torin 2 [Ligand Id: 8839] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1765602 |
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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 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3142] [GtoPdb: 2800] [UniProtKB: P78527] | ||||||||
| GtoPdb | - | - | 9.3 | pIC50 | 0.5 | nM | IC50 | J Med Chem (2011) 54: 1473-80 [PMID:21322566] |
| ChEMBL | Inhibition of DNA-PK | B | 9.3 | pIC50 | 0.5 | nM | IC50 | J Med Chem (2011) 54: 1473-1480 [PMID:21322566] |
| ChEMBL | Inhibition of DNAPK in human HCT116 cells assessed as after 1 hr by Western blot analysis | B | 6.93 | pEC50 | 118 | nM | EC50 | J Med Chem (2018) 61: 4656-4687 [PMID:29211480] |
| mechanistic target of rapamycin kinase/mTORC1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL4296661] [GtoPdb: 2109] [UniProtKB: P42345, Q8N122, Q9BVC4] | ||||||||
| ChEMBL | Inhibition of N-terminally FLAG-tagged mTORC1 (unknown origin) expressed in HEK293T cells using S6K1 or Akt1 as substrate after 20 mins by immunoblotting assay | B | 8 | pIC50 | <10 | nM | IC50 | J Med Chem (2018) 61: 4656-4687 [PMID:29211480] |
| GtoPdb | - | - | 8.55 | pIC50 | 2.81 | nM | IC50 | J Med Chem (2011) 54: 1473-80 [PMID:21322566] |
| ChEMBL | Inhibition of mTORC1 in human HCT116 cells assessed as reduction in T389 phosphorylation on RPS6KB1 after 1 hr by Western blot analysis | B | 9.6 | pEC50 | 0.25 | nM | EC50 | J Med Chem (2018) 61: 4656-4687 [PMID:29211480] |
| mechanistic target of rapamycin kinase/mTORC2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL4523999] [GtoPdb: 2109] [UniProtKB: P42345, Q6R327, Q9BPZ7, Q9BVC4] | ||||||||
| ChEMBL | Inhibition of N-terminally FLAG-tagged mTORC2 (unknown origin) expressed in human HeLa cells using S6K1 or Akt1 as substrate after 20 mins by immunoblotting assay | B | 8 | pIC50 | <10 | nM | IC50 | J Med Chem (2018) 61: 4656-4687 [PMID:29211480] |
| GtoPdb | - | - | 8.55 | pIC50 | 2.81 | nM | IC50 | J Med Chem (2011) 54: 1473-80 [PMID:21322566] |
| 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 hVPS34 | B | 8.07 | pIC50 | 8.58 | nM | IC50 | J Med Chem (2011) 54: 1473-1480 [PMID:21322566] |
| GtoPdb | - | - | 8.07 | pIC50 | 8.58 | nM | IC50 | J Med Chem (2011) 54: 1473-80 [PMID:21322566] |
| 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] | ||||||||
| GtoPdb | - | - | 7.61 | pIC50 | 24.5 | nM | IC50 | J Med Chem (2011) 54: 1473-80 [PMID:21322566] |
| ChEMBL | Inhibition of PI3K-C2beta | B | 7.61 | pIC50 | 24.5 | nM | IC50 | J Med Chem (2011) 54: 1473-1480 [PMID:21322566] |
| 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] | ||||||||
| GtoPdb | - | - | 7.55 | pIC50 | 28.1 | nM | IC50 | J Med Chem (2011) 54: 1473-80 [PMID:21322566] |
| ChEMBL | Inhibition of PI3K-C2alpha | B | 7.55 | pIC50 | 28.1 | nM | IC50 | J Med Chem (2011) 54: 1473-1480 [PMID:21322566] |
| phosphoinositide-3-kinase regulatory subunit 1/phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha/PI3-kinase p110-alpha/p85-alpha in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111367] [GtoPdb: 2503, 2153] [UniProtKB: P27986, P42336] | ||||||||
| ChEMBL | Inhibition of P110 alpha/p85alpha | B | 8.33 | pIC50 | 4.68 | nM | IC50 | J Med Chem (2011) 54: 1473-1480 [PMID:21322566] |
