ChEMBL ligand: CHEMBL3039502 (Duvelisib, INK-1197, IPI-145)
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 alpha/PI3-kinase p110-alpha subunit 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 beta/PI3-kinase p110-beta subunit in Human [ChEMBL: CHEMBL3145] [GtoPdb: 2154] [UniProtKB: P42338] 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!
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!

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 N-terminal His6-tagged recombinant full-length human p110alpha/untagged recombinant full length human p85alpha expressed in baculovirus infected Sf21 cells using phosphatidylinositol as substrate in presence of gamma-32P-ATP after 5 mins by thin layer chromatographic method	B	5	pIC50	<10000	nM	IC50	US-8193182-B2. Substituted isoquinolin-1(2H)-ones, and methods of use thereof (2012)
GtoPdb	-	-	5.8	pIC50	1602	nM	IC50	Chem Biol (2013) 20: 1364-74 [PMID:24211136]
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 PI3Kalpha (unknown origin)	B	5.8	pIC50	1602	nM	IC50	Eur J Med Chem (2019) 163: 413-427 [PMID:30530193]
GtoPdb	-	-	5.8	pIC50	1602	nM	IC50	Chem Biol (2013) 20: 1364-74 [PMID:24211136]
phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit beta/PI3-kinase p110-beta subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3145] [GtoPdb: 2154] [UniProtKB: P42338]
GtoPdb	-	-	7.07	pIC50	85	nM	IC50	Chem Biol (2013) 20: 1364-74 [PMID:24211136]
ChEMBL	Inhibition of PI3Kbeta (unknown origin)	B	7.07	pIC50	85	nM	IC50	Eur J Med Chem (2019) 163: 413-427 [PMID:30530193]
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 N-terminal His6-tagged recombinant full-length human p110delta/untagged recombinant full length p85alpha expressed in baculovirus infected Sf21 cells using phosphatidylinositol as substrate in presence of gamma-32P-ATP after 5 mins by thin layer chromatographic method	B	7	pIC50	<100	nM	IC50	US-8193182-B2. Substituted isoquinolin-1(2H)-ones, and methods of use thereof (2012)
GtoPdb	-	-	8.6	pIC50	2.5	nM	IC50	Chem Biol (2013) 20: 1364-74 [PMID:24211136]
ChEMBL	Inhibition of PI3KCdelta/PIK3R1 (unknown origin)	B	8.64	pIC50	2.3	nM	IC50	Eur J Med Chem (2018) 158: 405-413 [PMID:30237123]
ChEMBL	Inhibition of N-terminal His6-tagged recombinant full length human p110delta/untagged recombinant full length human p85alpha expressed in baculovirus infected Sf21 insect cells using PIP2 as substrate measured after 80 mins by transcreener fluorescence polarization assay	B	9	pIC50	1	nM	IC50	J Med Chem (2019) 62: 4936-4948 [PMID:31033293]
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 PI3Kdelta in human whole blood assessed as reduction in fMLP-stimulated CD63 expression in basophils preincubated for 30 mins followed by fMLP stimulation	B	5.66	pIC50	2206	nM	IC50	J Med Chem (2019) 62: 4936-4948 [PMID:31033293]
ChEMBL	Inhibition of PI3Kdelta (unknown origin)	B	7.57	pIC50	27	nM	IC50	Eur J Med Chem (2019) 163: 413-427 [PMID:30530193]
ChEMBL	Inhibition of PI3Kdelta in human whole blood assessed as reduction in anti-IgM-stimulated CD69 expression on B-cells preincubated for 60 mins followed by anti-IgM stimulation and measured after overnight incubation by flow cytometry	B	7.85	pIC50	14	nM	IC50	J Med Chem (2019) 62: 4936-4948 [PMID:31033293]
GtoPdb	-	-	8.6	pIC50	2.5	nM	IC50	Chem Biol (2013) 20: 1364-74 [PMID:24211136]
ChEMBL	Inhibition of N-terminal His6-tagged recombinant full length human PI3Kdelta expressed in baculovirus infected Sf21 insect cells incubated for 30 mins by HTRF assay	B	8.6	pIC50	2.5	nM	IC50	J Med Chem (2022) 65: 9893-9917 [PMID:35831917]
