM | IC50 | Medchemcomm (2012) 3: 1337-1355 |
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) | 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/PI3-kinase p110-gamma subunit 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 | 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] |
phosphatidylinositol 4-kinase alpha/PI4-kinase alpha subunit 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] |
phosphatidylinositol 4-kinase beta/PI4-kinase beta subunit 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 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]