ChEMBL ligand: CHEMBL1972466
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 human full length p110alpha/p85alpha using PIP2 as substrate after 30 mins in presence of ATP at 2xKm concentration by TR-FRET assay	B	5.12	pIC50	7600	nM	IC50	ACS Med Chem Lett (2020) 11: 1236-1243 [PMID:32551006]
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 N-terminal ploy-His-tagged human PI3Kalpha expressed in baculovirus-infected sf9 cells using PI(4,5)P2 as substrate after 15 mins by HTRF assay	B	5	pIC50	10000	nM	IC50	J Med Chem (2014) 57: 903-920 [PMID:24387221]
ChEMBL	Inhibition of N-terminus poly-His tagged human PI3Kalpha expressed in baculovirus infected insect sf9 cells coexpressing p85alpha using PI(4,5)P2 as substrate preincubated with compound for 15 mins measured after 10 mins by HTRF assay	B	5	pIC50	>10000	nM	IC50	J Med Chem (2012) 55: 4788-4805 [PMID:22524426]
ChEMBL	Inhibition of human recombinant PI3Kalpha assessed as PIP3 production by AlphaScreen assay	B	5.24	pIC50	5800	nM	IC50	Bioorg Med Chem Lett (2014) 24: 3936-3943 [PMID:25042253]
ChEMBL	Inhibition of human recombinant His6-tagged PI3K p110alpha expressed in baculovirus using DiC8-PI(4,5)P2 as substrate after 20 mins by AlphaScreen assay	B	5.24	pIC50	5700	nM	IC50	Bioorg Med Chem Lett (2012) 22: 6665-6670 [PMID:23010274]
ChEMBL	Inhibition of N-terminal His-tagged human p110alpha expressed in Sf9 cells co-expressing p85alpha regulatory subunit using phosphatidylinositol substrate and [gamma-33P]-ATP by basic thin layer chromatography technique based lipid kinase assay	B	6	pIC50	1000	nM	IC50	Bioorg Med Chem (2015) 23: 3796-3808 [PMID:25890698]
ChEMBL	Inhibition of PI3K p110alpha (unknown origin)	B	6	pIC50	>1000	nM	IC50	J Med Chem (2015) 58: 41-71 [PMID:25387153]
ChEMBL	Inhibition of human PI3Kalpha-mediated Akt phosphorylation at Ser473 residue expressed in human H460 cells after 0.5 to 2 hrs by Western blot analysis	B	6	pIC50	>1000	nM	IC50	J Med Chem (2012) 55: 4788-4805 [PMID:22524426]
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]
ChEMBL	Inhibition of PI3K p110beta (unknown origin)	B	5.7	pIC50	2000	nM	IC50	J Med Chem (2015) 58: 41-71 [PMID:25387153]
ChEMBL	Inhibition of PI3Kbeta (unknown origin) incubated for 60 mins in the presence of ATP by Kinase-Glo luminescence assay	B	7.19	pIC50	65	nM	IC50	Bioorg Med Chem (2022) 69: 116832-116832 [PMID:35752141]
ChEMBL	Inhibition of PI3Kbeta (unknown origin) expressed in Escherichia coli-infected fall armyworm sf21 cells co-expressing p85 by kinase-glo luminescence assay	B	7.28	pIC50	52	nM	IC50	Eur J Med Chem (2016) 122: 339-351 [PMID:27387421]
ChEMBL	Inhibition of human recombinant PI3Kbeta assessed as PIP3 production by AlphaScreen assay	B	7.31	pIC50	49	nM	IC50	Bioorg Med Chem Lett (2014) 24: 3936-3943 [PMID:25042253]
ChEMBL	Inhibition of human recombinant His6-tagged PI3K p110beta expressed in baculovirus using DiC8-PI(4,5)P2 as substrate after 20 mins by AlphaScreen assay	B	7.31	pIC50	49	nM	IC50	Bioorg Med Chem Lett (2012) 22: 6665-6670 [PMID:23010274]
ChEMBL	Inhibition of N-terminal ploy-His-tagged human PI3Kbeta expressed in baculovirus-infected sf21 cells using PI(4,5)P2 as substrate after 15 mins by HTRF assay	B	7.52	pIC50	30	nM	IC50	J Med Chem (2014) 57: 903-920 [PMID:24387221]
ChEMBL	Inhibition of N-terminus poly-His tagged human PI3Kbeta expressed in baculovirus infected insect S21 cells coexpressing p85alpha using PI(4,5)P2 as substrate preincubated with compound for 15 mins measured after 10 mins by HTRF assay	B	7.52	pIC50	30	nM	IC50	J Med Chem (2012) 55: 4788-4805 [PMID:22524426]
ChEMBL	Inhibition of PI3Kbeta in human MAD-MB-468 cells assessed as inhibition of Ser473 Akt phosphorylation by cellular potency assay	B	7.66	pIC50	22	nM	IC50	Bioorg Med Chem Lett (2014) 24: 3928-3935 [PMID:24992874]
ChEMBL	Inhibition of human PI3Kbeta-mediated Akt phosphorylation at Ser473 residue expressed in mouse MEF-3T3 cells after 0.5 to 2 hrs by Western blot analysis	B	7.96	pIC50	11	nM	IC50	J Med Chem (2012) 55: 4788-4805 [PMID:22524426]
