risovalisib [Ligand Id: 12382] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL4800252 (Cyh 33, Cyh33, CYH-33, Risovalisib)
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  • phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha/PI3-kinase p110-alpha subunit in Human [ChEMBL: CHEMBL4005] [GtoPdb: 2153] [UniProtKB: P42336]
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  • phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit delta/phosphoinositide-3-kinase regulatory subunit 1/PI3-kinase p110-delta/p85-alpha in Human [ChEMBL: CHEMBL2111432] [GtoPdb: 21552503] [UniProtKB: O00329P27986]
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  • phosphoinositide-3-kinase regulatory subunit 1/phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit beta/PI3K p110 beta/p85 alpha in Human [ChEMBL: CHEMBL3038510] [GtoPdb: 25032154] [UniProtKB: P27986P42338]
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  • mechanistic target of rapamycin kinase/Serine/threonine-protein kinase mTOR in Human [ChEMBL: CHEMBL2842] [GtoPdb: 2109] [UniProtKB: P42345]
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  • Raf-1 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase RAF in Human [ChEMBL: CHEMBL1906] [GtoPdb: 2184] [UniProtKB: P04049]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL Inhibition of human ERG expressed in CHO cells at holding potential of -80 mV by patch clamp assay B 4.4 pIC50 >40000 nM IC50 Eur J Med Chem (2021) 209: 112913-112913 [PMID:33109399]
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 human PI3Kalpha using PIP2 as substrate in presence of ATP measured after 30 mins by HTRF assay B 8.23 pIC50 5.9 nM IC50 Eur J Med Chem (2021) 209: 112913-112913 [PMID:33109399]
GtoPdb - - 8.23 pIC50 5.9 nM IC50 Eur J Med Chem (2021) 209: 112913 [PMID:33109399]
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: 21552503] [UniProtKB: O00329P27986]
ChEMBL Inhibition of human PI3K p110delta/p85alpha using PIP2 as substrate in presence of ATP measured after 40 mins by HTRF assay B 7.1 pIC50 78.7 nM IC50 Eur J Med Chem (2021) 209: 112913-112913 [PMID:33109399]
phosphoinositide-3-kinase regulatory subunit 1/phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit beta/PI3K p110 beta/p85 alpha in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3038510] [GtoPdb: 25032154] [UniProtKB: P27986P42338]
ChEMBL Inhibition of human PI3K p110beta/p85alpha using PIP2 as substrate incubated for 40 mins in presence of ATP measured after 40 mins by HTRF assay B 6.22 pIC50 598.1 nM IC50 Eur J Med Chem (2021) 209: 112913-112913 [PMID:33109399]
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 human full length recombinant mTOR in presence of [gamma33P-ATP] by radiometric scintillation counting analysis B 5 pIC50 >10000 nM IC50 Eur J Med Chem (2021) 209: 112913-112913 [PMID:33109399]
Raf-1 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase RAF in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1906] [GtoPdb: 2184] [UniProtKB: P04049]
ChEMBL Inhibition of human recombinant c-Raf Y340D/Y341D mutant (306 to end residues) using inactive MEK1 as substrate incubated for 40 mins in presence of [gamma33P-ATP] by radiometric scintillation counting analysis B 6 pIC50 1000 nM IC50 Eur J Med Chem (2021) 209: 112913-112913 [PMID:33109399]

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]