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ChEMBL ligand: CHEMBL1256459 (Torin1) |
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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 DNA-PK | B | 8.2 | pIC50 | 6.34 | nM | IC50 | J Med Chem (2010) 53: 7146-7155 [PMID:20860370] |
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 | 8.7 | pIC50 | 2 | nM | IC50 | J Med Chem (2018) 61: 4656-4687 [PMID:29211480] |
GtoPdb | Assayed using mTORC1 complex | - | 9.54 | pIC50 | 0.29 | nM | IC50 | J Med Chem (2010) 53: 7146-55 [PMID:20860370] |
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 | Assayed using mTORC1 complex | - | 9.54 | pIC50 | 0.29 | nM | IC50 | J Med Chem (2010) 53: 7146-55 [PMID:20860370] |
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 hVPS34 | B | 6.27 | pIC50 | 533 | nM | IC50 | J Med Chem (2010) 53: 7146-7155 [PMID:20860370] |
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 PI3K-C2 beta | B | 6.26 | pIC50 | 549 | nM | IC50 | J Med Chem (2010) 53: 7146-7155 [PMID:20860370] |
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 PI3K-C2 alpha | B | 6.75 | pIC50 | 176 | nM | IC50 | J Med Chem (2010) 53: 7146-7155 [PMID:20860370] |
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 P110alpha/p85-alpha | B | 6.6 | pIC50 | 250 | nM | IC50 | J Med Chem (2010) 53: 7146-7155 [PMID:20860370] |
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 | Binding affinity to PIK3CA | B | 7.64 | pKd | 23 | nM | Kd | J Med Chem (2010) 53: 7146-7155 [PMID:20860370] |
ChEMBL | Binding affinity to PIK3CA I800L mutant | B | 7.85 | pKd | 14 | nM | Kd | J Med Chem (2010) 53: 7146-7155 [PMID:20860370] |
ChEMBL | Inhibition of PI3Kalpha in human PC3 cells expressing Akt1 S473D mutant assessed as phosphorylation of Akt Thr308 by immunoblotting | B | 5.74 | pEC50 | 1800 | 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/p85-alpha | B | 6.25 | pIC50 | 564 | nM | IC50 | J Med Chem (2010) 53: 7146-7155 [PMID:20860370] |
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 | 6.77 | pIC50 | 171 | nM | IC50 | J Med Chem (2010) 53: 7146-7155 [PMID:20860370] |
phosphatidylinositol 4-kinase alpha/PI4-kinase alpha subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3667] [GtoPdb: 2148] [UniProtKB: P42356] | ||||||||
ChEMBL | Inhibition of PI4Kalpha | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2010) 53: 7146-7155 [PMID:20860370] |
phosphatidylinositol 4-kinase beta/PI4-kinase beta subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3268] [GtoPdb: 2149] [UniProtKB: Q9UBF8] | ||||||||
ChEMBL | Inhibition of PI4Kbeta | B | 5.18 | pIC50 | 6680 | nM | IC50 | J Med Chem (2010) 53: 7146-7155 [PMID:20860370] |
CDC42 binding protein kinase alpha/Serine/threonine-protein kinase MRCK-A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4516] [GtoPdb: 1507] [UniProtKB: Q5VT25] | ||||||||
ChEMBL | Binding affinity to MRCKA | B | 5 | pKd | 10000 | nM | Kd | J Med Chem (2010) 53: 7146-7155 [PMID:20860370] |
mechanistic target of rapamycin kinase/Serine/threonine-protein kinase mTOR in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2842] [GtoPdb: 2109] [UniProtKB: P42345] | ||||||||
ChEMBL | Binding affinity to mTOR | B | 9.38 | pKd | 0.42 | nM | Kd | J Med Chem (2010) 53: 7146-7155 [PMID:20860370] |
ChEMBL | Inhibition of human mTOR | B | 8.36 | pIC50 | 4.32 | nM | IC50 | J Med Chem (2010) 53: 7146-7155 [PMID:20860370] |
ChEMBL | Inhibition of human mTOR complex 1 after 30 mins by FRET assay | B | 9.54 | pIC50 | 0.29 | nM | IC50 | J Med Chem (2010) 53: 7146-7155 [PMID:20860370] |
GtoPdb | Assayed using mTORC1 complex | - | 9.54 | pIC50 | 0.29 | nM | IC50 | J Med Chem (2010) 53: 7146-55 [PMID:20860370] |
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 | 8.7 | pIC50 | 2 | nM | IC50 | J Med Chem (2010) 53: 7146-7155 [PMID:20860370] |
ChEMBL | Inhibition of mTOR in p53-deficient MEF assessed as phosphorylation of S6K1 at Thr389 by immunoblotting | B | 8.7 | pEC50 | 2 | nM | EC50 | J Med Chem (2011) 54: 1473-1480 [PMID:21322566] |
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]