ChEMBL	Inhibition of PI3Kbeta-mediated Akt phosphorylation at S473 in PTEN-deficient human PC3 cells after 0.5 to 2 hrs by Immunoblotting assay	B	8	pIC50	10	nM	IC50	J Med Chem (2014) 57: 903-920 [PMID:24387221]
ChEMBL	Inhibition of human PI3Kbeta-mediated Akt phosphorylation at Ser473 residue expressed in PTEN-deficient human PC3 cells by chemiluminescence assay	B	8	pIC50	10	nM	IC50	J Med Chem (2012) 55: 4788-4805 [PMID:22524426]
GtoPdb	-	-	8.3	pIC50	5	nM	IC50	Nat Med (2005) 11: 507-14 [PMID:15834429]
ChEMBL	Inhibition of N-terminal His-tagged human p110beta expressed in Sf9 cells co-expressing p85alpha regulatory subunit using phosphatidylinositol substrate and [gamma-33P]-ATP by basic thin layer chromatography technique based lipid kinase assay	B	8.4	pIC50	4	nM	IC50	Bioorg Med Chem (2015) 23: 3796-3808 [PMID:25890698]
ChEMBL	Inhibition of human PI3Kbeta-mediated Akt phosphorylation at T308 residue expressed in PTEN-deficient human PC3 cells after 2 hrs by Western blot analysis	B	8.52	pIC50	3	nM	IC50	J Med Chem (2012) 55: 4788-4805 [PMID:22524426]
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 p110delta catalytic subunit/p85alpha using PIP2 as substrate after 30 mins in presence of ATP at 2xKm concentration by TR-FRET assay	B	6.3	pIC50	500	nM	IC50	ACS Med Chem Lett (2020) 11: 1236-1243 [PMID:32551006]
GtoPdb	-	-	7	pIC50	100	nM	IC50	Nat Med (2005) 11: 507-14 [PMID:15834429]
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 poly-His tagged human PI3Kdelta expressed in baculovirus infected insect sf9 cells coexpressing p85alpha using PI(4,5)P2 as substrate preincubated with compound for 15 mins measured after 10 mins by HTRF assay	B	6.07	pIC50	851	nM	IC50	J Med Chem (2012) 55: 4788-4805 [PMID:22524426]
ChEMBL	Inhibition of N-terminal ploy-His-tagged human PI3Kdelta expressed in baculovirus-infected sf9 cells using PI(4,5)P2 as substrate after 15 mins by HTRF assay	B	6.07	pIC50	851	nM	IC50	J Med Chem (2014) 57: 903-920 [PMID:24387221]
ChEMBL	Inhibition of human PI3Kdelta-mediated Akt phosphorylation at Ser473 residue expressed in mouse MEF-3T3 cells after 0.5 to 2 hrs by Western blot analysis	B	6.6	pIC50	252	nM	IC50	J Med Chem (2012) 55: 4788-4805 [PMID:22524426]
ChEMBL	Inhibition of N-terminal His-tagged human p110delta expressed in Sf9 cells co-expressing p85alpha regulatory subunit using phosphatidylinositol substrate and [gamma-33P]-ATP by basic thin layer chromatography technique based lipid kinase assay	B	6.85	pIC50	140	nM	IC50	Bioorg Med Chem (2015) 23: 3796-3808 [PMID:25890698]
GtoPdb	-	-	7	pIC50	100	nM	IC50	Nat Med (2005) 11: 507-14 [PMID:15834429]
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 N-terminus poly-His tagged human PI3Kgamma expressed in baculovirus infected insect sf9 cells using PI(4,5)P2 as substrate preincubated with compound for 15 mins measured after 10 mins by HTRF assay	B	5	pIC50	>10000	nM	IC50	J Med Chem (2012) 55: 4788-4805 [PMID:22524426]
ChEMBL	Inhibition of C-terminal ploy-His-tagged human PI3Kgamma expressed in baculovirus-infected sf9 cells using PI(4,5)P2 as substrate after 15 mins by HTRF assay	B	5	pIC50	10000	nM	IC50	J Med Chem (2014) 57: 903-920 [PMID:24387221]
ChEMBL	Inhibition of human full length p110gamma using PIP2 as substrate after 30 mins in presence of ATP at 2xKm concentration by TR-FRET assay	B	5	pIC50	>10000	nM	IC50	ACS Med Chem Lett (2020) 11: 1236-1243 [PMID:32551006]
ChEMBL	Inhibition of human PI3Kgamma-mediated Akt phosphorylation at Ser473 residue expressed in mouse RAW264.7 cells after 0.5 to 2 hrs by Western blot analysis	B	6	pIC50	>1000	nM	IC50	J Med Chem (2012) 55: 4788-4805 [PMID:22524426]
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 recombinant human full-length N-terminal His6-tagged p110beta/human recombinant full-length untagged p85alpha expressed in baculovirus infected Sf21 insect cells using PIP2 as substrate after 30 mins in presence of ATP at 2xKm concentration by TR-FRET assay	B	7.2	pIC50	63	nM	IC50	ACS Med Chem Lett (2020) 11: 1236-1243 [PMID:32551006]
GtoPdb	-	-	8.3	pIC50	5	nM	IC50	Nat Med (2005) 11: 507-14 [PMID:15834429]

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]