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	Affinity Phenotypic Cellular interaction (Inhibition of pAkt in human lymphoma and leukemia cell lines) EUB0000696a PIK3CD	B	6	pIC50	<1000	nM	IC50	Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL	Inhibition of PI3Kdelta (unknown origin) using PIP2:PS as substrate in presence of ATP measured after 1 hr by ADP-Glo assay	B	6.5	pIC50	316	nM	IC50	J Med Chem (2023) 66: 11905-11926 [PMID:37606563]
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 P13Kdelta (unknown origin)	B	7.66	pIC50	22	nM	IC50	Eur J Med Chem (2023) 246: 114971-114971 [PMID:36462440]
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]
ChEMBL	Affinity Biochemical interaction (Enzymatic inhibition assay) EUB0000696a PIK3CD	B	7.85	pIC50	14	nM	IC50	Affinity Biochemical Literature for EUbOPEN Chemogenomics Library wave 3
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 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]