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ChEMBL ligand: CHEMBL4800252 (Cyh 33, Cyh33, CYH-33, Risovalisib) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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: 2155, 2503] [UniProtKB: O00329, P27986] | ||||||||
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: 2503, 2154] [UniProtKB: P27986, P42338] | ||||||||
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]