ChEMBL	Inhibition of PI3Kdelta in human Raji cells	B	8.6	pIC50	2.5	nM	IC50	J Med Chem (2019) 62: 4783-4814 [PMID:30582813]
ChEMBL	Inhibition of p110delta (unknown origin)	B	8.6	pIC50	2.5	nM	IC50	Eur J Med Chem (2021) 214: 113218-113218 [PMID:33540357]
ChEMBL	Inhibition of PI3Kdelta in human Ramos cells assessed as reduction in antihuman IgM-stimulated AKT phosphorylation at Ser473 residue preincubated for 60 mins followed by antihuman IgM stimulation and measured after 15 mins	B	9	pIC50	1	nM	IC50	J Med Chem (2019) 62: 4936-4948 [PMID:31033293]
ChEMBL	Inhibition of human PI3Kdelta (R108 to Q1044 residues) expressed in mammalian expression system incubated for 60 mins by ADAPTA assay	B	9.3	pIC50	<0.5	nM	IC50	ACS Med Chem Lett (2016) 7: 908-912 [PMID:27774127]
ChEMBL	Inhibition of P13Kdelta (unknown origin)	B	9.62	pIC50	0.24	nM	IC50	Eur J Med Chem (2023) 246: 114971-114971 [PMID:36462440]
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 recombinant human C-terminal His6-tagged p110gamma expressed in insect cells using phosphatidylinositol as substrate in presence of gamma-32P-ATP after 5 mins by thin layer chromatographic method	B	7	pIC50	<100	nM	IC50	US-8193182-B2. Substituted isoquinolin-1(2H)-ones, and methods of use thereof (2012)
ChEMBL	Inhibition of P13Kgamma (unknown origin)	B	7.3	pIC50	50	nM	IC50	Eur J Med Chem (2023) 246: 114971-114971 [PMID:36462440]
ChEMBL	Inhibition of p110gamma (unknown origin)	B	7.56	pIC50	27.4	nM	IC50	Eur J Med Chem (2021) 214: 113218-113218 [PMID:33540357]
ChEMBL	Inhibition of N-terminal His6-tagged recombinant full length human PI3Kgamma expressed in baculovirus infected Sf21 insect cells incubated for 30 mins by HTRF assay	B	7.57	pIC50	27	nM	IC50	J Med Chem (2022) 65: 9893-9917 [PMID:35831917]
ChEMBL	Inhibition of PI3Kgamma in human Raji cells	B	7.57	pIC50	27	nM	IC50	J Med Chem (2019) 62: 4783-4814 [PMID:30582813]
GtoPdb	-	-	7.57	pIC50	27	nM	IC50	Chem Biol (2013) 20: 1364-74 [PMID:24211136]
ChEMBL	Inhibition of PI3Kgamma in human whole blood assessed as reduction in anti-IgE-stimulated CD63 expression in basophils preincubated for 30 mins followed by anti-IgE stimulation	B	7.82	pIC50	15	nM	IC50	J Med Chem (2019) 62: 4936-4948 [PMID:31033293]
ChEMBL	Inhibition of PI3KCgamma (unknown origin)	B	7.92	pIC50	12	nM	IC50	Eur J Med Chem (2018) 158: 405-413 [PMID:30237123]
ChEMBL	Inhibition of human PI3Kgamma (S144 to A1102 residues) expressed in mammalian expression system incubated for 60 mins by ADAPTA assay	B	8.54	pIC50	2.9	nM	IC50	ACS Med Chem Lett (2016) 7: 908-912 [PMID:27774127]
ChEMBL	Inhibition of PI3Kgamma (unknown origin)	B	8.6	pIC50	2.5	nM	IC50	Eur J Med Chem (2019) 163: 413-427 [PMID:30530193]
ChEMBL	Inhibition of recombinant human full-length His-tagged PI3K p110gamma expressed in baculovirus expression system using PIP2 as substrate measured after 80 mins by transcreener fluorescence polarization assay	B	8.7	pIC50	2	nM	IC50	J Med Chem (2019) 62: 4936-4948 [PMID:31033293]
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 N-terminal His6-tagged recombinant full-length human p110beta/untagged recombinant full length p85alpha expressed in baculovirus infected Sf21 cells using phosphatidylinositol as substrate in presence of gamma-32P-ATP after 5 mins by thin layer chromatographic method	B	6	pIC50	<1000	nM	IC50	US-8193182-B2. Substituted isoquinolin-1(2H)-ones, and methods of use thereof (2012)
GtoPdb	-	-	7.07	pIC50	85	nM	IC50	Chem Biol (2013) 20: 1364-74 [PMID:24211136]

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]