ChEMBL ligand: CHEMBL3948730 (RP-5264, RP5264, Tgr 1202, TGR-1202 base, TGR-1202 FREE BASE, Umbralisib)
phosphoinositide-3-kinase regulatory subunit 1/phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha/PI3-kinase p110-alpha/p85-alpha in Human [ChEMBL: CHEMBL2111367] [GtoPdb: 2503, 2153] [UniProtKB: P27986, P42336] There should be some charts here, you may need to enable JavaScript!
phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit delta/PI3-kinase p110-delta subunit in Human [ChEMBL: CHEMBL3130] [GtoPdb: 2155] [UniProtKB: O00329] There should be some charts here, you may need to enable JavaScript!
phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma/PI3-kinase p110-gamma subunit in Human [ChEMBL: CHEMBL3267] [GtoPdb: 2156] [UniProtKB: P48736] 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!
casein kinase 1 epsilon in Human [GtoPdb: 1998] [UniProtKB: P49674] 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-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 human N-terminal His-tagged PI3Kalpha/p85alpha expressed in Spodoptera frugiperda using phosphatidylinositol as substrate	B	5	pIC50	>10000	nM	IC50	Eur J Med Chem (2019) 163: 413-427 [PMID:30530193]
phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit delta/PI3-kinase p110-delta subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3130] [GtoPdb: 2155] [UniProtKB: O00329]
ChEMBL	Inhibition of human PI3Kdelta using substrate PIP2:PS and ATP incubated for 1 hr by ADP-Glo assay	B	7.32	pIC50	48.4	nM	IC50	J Med Chem (2020) 63: 13973-13993 [PMID:33180507]
ChEMBL	Homogenous Time Resolved Fluorescence (HTRF) Assay: The homogenous time resolved fluorescence (HTRF) assay allows detection of 3,4,5-triphosphate (PIP3) formed as a result of phosphorylation of phosphotidylinositol 4,5-biphosphate (PIP2) by PI3K isoforms such as alpha, beta, gamma or delta PI3K isoform activity for alpha, beta, gamma or delta was determined using a PI3K human HTRF Assay Kit (Millipore, Billerica, Mass.) with modifications. All incubations were carried out at room temperature. Briefly, 0.5 ul of 40x inhibitor (in 100% DMSO) or 100% DMSO were added to each well of a 384-well black plate (Greiner Bio-One, Monroe, N.C.) containing 14.5ul 1x reaction buffer/PIP2 (10 mM MgCl2, 5 mM DTT, 1.38 uM PIP2) mix with or without enzyme and incubated for 10 min. After the initial incubation, 5 ul/well of 400 uM ATP was added and incubated for an additional 30 minutes. Reaction was terminated by adding 5 ul/well stop solution (Millipore, Billerica, Mass.).	B	7.65	pIC50	22.33	nM	IC50	US-9150579-B2. Selective PI3K delta inhibitors (2015)
ChEMBL	Inhibition of PI3Kdelta (unknown origin) using PIP2 as substrate preincubated for 10 mins followed by ATP addition measured after 30 mins by HTRF assay	B	7.85	pIC50	14	nM	IC50	J Med Chem (2019) 62: 4783-4814 [PMID:30582813]
GtoPdb	-	-	7.86	pIC50	13.83	nM	IC50	US20140011819 A1. Novel selective pi3k delta inhibitors. (2014)
ChEMBL	Inhibition of PI3Kdelta (unknown origin)	B	8.21	pIC50	6.2	nM	IC50	Eur J Med Chem (2019) 163: 413-427 [PMID:30530193]
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 PI3Kgamma (unknown origin)	B	5.85	pIC50	1400	nM	IC50	Eur J Med Chem (2019) 163: 413-427 [PMID:30530193]
ChEMBL	Inhibition of PI3Kgamma (unknown origin) using PIP2 as substrate preincubated for 10 mins followed by ATP addition measured after 30 mins by HTRF assay	B	6.92	pIC50	>120	nM	IC50	J Med Chem (2019) 62: 4783-4814 [PMID:30582813]
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 full length recombinant N-terminal His-tagged PI3Kbeta/p85alpha expressed in baculovirus infected Sf21 insect cells	B	5	pIC50	>10000	nM	IC50	Eur J Med Chem (2019) 163: 413-427 [PMID:30530193]
casein kinase 1 epsilon in Human [GtoPdb: 1998] [UniProtKB: P49674]
GtoPdb	-	-	5.22	pEC50	6000	nM	EC50	Blood (2017) 129: 88-99 [PMID:27784673]

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]