ChEMBL ligand: CHEMBL4800252 (Cyh 33, Cyh33, CYH-33, Risovalisib)
phosphoinositide-3-kinase regulatory subunit 1/Phosphatidylinositol 3-kinase regulatory subunit alpha in Human [ChEMBL: CHEMBL2506] [GtoPdb: 2503] [UniProtKB: P27986] There should be some charts here, you may need to enable JavaScript!
phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha/Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform in Human [ChEMBL: CHEMBL4005] [GtoPdb: 2153] [UniProtKB: P42336] There should be some charts here, you may need to enable JavaScript!
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: 2155, 2503] [UniProtKB: O00329, P27986] There should be some charts here, you may need to enable JavaScript!
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: 2503, 2154] [UniProtKB: P27986, P42338] There should be some charts here, you may need to enable JavaScript!
Raf-1 proto-oncogene, serine/threonine kinase/RAF proto-oncogene serine/threonine-protein kinase in Human [ChEMBL: CHEMBL1906] [GtoPdb: 2184] [UniProtKB: P04049] There should be some charts here, you may need to enable JavaScript!
mechanistic target of rapamycin kinase/Serine/threonine-protein kinase mTOR in Human [ChEMBL: CHEMBL2842] [GtoPdb: 2109] [UniProtKB: P42345] There should be some charts here, you may need to enable JavaScript!
Kv11.1/Voltage-gated inwardly rectifying potassium channel KCNH2 in Human [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] 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
phosphoinositide-3-kinase regulatory subunit 1/Phosphatidylinositol 3-kinase regulatory subunit alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2506] [GtoPdb: 2503] [UniProtKB: P27986]
ChEMBL	Inhibition on PI3K Kinase Activity: The activity of purified kinase was detected with Kinase-Glo® Plus kinase luminescent assay by measuring the amount of the remaining Kinase in the solution after the kinase reaction was completed. Kinase reaction was performed in a 384-well white plate (Greiner), 1 μL of tested compound or control DMSO was added into each well containing 5 μL reaction buffer [10 mM Tris-HCl pH 7.5, 50 mM NaCl, 3 mM MgCl2.1 mM DTT (dithiothreitol), 0.05% CHAPS (3-[(3-Cholamidopropyl)dimethylammonio]-1-propanesulfonate, 3-(3-cholaminopropyl)-dimethylamino-1-propanesulfonic acid), and the reaction buffer was supplemented with 12 μM of substrate, D-myo-Phosphatidylinositol-4,5-bisphosphate (4,5-phosphatidyl inositol diphosphate) and 2 μM ATP (adenosine triphosphate). And then 4 μL reaction buffer containing 62.5 nM PI3Kα or non-PI3Kα control was added to initiate the kinase reaction. After reaction was performed for 1 hour at room temperature, 10 μL of Kinase Glo-Plus mixture was added and incubated for 1 hour to quench the reaction. The chemiluminescence value was detected with EnVision 2104 multifunctional microplate reader (Perkinelmer).	B	8.55	pIC50	2.84	nM	IC50	US-9724352-B2. Pyrrolo[2,1-F[1,2,4]triazine compounds, preparation methods and applications thereof (2017)
phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha/Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform 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]
Raf-1 proto-oncogene, serine/threonine kinase/RAF proto-oncogene serine/threonine-protein kinase 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]
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]
Kv11.1/Voltage-gated inwardly rectifying potassium channel KCNH2 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]

ChEMBL data shown on this page come from version 36:

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]