Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
ChEMBL ligand: CHEMBL2387080 (GDC-0032, RG-7604, Taselisib) |
---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
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 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3142] [GtoPdb: 2800] [UniProtKB: P78527] | ||||||||
ChEMBL | Inhibition of DNA-dependent protein kinase (unknown origin) | B | 5.32 | pIC50 | >4800 | nM | IC50 | J Med Chem (2013) 56: 4597-4610 [PMID:23662903] |
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 VPS34 | B | 6.43 | pIC50 | 374 | nM | IC50 | J Med Chem (2013) 56: 4597-4610 [PMID:23662903] |
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) | B | 6.53 | pIC50 | 292 | nM | IC50 | J Med Chem (2013) 56: 4597-4610 [PMID:23662903] |
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 PI3KC2alpha (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2013) 56: 4597-4610 [PMID:23662903] |
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 recombinant PI3K alpha (unknown origin) using PIP2 as substrate by fluorescence polarization assay | B | 9.52 | pKi | 0.3 | nM | Ki | J Med Chem (2016) 59: 985-1002 [PMID:26741947] |
ChEMBL | Inhibition of PI3Kalpha (unknown origin) assessed as 3,4,5-inositoltriphosphate formation after 30 mins by fluorescence polarization assay | B | 9.54 | pKi | 0.29 | nM | Ki | J Med Chem (2013) 56: 4597-4610 [PMID:23662903] |
GtoPdb | - | - | 9.54 | pKi | 0.29 | nM | Ki | J Med Chem (2013) 56: 4597-610 [PMID:23662903] |
GtoPdb | - | - | 10.05 | pKi | 0.09 | nM | Ki | US20170015678. Benzoxazepin oxazolidinone compounds and methods of use (2017) |
ChEMBL | Inhibition of PI3Kalpha in human PC3 cells assessed as reduction of AKT phosphorylation | B | 7.51 | pIC50 | 31 | nM | IC50 | J Med Chem (2013) 56: 4597-4610 [PMID:23662903] |
ChEMBL | Inhibition of PI3Kalpha in human MCF7-neo/Her2 cells assessed as reduction of AKT phosphorylation at S473 | B | 8.4 | pIC50 | 4 | nM | IC50 | J Med Chem (2013) 56: 4597-4610 [PMID:23662903] |
ChEMBL | Inhibition of PI3K alpha (unknown origin) | B | 9.15 | pIC50 | <0.7 | nM | IC50 | ACS Med Chem Lett (2017) 8: 808-813 [PMID:28835793] |
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] | ||||||||
GtoPdb | - | - | 7.28 | pKi | 53 | nM | Ki | US20170015678. Benzoxazepin oxazolidinone compounds and methods of use (2017) |
GtoPdb | - | - | 8.04 | pKi | 9.1 | nM | Ki | J Med Chem (2013) 56: 4597-610 [PMID:23662903] |
ChEMBL | Inhibition of PI3Kbeta (unknown origin) | B | 8.04 | pKi | 9.1 | nM | Ki | J Med Chem (2013) 56: 4597-4610 [PMID:23662903] |
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] | ||||||||
GtoPdb | - | - | 9.68 | pKi | 0.21 | nM | Ki | J Med Chem (2013) 56: 4597-610 [PMID:23662903] |
ChEMBL | Inhibition of PI3Kdelta (unknown origin) | B | 9.92 | pKi | 0.12 | nM | Ki | J Med Chem (2013) 56: 4597-4610 [PMID:23662903] |
GtoPdb | - | - | 10.1 | pKi | 0.08 | nM | Ki | US20170015678. Benzoxazepin oxazolidinone compounds and methods of use (2017) |
ChEMBL | Inhibition of PI3K delta (unknown origin) | B | 9.15 | pIC50 | <0.7 | nM | IC50 | ACS Med Chem Lett (2017) 8: 808-813 [PMID:28835793] |
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] | ||||||||
GtoPdb | - | - | 8.84 | pKi | 1.43 | nM | Ki | US20170015678. Benzoxazepin oxazolidinone compounds and methods of use (2017) |
GtoPdb | - | - | 9.01 | pKi | 0.97 | nM | Ki | J Med Chem (2013) 56: 4597-610 [PMID:23662903] |
ChEMBL | Inhibition of PI3Kgamma (unknown origin) | B | 9.01 | pKi | 0.97 | nM | Ki | J Med Chem (2013) 56: 4597-4610 [PMID:23662903] |
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 | 5.92 | pKi | 1200 | nM | Ki | J Med Chem (2013) 56: 4597-4610 [PMID:23662903] |
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]