| 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 in human PC3 cells expressing Akt1 S473D mutant assessed as phosphorylation of Akt Thr308 by immunoblotting | B | 6.7 | pEC50 | 200 | nM | EC50 | J Med Chem (2011) 54: 1473-1480 [PMID:21322566] |
| phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit delta/phosphoinositide-3-kinase regulatory subunit 1/PI3-kinase p110-delta/p85-alpha in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111432] [GtoPdb: 2155, 2503] [UniProtKB: O00329, P27986] | ||||||||
| ChEMBL | Inhibition of P110delta/P85alpha | B | 7.76 | pIC50 | 17.5 | nM | IC50 | J Med Chem (2011) 54: 1473-1480 [PMID:21322566] |
| GtoPdb | - | - | 8.25 | pIC50 | 5.67 | nM | IC50 | J Med Chem (2011) 54: 1473-80 [PMID:21322566] |
| 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 P110gamma | B | 8.25 | pIC50 | 5.67 | nM | IC50 | J Med Chem (2011) 54: 1473-1480 [PMID:21322566] |
| phosphatidylinositol 4-kinase alpha/PI4-kinase alpha subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3667] [GtoPdb: 2148] [UniProtKB: P42356] | ||||||||
| ChEMBL | Inhibition of PI4K alpha | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2011) 54: 1473-1480 [PMID:21322566] |
| phosphatidylinositol 4-kinase beta/PI4-kinase beta subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3268] [GtoPdb: 2149] [UniProtKB: Q9UBF8] | ||||||||
| ChEMBL | Inhibition of PI4K beta | B | 7.74 | pIC50 | 18.3 | nM | IC50 | J Med Chem (2011) 54: 1473-1480 [PMID:21322566] |
| GtoPdb | - | - | 7.74 | pIC50 | 18.3 | nM | IC50 | J Med Chem (2011) 54: 1473-80 [PMID:21322566] |
| Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364] | ||||||||
| ChEMBL | Gametocytocidal activity against Plasmodium falciparum after 72 hrs by Alamar Blue assay | F | 8.1 | pIC50 | 8 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 2907-2911 [PMID:27156776] |
| ATM serine/threonine kinase/Serine-protein kinase ATM in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3797] [GtoPdb: 1934] [UniProtKB: Q13315] | ||||||||
| ChEMBL | Inhibition of ATM in human HCT116 cells assessed as after 1 hr by Western blot analysis | B | 7.55 | pEC50 | 28 | nM | EC50 | J Med Chem (2018) 61: 4656-4687 [PMID:29211480] |
| ATR serine/threonine kinase/Serine-protein kinase ATR in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5024] [GtoPdb: 1935] [UniProtKB: Q13535] | ||||||||
| ChEMBL | Inhibition of ATR in human HCT116 cells assessed as after 1 hr by Western blot analysis | B | 7.46 | pEC50 | 35 | nM | EC50 | J Med Chem (2018) 61: 4656-4687 [PMID:29211480] |
| mechanistic target of rapamycin kinase/Serine/threonine-protein kinase mTOR in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2842] [GtoPdb: 2109] [UniProtKB: P42345] | ||||||||
| GtoPdb | - | - | 8.55 | pIC50 | 2.81 | nM | IC50 | J Med Chem (2011) 54: 1473-80 [PMID:21322566] |
| ChEMBL | Inhibition of mTOR (unknown origin) | B | 9.6 | pIC50 | 0.25 | nM | IC50 | Bioorg Med Chem (2018) 26: 4537-4543 [PMID:30077608] |
| mechanistic target of rapamycin kinase/Serine/threonine-protein kinase mTOR in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1255165] [GtoPdb: 2109] [UniProtKB: Q9JLN9] | ||||||||
| ChEMBL | Inhibition of mTOR in p53-deficient MEF assessed as phosphorylation of S6K1 at Thr389 by immunoblotting | B | 9.6 | pEC50 | 0.25 | nM | EC50 | J Med Chem (2011) 54: 1473-1480 [PMID:21322566] |
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]
